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Book
1 online resource Digital: text file; PDF.
  • Preface-- Chanelling drug discovery-- Chanome old and new-- High throughput screening-- Automated electrophysiology-- Structure/crystallization/modeling studies-- Toxins - does nature do ion channel drug discovery better than us? Structure and function of Sodium Channels, pharmacophores and binding sites-- AMPA modulators - a case history-- Inhibition of the epithelial sodium channel (ENaC) as a therapeutic approach to respiratory disease-- CFTR channel modulation as a therapeutic approach-- TRPs are a pain: a case history on TRPV1 antagonist development-- The Retigabine story - the M current to therapeutically useful anticonvulsant-- Icrac and Orai - a STIMulating channel-- hERG past, present and future? Antibodies as ion channel modulators-- Summary and the future-- Index.
  • (source: Nielsen Book Data)
Ion channel drug discovery is a rapidly evolving field fuelled by recent, but significant, advances in our understanding of ion channel function combined with enabling technologies such as automated electrophysiology. The resurgent interest in this target class by both pharmaceutical and academic scientists was clearly highlighted by the over-subscribed RSC/BPS 'Ion Channels as Therapeutic Targets' symposium in February 2009. This book builds on the platform created by that meeting, covering themes including advances in screening technology, ion channel structure and modelling and up-to-date case histories of the discovery of modulators of a range of channels, both voltage-gated and non-voltage-gated channels. The editors have built an extensive network of contacts in the field through their first-hand scientific experience, collaborations and conference participation and the organisation of the meeting at Novartis, Horsham, increased the network enabling the editors to draw on the experience of eminent researchers in the field. Interest and investment in ion channel modulation in both industrial and academic settings continues to grow as new therapeutic opportunities are identified and realised for ion channel modulation. This book provides a reference text by covering a combination of recent advances in the field, from technological and medicinal chemistry perspectives, as well as providing an introduction to the new 'ion channel drug discoverer'. The book has contributions from highly respected academic researchers, industrial researchers at the cutting edge of drug discovery and experts in enabling technology. This combination provides a complete picture of the field of interest to a wide range of readers.
(source: Nielsen Book Data)
  • Preface-- Chanelling drug discovery-- Chanome old and new-- High throughput screening-- Automated electrophysiology-- Structure/crystallization/modeling studies-- Toxins - does nature do ion channel drug discovery better than us? Structure and function of Sodium Channels, pharmacophores and binding sites-- AMPA modulators - a case history-- Inhibition of the epithelial sodium channel (ENaC) as a therapeutic approach to respiratory disease-- CFTR channel modulation as a therapeutic approach-- TRPs are a pain: a case history on TRPV1 antagonist development-- The Retigabine story - the M current to therapeutically useful anticonvulsant-- Icrac and Orai - a STIMulating channel-- hERG past, present and future? Antibodies as ion channel modulators-- Summary and the future-- Index.
  • (source: Nielsen Book Data)
Ion channel drug discovery is a rapidly evolving field fuelled by recent, but significant, advances in our understanding of ion channel function combined with enabling technologies such as automated electrophysiology. The resurgent interest in this target class by both pharmaceutical and academic scientists was clearly highlighted by the over-subscribed RSC/BPS 'Ion Channels as Therapeutic Targets' symposium in February 2009. This book builds on the platform created by that meeting, covering themes including advances in screening technology, ion channel structure and modelling and up-to-date case histories of the discovery of modulators of a range of channels, both voltage-gated and non-voltage-gated channels. The editors have built an extensive network of contacts in the field through their first-hand scientific experience, collaborations and conference participation and the organisation of the meeting at Novartis, Horsham, increased the network enabling the editors to draw on the experience of eminent researchers in the field. Interest and investment in ion channel modulation in both industrial and academic settings continues to grow as new therapeutic opportunities are identified and realised for ion channel modulation. This book provides a reference text by covering a combination of recent advances in the field, from technological and medicinal chemistry perspectives, as well as providing an introduction to the new 'ion channel drug discoverer'. The book has contributions from highly respected academic researchers, industrial researchers at the cutting edge of drug discovery and experts in enabling technology. This combination provides a complete picture of the field of interest to a wide range of readers.
(source: Nielsen Book Data)
Book
1 online resource (xi, 240 pages) : illustrations (some color).
  • Preface.- List of Contributors.- Engineering G Protein-Coupled Receptors for Drug Design-- M. Congreve et al.- Structural Insights into Activation and Allosteric Modulation of G Protein-Coupled Receptors-- A.C. Kruse.- Epigenetic Drug Discovery-- Chun-wa Chung.- Crystallography and Biopharmaceuticals-- R. Pauptit.- Structural Chemistry and Molecular Modeling in the Design of DPP4 Inhibitors-- G. Scapin.- Considerations for Structure-Based Drug Design Targeting HIV-1 Reverse Transcriptase-- E. Arnold et al.-Protein-Ligand Interactions as the Basis for Drug Action-- G. Klebe.- The Protein Data Bank: Overview and Tools for Drug Discovery-- H. M. Berman et al.- Small Molecule Crystal Structures in Drug Discovery-- C. Groom.- Protein Aggregation and its Prediction-- R. Grana-Montes, S.Ventura.- Importance of Protonation States for the Binding of Ligands to Pharmaceutical Targets-- A. Podjarny, E. Howard.- Protein-Protein Interactions: Structures and Druggability-- D.B. Ascher et al.- Achieving High Quality Ligand Chemistry in Protein-Ligand Crystal Structures for Drug Design-- O.S. Smart, G. Bricogne.- Molecular Obesity, Potency and Other Addictions in Drug Discovery-- M.M. Hann.- Adventures in Small Molecule Fragment Screening by X-ray Crystallography for Drug Discovery-- J.D. Bauman et al.- Structure-Based Drug Design to Perturb Function of a tRNA-Modifying Enzyme by Active Site and Protein-Protein Interface Inhibition-- G. Klebe.- Molecular Interaction Analysis for Discovery of Drugs Targeting Enzymes and for Resolving Biological Function-- U.H. Danielson.
  • (source: Nielsen Book Data)
The present work offers a snapshot of the state-of-the-art of crystallographic, analytical, and computational methods used in modern drug design and development. Topics discussed include: drug design against complex systems (membrane proteins, cell surface receptors, epigenetic targets, and ribosomes); modulation of protein-protein interactions; the impact of small molecule structures in drug discovery and the application of concepts such as molecular geometry, conformation, and flexibility to drug design; methodologies for understanding and characterizing protein states and protein-ligand interactions during the drug design process; and monoclonal antibody therapies. These methods are illustrated through their application to problems of medical and biological significance, such as viral and bacterial infections, diabetes, autoimmune disease, and CNS diseases. As approaches to drug discovery have changed over time, so have the methodologies used to solve the varied, new, and difficult problems encountered in drug discovery. In recent years we have seen great progress in the fields of genetics, biology, chemistry, and medicine, but there are still many unmet medical needs, from bacterial infections to cancer to chronic maladies, that require novel, different, or better therapies. This work will be of interest to researchers and policy makers interested in the latest developments in drug design.
(source: Nielsen Book Data)
  • Preface.- List of Contributors.- Engineering G Protein-Coupled Receptors for Drug Design-- M. Congreve et al.- Structural Insights into Activation and Allosteric Modulation of G Protein-Coupled Receptors-- A.C. Kruse.- Epigenetic Drug Discovery-- Chun-wa Chung.- Crystallography and Biopharmaceuticals-- R. Pauptit.- Structural Chemistry and Molecular Modeling in the Design of DPP4 Inhibitors-- G. Scapin.- Considerations for Structure-Based Drug Design Targeting HIV-1 Reverse Transcriptase-- E. Arnold et al.-Protein-Ligand Interactions as the Basis for Drug Action-- G. Klebe.- The Protein Data Bank: Overview and Tools for Drug Discovery-- H. M. Berman et al.- Small Molecule Crystal Structures in Drug Discovery-- C. Groom.- Protein Aggregation and its Prediction-- R. Grana-Montes, S.Ventura.- Importance of Protonation States for the Binding of Ligands to Pharmaceutical Targets-- A. Podjarny, E. Howard.- Protein-Protein Interactions: Structures and Druggability-- D.B. Ascher et al.- Achieving High Quality Ligand Chemistry in Protein-Ligand Crystal Structures for Drug Design-- O.S. Smart, G. Bricogne.- Molecular Obesity, Potency and Other Addictions in Drug Discovery-- M.M. Hann.- Adventures in Small Molecule Fragment Screening by X-ray Crystallography for Drug Discovery-- J.D. Bauman et al.- Structure-Based Drug Design to Perturb Function of a tRNA-Modifying Enzyme by Active Site and Protein-Protein Interface Inhibition-- G. Klebe.- Molecular Interaction Analysis for Discovery of Drugs Targeting Enzymes and for Resolving Biological Function-- U.H. Danielson.
  • (source: Nielsen Book Data)
The present work offers a snapshot of the state-of-the-art of crystallographic, analytical, and computational methods used in modern drug design and development. Topics discussed include: drug design against complex systems (membrane proteins, cell surface receptors, epigenetic targets, and ribosomes); modulation of protein-protein interactions; the impact of small molecule structures in drug discovery and the application of concepts such as molecular geometry, conformation, and flexibility to drug design; methodologies for understanding and characterizing protein states and protein-ligand interactions during the drug design process; and monoclonal antibody therapies. These methods are illustrated through their application to problems of medical and biological significance, such as viral and bacterial infections, diabetes, autoimmune disease, and CNS diseases. As approaches to drug discovery have changed over time, so have the methodologies used to solve the varied, new, and difficult problems encountered in drug discovery. In recent years we have seen great progress in the fields of genetics, biology, chemistry, and medicine, but there are still many unmet medical needs, from bacterial infections to cancer to chronic maladies, that require novel, different, or better therapies. This work will be of interest to researchers and policy makers interested in the latest developments in drug design.
(source: Nielsen Book Data)
Book
1 online resource
  • Part I: General Aspects. Serendipitous Target-Based Drug Discoveries / János Fischer, David P Rotella
  • Drug Discoveries and Molecular Mechanism of Action / David C Swinney
  • Part II: Drug Class. Insulin Analogs - Improving the Therapy of Diabetes / John M Beals
  • Part III: Case Histories. The Discovery of Stendra (Avanafil) for the Treatment of Erectile Dysfunction / Koichiro Yamada, Toshiaki Sakamoto, Kenji Omori, Kohei Kikkawa
  • Dapagliflozin, A Selective SGLT2 Inhibitor for Treatment of Diabetes / William N Washburn
  • Elvitegravir, A New HIV-1 Integrase Inhibitor for Antiretroviral Therapy / Hisashi Shinkai
  • Discovery of Linagliptin for the Treatment of Type 2 Diabetes Mellitus / Matthias Eckhardt, Thomas Klein, Herbert Nar, Sandra Thiemann
  • The Discovery of Alimta (Pemetrexed) / Edward C Taylor
  • Perampanel: A Novel, Noncompetitive AMPA Receptor Antagonist for the Treatment of Epilepsy / Shigeki Hibi
  • Discovery and Development of Telaprevir (Incivek): A Protease Inhibitor to Treat Hepatitis C Infection / Bhisetti G Rao, Mark Murcko, Mark J Tebbe, Ann D Kwong
  • Antibody-Drug Conjugates: Design and Development of Trastuzumab Emtansine (T-DM1) / Sandhya Girish, Gail D Lewis Phillips, Fredric S Jacobson, Jagath R Junutula, Ellie Guardino.
  • Part I: General Aspects. Serendipitous Target-Based Drug Discoveries / János Fischer, David P Rotella
  • Drug Discoveries and Molecular Mechanism of Action / David C Swinney
  • Part II: Drug Class. Insulin Analogs - Improving the Therapy of Diabetes / John M Beals
  • Part III: Case Histories. The Discovery of Stendra (Avanafil) for the Treatment of Erectile Dysfunction / Koichiro Yamada, Toshiaki Sakamoto, Kenji Omori, Kohei Kikkawa
  • Dapagliflozin, A Selective SGLT2 Inhibitor for Treatment of Diabetes / William N Washburn
  • Elvitegravir, A New HIV-1 Integrase Inhibitor for Antiretroviral Therapy / Hisashi Shinkai
  • Discovery of Linagliptin for the Treatment of Type 2 Diabetes Mellitus / Matthias Eckhardt, Thomas Klein, Herbert Nar, Sandra Thiemann
  • The Discovery of Alimta (Pemetrexed) / Edward C Taylor
  • Perampanel: A Novel, Noncompetitive AMPA Receptor Antagonist for the Treatment of Epilepsy / Shigeki Hibi
  • Discovery and Development of Telaprevir (Incivek): A Protease Inhibitor to Treat Hepatitis C Infection / Bhisetti G Rao, Mark Murcko, Mark J Tebbe, Ann D Kwong
  • Antibody-Drug Conjugates: Design and Development of Trastuzumab Emtansine (T-DM1) / Sandhya Girish, Gail D Lewis Phillips, Fredric S Jacobson, Jagath R Junutula, Ellie Guardino.
Book
1 online resource (xiii, 550 pages) : illustrations (some color).
  • 1 Hybrid QM/MM Methods: Treating Electronic Phenomena in Very Large Molecular Systems.- 2 Structure, Thermodynamics and Energetics of Drug-DNA Interactions: Computer Modeling and Experiment.- 3 Formation of DNA Lesions, Its Prevention and Repair.- 4 DNA dependent DNA Polymerases as Targets for Low-Weight Molecular Inhibitors: State of Art and Prospects of Rational Design.- 5 Molecular structures, relative stability, and proton affinities of nucleotides: Broad view and novel findings.- 6 Quantum Chemical Approaches in Modeling the Structure of Quadruplex DNA and Its Interaction with Metal Ions and Small Molecules.- 7 Density Functional Theory Calculations of Enzyme-Inhibitor Interactions in Medicinal Chemistry and Drug Design.- 8 Molecular Dynamics Simulations of Lipid Bilayers with Incorporated Peptides.- 9 Polyphenol Glycosides as Potential Remedies in Kidney Stones Therapy. Experimental Research Supported by Computational Studies.- 10 Quantum-Chemical Investigation of Epoxidic Compounds Transformation. Application for In Vitro and In Vivo Processes Modeling.- 11 Computational Toxicology in Drug Discovery: opportunities and limitations.- 12 Consensus Drug Design Using it Microcosm.- 13 Continuous Molecular Fields Approach Applied to Structure-Activity Modeling.- 14 Quantitative Structure-Pharmacokinetic Relationships of Drugs within the Framework of Biopharmaceutics Classification System by Using Simplex Representation of Molecular Structure.- 15 (How to) Profit from Molecular Dynamics-based Ensemble Docking.- 16 Cheminformatics on Crossroad of Eras.
  • (source: Nielsen Book Data)
The proposed volume provides both fundamental and detailed information about the computational and computational-experimental studies which improve our knowledge of how leaving matter functions, the different properties of drugs (including the calculation and the design of new ones), and the creation of completely new ways of treating numerical diseases. Whenever it is possible, the interplay between theory and experiment is provided. The book features computational techniques such as quantum-chemical and molecular dynamic approaches and quantitative structure-activity relationships. The initial chapters describe the state-of-the art research on the computational investigations in molecular biology, molecular pharmacy, and molecular medicine performed with the use of pure quantum-chemical techniques. The central part of the book illustrates the status of computational techniques that utilize hybrid, so called QM/MM approximations as well as the results of the QSAR studies which now are the most popular in predicting drugs' efficiency. The last chapters describe combined computational and experimental investigations.
(source: Nielsen Book Data)
  • 1 Hybrid QM/MM Methods: Treating Electronic Phenomena in Very Large Molecular Systems.- 2 Structure, Thermodynamics and Energetics of Drug-DNA Interactions: Computer Modeling and Experiment.- 3 Formation of DNA Lesions, Its Prevention and Repair.- 4 DNA dependent DNA Polymerases as Targets for Low-Weight Molecular Inhibitors: State of Art and Prospects of Rational Design.- 5 Molecular structures, relative stability, and proton affinities of nucleotides: Broad view and novel findings.- 6 Quantum Chemical Approaches in Modeling the Structure of Quadruplex DNA and Its Interaction with Metal Ions and Small Molecules.- 7 Density Functional Theory Calculations of Enzyme-Inhibitor Interactions in Medicinal Chemistry and Drug Design.- 8 Molecular Dynamics Simulations of Lipid Bilayers with Incorporated Peptides.- 9 Polyphenol Glycosides as Potential Remedies in Kidney Stones Therapy. Experimental Research Supported by Computational Studies.- 10 Quantum-Chemical Investigation of Epoxidic Compounds Transformation. Application for In Vitro and In Vivo Processes Modeling.- 11 Computational Toxicology in Drug Discovery: opportunities and limitations.- 12 Consensus Drug Design Using it Microcosm.- 13 Continuous Molecular Fields Approach Applied to Structure-Activity Modeling.- 14 Quantitative Structure-Pharmacokinetic Relationships of Drugs within the Framework of Biopharmaceutics Classification System by Using Simplex Representation of Molecular Structure.- 15 (How to) Profit from Molecular Dynamics-based Ensemble Docking.- 16 Cheminformatics on Crossroad of Eras.
  • (source: Nielsen Book Data)
The proposed volume provides both fundamental and detailed information about the computational and computational-experimental studies which improve our knowledge of how leaving matter functions, the different properties of drugs (including the calculation and the design of new ones), and the creation of completely new ways of treating numerical diseases. Whenever it is possible, the interplay between theory and experiment is provided. The book features computational techniques such as quantum-chemical and molecular dynamic approaches and quantitative structure-activity relationships. The initial chapters describe the state-of-the art research on the computational investigations in molecular biology, molecular pharmacy, and molecular medicine performed with the use of pure quantum-chemical techniques. The central part of the book illustrates the status of computational techniques that utilize hybrid, so called QM/MM approximations as well as the results of the QSAR studies which now are the most popular in predicting drugs' efficiency. The last chapters describe combined computational and experimental investigations.
(source: Nielsen Book Data)
Book
xii, 270 pages : illustrations (some color) ; 25 cm
  • States of matter related to pharmacuetical formulations / Beverly J. Sandmann, Ann Newman, and Gregory T. Knipp
  • Physical properties of solutions / Beverly Sandmann, Antoine Al-Achi, Robert Greenwood
  • Ionic equilibrium and buffers / Beverly Sandmann, Alekha K. Dash, Antoine Al-Achi, Robert Greenwood
  • Solubility, dissolution, and partitioning/ Beverly J. Sandmann and Mansoor M. Amiji
  • Mass transport / Mansoor M. Amiji
  • Complexation and protein binding / Mansoor M. Amiji
  • Dispersed systems / W. Cary Mobley
  • Interfacial phenomena / Maria Polikandritou Lambros and SHihong Li Nocolaou
  • Rheology / Maria Polikandritou Lambros
  • Chemical kinetics of pharmaceuticals / Thomas J. Cook.
This is a unique practice-oriented introduction to physical pharmacy. Applied Physical Pharmacy explores the fundamental physicochemical properties and processes important for understanding how drugs are transformed into usable and stable drug products that release their drug upon administration, and for understanding the different processes that the released drug may encounter on its way to its pharmacological target prior to being eliminated by the body. Applied Physical Pharmacy begins with a review of key biopharmaceutics concepts of drug liberation, absorption, distribution, metabolism, and excretion. These concepts, which describe the fate of the drug in the body, set the framework for subsequent chapters that describe physicochemical properties and processes such as states of matter, solutions, ionization, dissolution and partitioning, mass transport, complexation, and protein binding. Concepts in these chapters are important for not only understanding a drug's fate in the body, but also for providing a scientific basis for rational drug formulation and usage. Other physical pharmacy topics important to drug formulation are discussed in the chapters that follow, which describe dispersed systems, rheology, and interfacial phenomena. The book concludes with an overview of the principles of kinetics that are essential to understanding the rates at which many of the processes discussed in previous chapters occur. To facilitate learning, chapters are enhanced by Learning Objectives, Key Points, Problems, and Clinical Questions. To make the book as relevant to real-world practice as possible, this edition includes an increased number of clinical examples and applications.
(source: Nielsen Book Data)
  • States of matter related to pharmacuetical formulations / Beverly J. Sandmann, Ann Newman, and Gregory T. Knipp
  • Physical properties of solutions / Beverly Sandmann, Antoine Al-Achi, Robert Greenwood
  • Ionic equilibrium and buffers / Beverly Sandmann, Alekha K. Dash, Antoine Al-Achi, Robert Greenwood
  • Solubility, dissolution, and partitioning/ Beverly J. Sandmann and Mansoor M. Amiji
  • Mass transport / Mansoor M. Amiji
  • Complexation and protein binding / Mansoor M. Amiji
  • Dispersed systems / W. Cary Mobley
  • Interfacial phenomena / Maria Polikandritou Lambros and SHihong Li Nocolaou
  • Rheology / Maria Polikandritou Lambros
  • Chemical kinetics of pharmaceuticals / Thomas J. Cook.
This is a unique practice-oriented introduction to physical pharmacy. Applied Physical Pharmacy explores the fundamental physicochemical properties and processes important for understanding how drugs are transformed into usable and stable drug products that release their drug upon administration, and for understanding the different processes that the released drug may encounter on its way to its pharmacological target prior to being eliminated by the body. Applied Physical Pharmacy begins with a review of key biopharmaceutics concepts of drug liberation, absorption, distribution, metabolism, and excretion. These concepts, which describe the fate of the drug in the body, set the framework for subsequent chapters that describe physicochemical properties and processes such as states of matter, solutions, ionization, dissolution and partitioning, mass transport, complexation, and protein binding. Concepts in these chapters are important for not only understanding a drug's fate in the body, but also for providing a scientific basis for rational drug formulation and usage. Other physical pharmacy topics important to drug formulation are discussed in the chapters that follow, which describe dispersed systems, rheology, and interfacial phenomena. The book concludes with an overview of the principles of kinetics that are essential to understanding the rates at which many of the processes discussed in previous chapters occur. To facilitate learning, chapters are enhanced by Learning Objectives, Key Points, Problems, and Clinical Questions. To make the book as relevant to real-world practice as possible, this edition includes an increased number of clinical examples and applications.
(source: Nielsen Book Data)
Chemistry & ChemEng Library (Swain)
Status of items at Chemistry & ChemEng Library (Swain)
Chemistry & ChemEng Library (Swain) Status
Stacks
RS403 .A676 2014 Unknown
Book
1 online resource (vii, 237 pages) : illustrations (some color). Digital: text file; PDF.
  • Carbohydrate-Based Synthetic Chemistry in the Context of Drug Design.- Iminosugars: Therapeutic Applications and Synthetic Considerations.- Computational Docking as a Tool for the Rational Design of Carbohydrate-Based Drugs.- Discovery and Development of Selective Renal Sodium-Dependent Glucose Cotransporter 2 (SGLT2) Dapagliflozin for the Treatment of Type 2 Diabetes.- Design, Synthesis, and Applications of Galectin Modulators in Human Health.- Discovery and Application of FimH Antagonists.- Carbohydrate-Based Anti-Virulence Compounds Against Chronic Pseudomonas aeruginosa Infections with a Focus on Small Molecules.- The Evolution of a Glycoconjugate Vaccine for Candida albicans.
  • (source: Nielsen Book Data)
Medicinal chemistry is both science and art. The science of medicinal chemistry offers mankind one of its best hopes for improving the quality of life. The art of medicinal chemistry continues to challenge its practitioners with the need for both intuition and experience to discover new drugs. Hence sharing the experience of drug research is uniquely beneficial to the field of medicinal chemistry. Drug research requires interdisciplinary team-work at the interface between chemistry, biology and medicine. Therefore, the topic-related series Topics in Medicinal Chemistry covers all relevant aspects of drug research, e.g. pathobiochemistry of diseases, identification and validation of (emerging) drug targets, structural biology, drugability of targets, drug design approaches, chemogenomics, synthetic chemistry including combinatorial methods, bioorganic chemistry, natural compounds, high-throughput screening, pharmacological in vitro and in vivo investigations, drug-receptor interactions on the molecular level, structure-activity relationships, drug absorption, distribution, metabolism, elimination, toxicology and pharmacogenomics. In general, special volumes are edited by well known guest editors.
(source: Nielsen Book Data)
  • Carbohydrate-Based Synthetic Chemistry in the Context of Drug Design.- Iminosugars: Therapeutic Applications and Synthetic Considerations.- Computational Docking as a Tool for the Rational Design of Carbohydrate-Based Drugs.- Discovery and Development of Selective Renal Sodium-Dependent Glucose Cotransporter 2 (SGLT2) Dapagliflozin for the Treatment of Type 2 Diabetes.- Design, Synthesis, and Applications of Galectin Modulators in Human Health.- Discovery and Application of FimH Antagonists.- Carbohydrate-Based Anti-Virulence Compounds Against Chronic Pseudomonas aeruginosa Infections with a Focus on Small Molecules.- The Evolution of a Glycoconjugate Vaccine for Candida albicans.
  • (source: Nielsen Book Data)
Medicinal chemistry is both science and art. The science of medicinal chemistry offers mankind one of its best hopes for improving the quality of life. The art of medicinal chemistry continues to challenge its practitioners with the need for both intuition and experience to discover new drugs. Hence sharing the experience of drug research is uniquely beneficial to the field of medicinal chemistry. Drug research requires interdisciplinary team-work at the interface between chemistry, biology and medicine. Therefore, the topic-related series Topics in Medicinal Chemistry covers all relevant aspects of drug research, e.g. pathobiochemistry of diseases, identification and validation of (emerging) drug targets, structural biology, drugability of targets, drug design approaches, chemogenomics, synthetic chemistry including combinatorial methods, bioorganic chemistry, natural compounds, high-throughput screening, pharmacological in vitro and in vivo investigations, drug-receptor interactions on the molecular level, structure-activity relationships, drug absorption, distribution, metabolism, elimination, toxicology and pharmacogenomics. In general, special volumes are edited by well known guest editors.
(source: Nielsen Book Data)

7. Chemistry of drugs [2014]

Book
x, 260 p. : ill. ; 24 cm.
Chemistry & ChemEng Library (Swain)
Status of items at Chemistry & ChemEng Library (Swain)
Chemistry & ChemEng Library (Swain) Status
Stacks
RS403 .B27 2014 Unknown
Book
1 online resource (xv, 415 pages)
  • Preface vii Contributors xiii 1 What Are Our Models Really Telling Us? A Practical Tutorial onAvoiding Common Mistakes when Building Predictive Models 1 W. Patrick Walters 2 The Challenge of Creativity in Drug Design 33 Ajay N. Jain 3 A Rough Set Theory Approach to the Analysis of Gene ExpressionProfiles 51 Joachim Petit, Nathalie Meurice, Jose Luis Medina-Franco, and Gerald M. Maggiora 4 Bimodal Partial Least-Squares Approach and Its Application toChemogenomics Studies for Molecular Design 85 Kiyoshi Hasegawa and Kimito Funatsu 5 Stability in Molecular Fingerprint Comparison 97 Anthony Nicholls and Brian Kelley 6 C ritical Assessment of Virtual Screening for HitIdentification 113 Dagmar Stumpfe and Jurgen Bajorath 7 Chemometric Applications of Naive Bayesian Models in DrugDiscovery: Beyond Compound Ranking 131 Eugen Lounkine, Peter S. Kutchukian, and Meir Glick 8 Chemoinformatics in Lead Optimization 149 Darren V. S. Green and Matthew Segall 9 Using Chemoinformatics Tools to Analyze Chemical Arrays inLead Optimization 179 George Papadatos, Valerie J. Gillet, Christopher N. Luscombe, Iain M. McLay, Stephen D. Pickett, and Peter Willett 10 Exploration of Structure Activity Relationships (SAR s)and Transfer of Key Elements in Lead Optimization 205 Hans Matter, Stefan Gussregen, Friedemann Schmidt, GerhardHessler, Thorsten Naumann, and Karl-Heinz Baringhaus 11 Development and Applications of Global ADMET Models: InSilico Prediction of Human Microsomal Lability 245 Karl-Heinz Baringhaus, Gerhard Hessler, Hans Matter, andFriedemann Schmidt 12 Chemoinformatics and Beyond: Moving from Simple Models toComplex Relationships in Pharmaceutical Computational Toxicology267 Catrin Hasselgren, Daniel Muthas, Ernst Ahlberg, SamuelAndersson, Lars Carlsson, Tobias Noeske, Jonna Stalring, andScott Boyer 13 Applications of Cheminformatics in Pharmaceutical Research:Experiences at Boehringer Ingelheim in Germany 291 Bernd Beck, Michael Bieler, Peter Haebel, AndreasTeckentrup, Alexander Weber, and Nils Weskamp 14 Lessons Learned from 30 Years of Developing SuccessfulIntegrated Cheminformatic Systems 321 Michael S. Lajiness and Thomas R. Hagadone 15 Molecular Similarity Analysis 343 Jose L. Medina-Franco and Gerald M. Maggiora Index 401.
  • (source: Nielsen Book Data)
The first guide to address the strengths, weaknesses, case studies, and applications of cheminformatics approaches to drug discovery, Chemoinformatics addresses how these in silico techniques are applied in both academic and industrial research environments. Discussing approaches that have been successful as well as those that have not, the text outlines cheminformatics infrastructure tools and their implementation and describes the impact of different approaches on experimental or pharmaceutical research. A valuable resource for computational, medicinal/pharmaceutical scientists, chemical biologists, and computational biologists, the text includes case studies and applications by experimental and industrial researchers.
(source: Nielsen Book Data)
  • Preface vii Contributors xiii 1 What Are Our Models Really Telling Us? A Practical Tutorial onAvoiding Common Mistakes when Building Predictive Models 1 W. Patrick Walters 2 The Challenge of Creativity in Drug Design 33 Ajay N. Jain 3 A Rough Set Theory Approach to the Analysis of Gene ExpressionProfiles 51 Joachim Petit, Nathalie Meurice, Jose Luis Medina-Franco, and Gerald M. Maggiora 4 Bimodal Partial Least-Squares Approach and Its Application toChemogenomics Studies for Molecular Design 85 Kiyoshi Hasegawa and Kimito Funatsu 5 Stability in Molecular Fingerprint Comparison 97 Anthony Nicholls and Brian Kelley 6 C ritical Assessment of Virtual Screening for HitIdentification 113 Dagmar Stumpfe and Jurgen Bajorath 7 Chemometric Applications of Naive Bayesian Models in DrugDiscovery: Beyond Compound Ranking 131 Eugen Lounkine, Peter S. Kutchukian, and Meir Glick 8 Chemoinformatics in Lead Optimization 149 Darren V. S. Green and Matthew Segall 9 Using Chemoinformatics Tools to Analyze Chemical Arrays inLead Optimization 179 George Papadatos, Valerie J. Gillet, Christopher N. Luscombe, Iain M. McLay, Stephen D. Pickett, and Peter Willett 10 Exploration of Structure Activity Relationships (SAR s)and Transfer of Key Elements in Lead Optimization 205 Hans Matter, Stefan Gussregen, Friedemann Schmidt, GerhardHessler, Thorsten Naumann, and Karl-Heinz Baringhaus 11 Development and Applications of Global ADMET Models: InSilico Prediction of Human Microsomal Lability 245 Karl-Heinz Baringhaus, Gerhard Hessler, Hans Matter, andFriedemann Schmidt 12 Chemoinformatics and Beyond: Moving from Simple Models toComplex Relationships in Pharmaceutical Computational Toxicology267 Catrin Hasselgren, Daniel Muthas, Ernst Ahlberg, SamuelAndersson, Lars Carlsson, Tobias Noeske, Jonna Stalring, andScott Boyer 13 Applications of Cheminformatics in Pharmaceutical Research:Experiences at Boehringer Ingelheim in Germany 291 Bernd Beck, Michael Bieler, Peter Haebel, AndreasTeckentrup, Alexander Weber, and Nils Weskamp 14 Lessons Learned from 30 Years of Developing SuccessfulIntegrated Cheminformatic Systems 321 Michael S. Lajiness and Thomas R. Hagadone 15 Molecular Similarity Analysis 343 Jose L. Medina-Franco and Gerald M. Maggiora Index 401.
  • (source: Nielsen Book Data)
The first guide to address the strengths, weaknesses, case studies, and applications of cheminformatics approaches to drug discovery, Chemoinformatics addresses how these in silico techniques are applied in both academic and industrial research environments. Discussing approaches that have been successful as well as those that have not, the text outlines cheminformatics infrastructure tools and their implementation and describes the impact of different approaches on experimental or pharmaceutical research. A valuable resource for computational, medicinal/pharmaceutical scientists, chemical biologists, and computational biologists, the text includes case studies and applications by experimental and industrial researchers.
(source: Nielsen Book Data)
Book
1 online resource.
  • Overview on Parkinson disease. Rational for pharmacological intervention-- Dopaminergic pathway and L-Dopa treatments. Future challenges-- COMT Inhibitors: present problems and relevance of the new ones-- MAO inhibitors for PD (Safinamide)-- Dopamine agonist: present and future (Pardoprunox)-- Therapies for dopaminergic-induced dyskinesias in Parkinson disease. (Fipamizole)-- Beyond the dopamine receptor: regulation of protein phosphatases-- Molecular chaperones as rational drug targets for Parkinson's disease therapeutics-- Alpha-synuclein assembly as a therapeutic target of PD-- Alpha-synuclein (alpha-syn) phosphorylating polo-like kinase 2 (PLK2) as target for PD-- Hsp70 molecular chaperones and Parkinson's disease-- Glutamate receptors as therapeutic targets for Parkinson's disease-- Targeting adenosine A2A receptors in Parkinson's disease-- Leucine-rich repeat kinase-2 as target for Parkinson's disease-- Phosphodiesterase inhibitors for PD treatment-- P2X7 purinergic receptor: role in neurological disorders-- Therapeutic role of 5-HT1A receptors in the treatment of schizophrenia and Parkinson's disease-- D3 dopamine receptor agonists: neuroprotection in Parkinson's disease-- Antioxidants and PD-- Tryptophan metabolism in Parkinson's disease-- Grafted neural stem cell-derived dopaminergic neurons for PD Therapy-- Gene therapy for Parkinson's disease-- Carotid body autotransplantation in Parkinson disease--Neurotrophic factor therapy for Parkinson's disease.
  • (source: Nielsen Book Data)
Affecting over 1.5 million people across the world, Parkinson's disease is a progressive neurological condition characterized, in part, by the loss of dopaminergic neurons in the substantia nigra pars compacta. It affects 1.5% of the global population over 65 years of age. As life expectancy is increasing, over the next few years the number of patients with Parkinson's disease will grow exponentially. To date, there are no available treatments that are capable of curing Parkinson's disease, and the current goal of therapy, dopamine replacement strategies, is to reduce symptoms. After several years of disease progression, treatment is complicated by the onset of motor fluctuations and dyskinesias. This information reveals the great importance and social need of finding an effective therapeutic intervention for Parkinson's disease. This exemplary new book reviews some of the most outstanding examples of new drugs currently in pharmaceutical development or new targets currently undergoing the validation process to try to reach the Parkinson's drug market in the next few years as potential disease modifying drugs. Providing up to date and comprehensive coverage, this book is essential reading for researchers working in academia and industry in any aspect of medicinal chemistry or drug discovery.
(source: Nielsen Book Data)
  • Overview on Parkinson disease. Rational for pharmacological intervention-- Dopaminergic pathway and L-Dopa treatments. Future challenges-- COMT Inhibitors: present problems and relevance of the new ones-- MAO inhibitors for PD (Safinamide)-- Dopamine agonist: present and future (Pardoprunox)-- Therapies for dopaminergic-induced dyskinesias in Parkinson disease. (Fipamizole)-- Beyond the dopamine receptor: regulation of protein phosphatases-- Molecular chaperones as rational drug targets for Parkinson's disease therapeutics-- Alpha-synuclein assembly as a therapeutic target of PD-- Alpha-synuclein (alpha-syn) phosphorylating polo-like kinase 2 (PLK2) as target for PD-- Hsp70 molecular chaperones and Parkinson's disease-- Glutamate receptors as therapeutic targets for Parkinson's disease-- Targeting adenosine A2A receptors in Parkinson's disease-- Leucine-rich repeat kinase-2 as target for Parkinson's disease-- Phosphodiesterase inhibitors for PD treatment-- P2X7 purinergic receptor: role in neurological disorders-- Therapeutic role of 5-HT1A receptors in the treatment of schizophrenia and Parkinson's disease-- D3 dopamine receptor agonists: neuroprotection in Parkinson's disease-- Antioxidants and PD-- Tryptophan metabolism in Parkinson's disease-- Grafted neural stem cell-derived dopaminergic neurons for PD Therapy-- Gene therapy for Parkinson's disease-- Carotid body autotransplantation in Parkinson disease--Neurotrophic factor therapy for Parkinson's disease.
  • (source: Nielsen Book Data)
Affecting over 1.5 million people across the world, Parkinson's disease is a progressive neurological condition characterized, in part, by the loss of dopaminergic neurons in the substantia nigra pars compacta. It affects 1.5% of the global population over 65 years of age. As life expectancy is increasing, over the next few years the number of patients with Parkinson's disease will grow exponentially. To date, there are no available treatments that are capable of curing Parkinson's disease, and the current goal of therapy, dopamine replacement strategies, is to reduce symptoms. After several years of disease progression, treatment is complicated by the onset of motor fluctuations and dyskinesias. This information reveals the great importance and social need of finding an effective therapeutic intervention for Parkinson's disease. This exemplary new book reviews some of the most outstanding examples of new drugs currently in pharmaceutical development or new targets currently undergoing the validation process to try to reach the Parkinson's drug market in the next few years as potential disease modifying drugs. Providing up to date and comprehensive coverage, this book is essential reading for researchers working in academia and industry in any aspect of medicinal chemistry or drug discovery.
(source: Nielsen Book Data)
Book
xiii, 146 p. : ill. ; 24 cm
  • Carbohydrates Lipids Proteins Enzymes Inorganics Vitamins Steroids Plant Acids Flavonoids Alkaloids Tannins Resins Glycosides Gums Balsams Volatile Oils Analgesics Anesthetics Sulfa Drugs (Sulfonamides) Psychotropic Drugs Antibiotics Nucleic Acids General Bibliography.
  • (source: Nielsen Book Data)
Written by an author with more than 40 years of teaching experience in the field, Experiments in Pharmaceutical Chemistry, Second Edition responds to a critical classroom need for material on directed laboratory investigations in biological and pharmaceutical chemistry. This new edition supplies 75 experiments, expanding the range of topics to 22 major areas of pharmaceutical chemistry. These include biochemical groups, botanical classes important to pharmacy, and major drug classifications: Carbohydrates Lipids Proteins Enzymes Inorganics Vitamins Steroids Plant Acids Flavonoids Alkaloids Tannins Resins Glycosides Gums Balsams Volatile Oils Analgesics Anesthetics Sulfa Drugs (Sulfonamides) Psychotropic Drugs Antibiotics Nucleic Acids Sections contain introductions to basic concepts underlying the fields addressed and a specific bibliography relating to each field. Each experiment provides detailed instructions in a user-friendly format, and can be carried out, in most cases, without the need for expensive instrumentation. This comprehensive laboratory manual offers much-needed instructional material for teaching laboratory classes in pharmaceutical chemistry. The breadth of subject matter covered provides a variety of choices for structuring a laboratory course.
(source: Nielsen Book Data)
  • Carbohydrates Lipids Proteins Enzymes Inorganics Vitamins Steroids Plant Acids Flavonoids Alkaloids Tannins Resins Glycosides Gums Balsams Volatile Oils Analgesics Anesthetics Sulfa Drugs (Sulfonamides) Psychotropic Drugs Antibiotics Nucleic Acids General Bibliography.
  • (source: Nielsen Book Data)
Written by an author with more than 40 years of teaching experience in the field, Experiments in Pharmaceutical Chemistry, Second Edition responds to a critical classroom need for material on directed laboratory investigations in biological and pharmaceutical chemistry. This new edition supplies 75 experiments, expanding the range of topics to 22 major areas of pharmaceutical chemistry. These include biochemical groups, botanical classes important to pharmacy, and major drug classifications: Carbohydrates Lipids Proteins Enzymes Inorganics Vitamins Steroids Plant Acids Flavonoids Alkaloids Tannins Resins Glycosides Gums Balsams Volatile Oils Analgesics Anesthetics Sulfa Drugs (Sulfonamides) Psychotropic Drugs Antibiotics Nucleic Acids Sections contain introductions to basic concepts underlying the fields addressed and a specific bibliography relating to each field. Each experiment provides detailed instructions in a user-friendly format, and can be carried out, in most cases, without the need for expensive instrumentation. This comprehensive laboratory manual offers much-needed instructional material for teaching laboratory classes in pharmaceutical chemistry. The breadth of subject matter covered provides a variety of choices for structuring a laboratory course.
(source: Nielsen Book Data)
Chemistry & ChemEng Library (Swain)
Status of items at Chemistry & ChemEng Library (Swain)
Chemistry & ChemEng Library (Swain) Status
Stacks
RS407 .D53 2014 Unknown
Book
xii, 385 p. : ill.
  • Generic Drug Product Development and Therapeutic Equivalence-- Leon Shargel and Isadore Kanfer Active Pharmaceutical Ingredients-- Edward M. Cohen and Steven Sutherland Analytical Methods Development and Methods Validation for Oral Solid Dosage Forms-- Quanyin Gao and Dilip R. Sanvordeker Experimental Formulation Development-- Isadore Kanfer, Roderick B. Walker, Raimar Lobenberg, and Nadia Araci Bou-Chacra Scale-up, Technology Transfer, and Process Performance Qualification-- Salah U. Ahmed, Ashok Katdare, Venkatesh Naini, and Dilip Wadgaonkar Drug Stability-- Pranab K. Bhattacharyya Quality Control and Quality Assurance-- Loren Gelber Drug Product Performance: In Vitro-- Pradeep M. Sathe, John Duan, and Lawrence X. Yu ANDA Regulatory Approval Process-- Timothy W. Ames and Aaron Sigler Bioequivalence and Drug Product Assessment: In Vivo-- Barbara M. Davit and Dale P. Conner Statistical Considerations for Establishing Bioequivalence-- Charles Bon and Sanford Bolton Outsourcing Bioavailability and Bioequivalence Studies to Contract Research Organizations-- Patrick K. Noonan Postapproval Changes and Postmarketing Reporting of Adverse Drug Experiences-- Lorien Armour and Leon Shargel The United States Pharmacopeia/National Formulary: Its History, Organization, and Role in Harmonization-- William Brown and Margareth R. C. Marques Legal and Legislative Hurdles to Generic Drug Development, Approval, and Marketing-- Arthur T. Tsien Index.
  • (source: Nielsen Book Data)
In this era of increased pharmaceutical industry competition, success for generic drug companies is dependent on their ability to manufacture therapeutic-equivalent drug products in an economical and timely manner, while also being cognizant of patent infringement and other legal and regulatory concerns. Generic Drug Product Development: Solid Oral Dosage Forms, Second Edition presents in-depth discussions from more than 30 noted specialists describing the development of generic drug products-from the raw materials to the development of a therapeutic-equivalent drug product to regulatory approval. Major topics discussed include: * Active pharmaceutical ingredients * Experimental formulation development, including a new section on Quality by Design (QbD) * Scale-up * Commercial product formulation * Quality control and bioequivalence * Drug product performance * ANDA regulatory process * Post-approval changes * Post-marketing surveillance * Legislative and patent challenges This second edition also contains a new chapter on the relationship between the FDA and the United States Pharmacopeia and in Chapter 4, using specific examples, the application of Quality by Design (QbD) during formulation development is examined.The book is a thorough guide to the development of solid oral generic dosage formulations. This textbook is ideal for the pharmaceutical industry, graduate programs in pharmaceutical sciences, and health professionals working in the area of generic drug development.
(source: Nielsen Book Data)
  • Generic Drug Product Development and Therapeutic Equivalence-- Leon Shargel and Isadore Kanfer Active Pharmaceutical Ingredients-- Edward M. Cohen and Steven Sutherland Analytical Methods Development and Methods Validation for Oral Solid Dosage Forms-- Quanyin Gao and Dilip R. Sanvordeker Experimental Formulation Development-- Isadore Kanfer, Roderick B. Walker, Raimar Lobenberg, and Nadia Araci Bou-Chacra Scale-up, Technology Transfer, and Process Performance Qualification-- Salah U. Ahmed, Ashok Katdare, Venkatesh Naini, and Dilip Wadgaonkar Drug Stability-- Pranab K. Bhattacharyya Quality Control and Quality Assurance-- Loren Gelber Drug Product Performance: In Vitro-- Pradeep M. Sathe, John Duan, and Lawrence X. Yu ANDA Regulatory Approval Process-- Timothy W. Ames and Aaron Sigler Bioequivalence and Drug Product Assessment: In Vivo-- Barbara M. Davit and Dale P. Conner Statistical Considerations for Establishing Bioequivalence-- Charles Bon and Sanford Bolton Outsourcing Bioavailability and Bioequivalence Studies to Contract Research Organizations-- Patrick K. Noonan Postapproval Changes and Postmarketing Reporting of Adverse Drug Experiences-- Lorien Armour and Leon Shargel The United States Pharmacopeia/National Formulary: Its History, Organization, and Role in Harmonization-- William Brown and Margareth R. C. Marques Legal and Legislative Hurdles to Generic Drug Development, Approval, and Marketing-- Arthur T. Tsien Index.
  • (source: Nielsen Book Data)
In this era of increased pharmaceutical industry competition, success for generic drug companies is dependent on their ability to manufacture therapeutic-equivalent drug products in an economical and timely manner, while also being cognizant of patent infringement and other legal and regulatory concerns. Generic Drug Product Development: Solid Oral Dosage Forms, Second Edition presents in-depth discussions from more than 30 noted specialists describing the development of generic drug products-from the raw materials to the development of a therapeutic-equivalent drug product to regulatory approval. Major topics discussed include: * Active pharmaceutical ingredients * Experimental formulation development, including a new section on Quality by Design (QbD) * Scale-up * Commercial product formulation * Quality control and bioequivalence * Drug product performance * ANDA regulatory process * Post-approval changes * Post-marketing surveillance * Legislative and patent challenges This second edition also contains a new chapter on the relationship between the FDA and the United States Pharmacopeia and in Chapter 4, using specific examples, the application of Quality by Design (QbD) during formulation development is examined.The book is a thorough guide to the development of solid oral generic dosage formulations. This textbook is ideal for the pharmaceutical industry, graduate programs in pharmaceutical sciences, and health professionals working in the area of generic drug development.
(source: Nielsen Book Data)
Book
xiv, 243 pages : illustrations (some color) ; 25 cm
  • Table of Contents -- Chapter 1: Seduced by drug discovery -- Chapter 2: The small molecules of life -- Chapter 3: Proteins: molecular wonders in three dimensions -- Chapter 4. Proteins perform multiple functions: enzymes, receptors, ion channels -- Chapter 5: Drug discovery and development: the road from an idea to promoting -- human health -- Chapter 6: Finasteride: the Gary and Jerry show -- Chapter 7: Basic research, snake venoms, and ACE inhibitors: Ondetti, Cushman, and -- Patchett -- Chapter 8: Statins: protection against heart attacks and strokes -- Chapter 9: The perils of Primaxin -- Chapter 10: Avermectins: molecules of life battle parasites -- Chapter 11: Fludalanine: nice try but no hallelujah -- Chapter 12: Diabetes Breakthrough: Januvia and Janumet.
  • (source: Nielsen Book Data)
Pharmeceutical drug discovery has wide-reaching and obvious effects on the lives of people everywhere, and yet the general public knows very little about the way in which these important products are conceived. We rely on pharmaceuticals to keep us healthy in countless ways, with almost no understanding of the process behind the creation of the drugs we use. in Hallelujah Moments, Eugene Cordes reveals just how some of the most important and influential drugs are made. He shares his firsthand knowledge of the drug-discovery world, having spent a long and distinguished career on both the academic and industrial side of pharmaceutical research. These tales are "adventure stories, " and they follow important drugs like Proscar, Capoten, and Mevacor from the idea stage all the way to the point of being made publicly available. Cordes shows us the dynamic and critical thinking needed to create a useful drug, and the human stories of risk-taking, problem-solving, and, in many cases, failure. Written accessibly for a non-scientist audience, Hallelujah Moments brings the general public up to speed on the fascinating world of drug discovery like never before.
(source: Nielsen Book Data)
  • Table of Contents -- Chapter 1: Seduced by drug discovery -- Chapter 2: The small molecules of life -- Chapter 3: Proteins: molecular wonders in three dimensions -- Chapter 4. Proteins perform multiple functions: enzymes, receptors, ion channels -- Chapter 5: Drug discovery and development: the road from an idea to promoting -- human health -- Chapter 6: Finasteride: the Gary and Jerry show -- Chapter 7: Basic research, snake venoms, and ACE inhibitors: Ondetti, Cushman, and -- Patchett -- Chapter 8: Statins: protection against heart attacks and strokes -- Chapter 9: The perils of Primaxin -- Chapter 10: Avermectins: molecules of life battle parasites -- Chapter 11: Fludalanine: nice try but no hallelujah -- Chapter 12: Diabetes Breakthrough: Januvia and Janumet.
  • (source: Nielsen Book Data)
Pharmeceutical drug discovery has wide-reaching and obvious effects on the lives of people everywhere, and yet the general public knows very little about the way in which these important products are conceived. We rely on pharmaceuticals to keep us healthy in countless ways, with almost no understanding of the process behind the creation of the drugs we use. in Hallelujah Moments, Eugene Cordes reveals just how some of the most important and influential drugs are made. He shares his firsthand knowledge of the drug-discovery world, having spent a long and distinguished career on both the academic and industrial side of pharmaceutical research. These tales are "adventure stories, " and they follow important drugs like Proscar, Capoten, and Mevacor from the idea stage all the way to the point of being made publicly available. Cordes shows us the dynamic and critical thinking needed to create a useful drug, and the human stories of risk-taking, problem-solving, and, in many cases, failure. Written accessibly for a non-scientist audience, Hallelujah Moments brings the general public up to speed on the fascinating world of drug discovery like never before.
(source: Nielsen Book Data)
SAL1&2 (on-campus shelving)
Status of items at SAL1&2 (on-campus shelving)
SAL1&2 (on-campus shelving) Status
Stacks Request
RM301.25 .C67 2014 Unknown
Book
online resource (ix, 326 pages) : illustrations (some color).
  • 1 Hydrophilic Matrix Dosage Forms: Definitions, General Attributes and the Evolution of Clinical Utilization
  • 2 Design and Evaluation of Hydroxypropyl Methylcellulose Matrix Tablets for Oral Controlled Release: a Historical Perspective
  • 3 An Industrial Perspective on Hydrophilic Matrix Tablets based on Hyproxypropyl Methylcellulose (Hypromellose)
  • 4 Natural Polysaccharides in Hydrophilic Matrices
  • 5 Applications of Polyethylene Oxide (POLYOX) in Hydrophilic Matrices
  • 6 A Formulation Development Perspective on Critical Interactions Affecting the Performance of Hydrophilic Matrix Tablets
  • 7 In vitro Physical and Imaging Techniques to Evaluate Drug Release Mechanisms from Hydrophilic Matrix Tablets
  • 8 Physiologically-Based Pharmacokinetic Modelling in the Development and Evaluation of Hydrophilic Matrix Tablets
  • 9 Approaches to Rapid In Vivo Optimization of Hydrophilic Matrix Tablets
  • 10 Extrusion: an Enabling Technology for Controlled Release Hydrophilic Matrix Systems
  • 11 Microenvironmental pH Control and Mixed Polymer Approaches to Optimize Drug Delivery with Hydrophilic Matrix Tablets
  • 12 Evolving Biopharmaceutics Perspectives for Hydrophilic Matrix Tablets: Dosage Form-Food Interactions and Dosage Form Gastrointestinal Tract Interactions.
This detailed volume addresses key issues and subtle nuances involved in developing hydrophilic matrix tablets as an approach to oral controlled release. It brings together information from more than five decades of research and development on hydrophilic matrix tablets and provides perspective on contemporary issues. Twelve comprehensive chapters explore a variety of topics including polymers (hypromellose, natural polysaccharides and polyethylene oxide) and their utilization in hydrophilic matrices, critical interactions impacting tablet performance, in vitro physical and imaging techniques, and microenvironmental pH control and mixed polymer approaches, among others. In one collective volume, Hydrophilic Matrix Tablets for Oral Controlled Release provides a single source of current knowledge, including sections of previously unpublished data. It is an important resource for industrial and academic scientists investigating and developing these oral controlled release formulations.
  • 1 Hydrophilic Matrix Dosage Forms: Definitions, General Attributes and the Evolution of Clinical Utilization
  • 2 Design and Evaluation of Hydroxypropyl Methylcellulose Matrix Tablets for Oral Controlled Release: a Historical Perspective
  • 3 An Industrial Perspective on Hydrophilic Matrix Tablets based on Hyproxypropyl Methylcellulose (Hypromellose)
  • 4 Natural Polysaccharides in Hydrophilic Matrices
  • 5 Applications of Polyethylene Oxide (POLYOX) in Hydrophilic Matrices
  • 6 A Formulation Development Perspective on Critical Interactions Affecting the Performance of Hydrophilic Matrix Tablets
  • 7 In vitro Physical and Imaging Techniques to Evaluate Drug Release Mechanisms from Hydrophilic Matrix Tablets
  • 8 Physiologically-Based Pharmacokinetic Modelling in the Development and Evaluation of Hydrophilic Matrix Tablets
  • 9 Approaches to Rapid In Vivo Optimization of Hydrophilic Matrix Tablets
  • 10 Extrusion: an Enabling Technology for Controlled Release Hydrophilic Matrix Systems
  • 11 Microenvironmental pH Control and Mixed Polymer Approaches to Optimize Drug Delivery with Hydrophilic Matrix Tablets
  • 12 Evolving Biopharmaceutics Perspectives for Hydrophilic Matrix Tablets: Dosage Form-Food Interactions and Dosage Form Gastrointestinal Tract Interactions.
This detailed volume addresses key issues and subtle nuances involved in developing hydrophilic matrix tablets as an approach to oral controlled release. It brings together information from more than five decades of research and development on hydrophilic matrix tablets and provides perspective on contemporary issues. Twelve comprehensive chapters explore a variety of topics including polymers (hypromellose, natural polysaccharides and polyethylene oxide) and their utilization in hydrophilic matrices, critical interactions impacting tablet performance, in vitro physical and imaging techniques, and microenvironmental pH control and mixed polymer approaches, among others. In one collective volume, Hydrophilic Matrix Tablets for Oral Controlled Release provides a single source of current knowledge, including sections of previously unpublished data. It is an important resource for industrial and academic scientists investigating and developing these oral controlled release formulations.
Medical Library (Lane)
Status of items at Medical Library (Lane)
Medical Library (Lane) Status
Check Medical Library (Lane) catalog for status
SPRINGER Unknown
Book
1 online resource (ix, 326 pages) : illustrations (some color).
  • 1 Hydrophilic Matrix Dosage Forms: Definitions, General Attributes and the Evolution of Clinical Utilization
  • 2 Design and Evaluation of Hydroxypropyl Methylcellulose Matrix Tablets for Oral Controlled Release: a Historical Perspective
  • 3 An Industrial Perspective on Hydrophilic Matrix Tablets based on Hyproxypropyl Methylcellulose (Hypromellose)
  • 4 Natural Polysaccharides in Hydrophilic Matrices
  • 5 Applications of Polyethylene Oxide (POLYOX) in Hydrophilic Matrices
  • 6 A Formulation Development Perspective on Critical Interactions Affecting the Performance of Hydrophilic Matrix Tablets
  • 7 In vitro Physical and Imaging Techniques to Evaluate Drug Release Mechanisms from Hydrophilic Matrix Tablets
  • 8 Physiologically-Based Pharmacokinetic Modelling in the Development and Evaluation of Hydrophilic Matrix Tablets
  • 9 Approaches to Rapid In Vivo Optimization of Hydrophilic Matrix Tablets
  • 10 Extrusion: an Enabling Technology for Controlled Release Hydrophilic Matrix Systems
  • 11 Microenvironmental pH Control and Mixed Polymer Approaches to Optimize Drug Delivery with Hydrophilic Matrix Tablets
  • 12 Evolving Biopharmaceutics Perspectives for Hydrophilic Matrix Tablets: Dosage Form-Food Interactions and Dosage Form Gastrointestinal Tract Interactions.
This detailed volume addresses key issues and subtle nuances involved in developing hydrophilic matrix tablets as an approach to oral controlled release. It brings together information from more than five decades of research and development on hydrophilic matrix tablets and provides perspective on contemporary issues. Twelve comprehensive chapters explore a variety of topics including polymers (hypromellose, natural polysaccharides and polyethylene oxide) and their utilization in hydrophilic matrices, critical interactions impacting tablet performance, in vitro physical and imaging techniques, and microenvironmental pH control and mixed polymer approaches, among others. In one collective volume, Hydrophilic Matrix Tablets for Oral Controlled Release provides a single source of current knowledge, including sections of previously unpublished data. It is an important resource for industrial and academic scientists investigating and developing these oral controlled release formulations.
  • 1 Hydrophilic Matrix Dosage Forms: Definitions, General Attributes and the Evolution of Clinical Utilization
  • 2 Design and Evaluation of Hydroxypropyl Methylcellulose Matrix Tablets for Oral Controlled Release: a Historical Perspective
  • 3 An Industrial Perspective on Hydrophilic Matrix Tablets based on Hyproxypropyl Methylcellulose (Hypromellose)
  • 4 Natural Polysaccharides in Hydrophilic Matrices
  • 5 Applications of Polyethylene Oxide (POLYOX) in Hydrophilic Matrices
  • 6 A Formulation Development Perspective on Critical Interactions Affecting the Performance of Hydrophilic Matrix Tablets
  • 7 In vitro Physical and Imaging Techniques to Evaluate Drug Release Mechanisms from Hydrophilic Matrix Tablets
  • 8 Physiologically-Based Pharmacokinetic Modelling in the Development and Evaluation of Hydrophilic Matrix Tablets
  • 9 Approaches to Rapid In Vivo Optimization of Hydrophilic Matrix Tablets
  • 10 Extrusion: an Enabling Technology for Controlled Release Hydrophilic Matrix Systems
  • 11 Microenvironmental pH Control and Mixed Polymer Approaches to Optimize Drug Delivery with Hydrophilic Matrix Tablets
  • 12 Evolving Biopharmaceutics Perspectives for Hydrophilic Matrix Tablets: Dosage Form-Food Interactions and Dosage Form Gastrointestinal Tract Interactions.
This detailed volume addresses key issues and subtle nuances involved in developing hydrophilic matrix tablets as an approach to oral controlled release. It brings together information from more than five decades of research and development on hydrophilic matrix tablets and provides perspective on contemporary issues. Twelve comprehensive chapters explore a variety of topics including polymers (hypromellose, natural polysaccharides and polyethylene oxide) and their utilization in hydrophilic matrices, critical interactions impacting tablet performance, in vitro physical and imaging techniques, and microenvironmental pH control and mixed polymer approaches, among others. In one collective volume, Hydrophilic Matrix Tablets for Oral Controlled Release provides a single source of current knowledge, including sections of previously unpublished data. It is an important resource for industrial and academic scientists investigating and developing these oral controlled release formulations.
Book
1 online resource.
Increasing the potency of therapeutic compounds, while limiting side-effects, is a common goal in medicinal chemistry. Ligands that effectively bind metal ions and also include specific features to enhance targeting, reporting, and overall efficacy are driving innovation in areas of disease diagnosis and therapy. Ligand Design in Medicinal Inorganic Chemistry presents the state-of-the-art in ligand design for medicinal inorganic chemistry applications. Each individual chapter describes and explores the application of compounds that either target a disease site, or are activated by a disease-specific biological process. Ligand design is discussed in the following areas: * Platinum, Ruthenium, and Gold-containing anticancer agents * Emissive metal-based optical probes * Metal-based antimalarial agents * Metal overload disorders * Modulation of metal-protein interactions in neurodegenerative diseases * Photoactivatable metal complexes and their use in biology and medicine * Radiodiagnostic agents and Magnetic Resonance Imaging (MRI) agents * Carbohydrate-containing ligands and Schiff-base ligands in Medicinal Inorganic Chemistry * Metalloprotein inhibitors Ligand Design in Medicinal Inorganic Chemistry provides graduate students, industrial chemists and academic researchers with a launching pad for new research in medicinal chemistry.
(source: Nielsen Book Data)
Increasing the potency of therapeutic compounds, while limiting side-effects, is a common goal in medicinal chemistry. Ligands that effectively bind metal ions and also include specific features to enhance targeting, reporting, and overall efficacy are driving innovation in areas of disease diagnosis and therapy. Ligand Design in Medicinal Inorganic Chemistry presents the state-of-the-art in ligand design for medicinal inorganic chemistry applications. Each individual chapter describes and explores the application of compounds that either target a disease site, or are activated by a disease-specific biological process. Ligand design is discussed in the following areas: * Platinum, Ruthenium, and Gold-containing anticancer agents * Emissive metal-based optical probes * Metal-based antimalarial agents * Metal overload disorders * Modulation of metal-protein interactions in neurodegenerative diseases * Photoactivatable metal complexes and their use in biology and medicine * Radiodiagnostic agents and Magnetic Resonance Imaging (MRI) agents * Carbohydrate-containing ligands and Schiff-base ligands in Medicinal Inorganic Chemistry * Metalloprotein inhibitors Ligand Design in Medicinal Inorganic Chemistry provides graduate students, industrial chemists and academic researchers with a launching pad for new research in medicinal chemistry.
(source: Nielsen Book Data)
Book
xiii, 418 p. : ill. ; 26 cm.
  • 1 A Brief History of Drug Discovery 2 The Modern Drug Process 3 A Trip through the Body 4 Enzymes as Drug Targets 5 Receptors as Drug Targets 6 Oligonucleotides as Drug Targets 7 Pharmacokinetics 8 Metaboism 9 Molecular Structure and Diversity 10 Lead Discovery 11 Lead Optimization- Traditional Methods 12 Lead Optimization- Hansch Analysis 13 Aspects in Pharmaceutical Synthesis.
  • (source: Nielsen Book Data)
Emphasizing applications of chemistry while reinforcing theory - especially in the areas of organic and physical chemistry - this new text prepares readers for career success in the pharmaceutical, medical, and biotech industries. Medicinal Chemistry: The Modern Drug Discovery Process delivers a comprehensive introduction to medicinal chemistry at an appropriate level of detail for a diverse range of readers. By highlighting the concepts and skills related to drug discovery, Stevens deepens readers' understanding of the knowledge and techniques necessary for their careers.
(source: Nielsen Book Data)
  • 1 A Brief History of Drug Discovery 2 The Modern Drug Process 3 A Trip through the Body 4 Enzymes as Drug Targets 5 Receptors as Drug Targets 6 Oligonucleotides as Drug Targets 7 Pharmacokinetics 8 Metaboism 9 Molecular Structure and Diversity 10 Lead Discovery 11 Lead Optimization- Traditional Methods 12 Lead Optimization- Hansch Analysis 13 Aspects in Pharmaceutical Synthesis.
  • (source: Nielsen Book Data)
Emphasizing applications of chemistry while reinforcing theory - especially in the areas of organic and physical chemistry - this new text prepares readers for career success in the pharmaceutical, medical, and biotech industries. Medicinal Chemistry: The Modern Drug Discovery Process delivers a comprehensive introduction to medicinal chemistry at an appropriate level of detail for a diverse range of readers. By highlighting the concepts and skills related to drug discovery, Stevens deepens readers' understanding of the knowledge and techniques necessary for their careers.
(source: Nielsen Book Data)
Chemistry & ChemEng Library (Swain)
Status of items at Chemistry & ChemEng Library (Swain)
Chemistry & ChemEng Library (Swain) Status
Stacks
RS403 .S745 2014 Unknown
Book
1 online resource.
The inspiration provided by biologically active natural products to conceive of hybrids, congeners, analogs and unnatural variants is discussed by experts in the field in 15 highly informative chapters. Using well-documented case studies from drug development projects over the past decade, this handbook and ready reference demonstrates the current importance and future potential of natural products as drug precursors, highlighting the lessons learned and pointing to future directions in the field. The examples are carefully chosen so as to represent a wide range of chemical structures as well as therapeutic indications and include such "classical" cases as taxol and the vinca alkaloids as well the latest developments in protease inhibitors, antimicrobials, antifungals, antisense nucleosides, and epothilones.
(source: Nielsen Book Data)
The inspiration provided by biologically active natural products to conceive of hybrids, congeners, analogs and unnatural variants is discussed by experts in the field in 15 highly informative chapters. Using well-documented case studies from drug development projects over the past decade, this handbook and ready reference demonstrates the current importance and future potential of natural products as drug precursors, highlighting the lessons learned and pointing to future directions in the field. The examples are carefully chosen so as to represent a wide range of chemical structures as well as therapeutic indications and include such "classical" cases as taxol and the vinca alkaloids as well the latest developments in protease inhibitors, antimicrobials, antifungals, antisense nucleosides, and epothilones.
(source: Nielsen Book Data)
Book
online resource (xvii, 597 pages) : illustrations ; 26 cm
  • Small molecule formulation screening strategies in drug discovery / Gary W. Caldwell ... [et al.]
  • Assessment of drug plasma protein binding in drug discovery / Dennis Kalamaridis and Nayan Patel
  • Drug partition in red blood cells / Dennis Kalamaridis and Karen DiLoreto
  • Permeability assessment using 5-day cultured caco-2 cell monolayers / Gary W. Caldwell ... [et al.]
  • In situ single pass perfused rat intestinal model / Maria Markowska and L. Mark Kao
  • Metabolic stability assessed by liver microsomes and hepatocytes / Kevin J. Coe and Tatiana Koudriakova
  • Metabolic assessment in alamethicin-activated liver microsomes : co-activating CYPs and UGTs / Gary W. Caldwell and Zhengyin Yan
  • Phenotyping UDP-glucuronosyltransferases (UGTs) involved in human drug metabolism : an update / Michael H. Court
  • In vitro CYP/FMO reaction phenotyping / Carlo Sensenhauser
  • Human pregnane X receptor (hPXR) activation assay in stable cell lines / Judy L. Raucy
  • Characterization of constitutive androstane receptor (CAR) activation / Caitlin Lynch, Haishan Li, and Hongbing Wang
  • DNA binding (gel retardation assay) analysis for Identification of aryl hydrocarbon (Ah) receptor agonists and antagonists / Anatoly A. Soshilov and Michael S. Denison
  • Cell-based assays for identification of aryl hydrocarbon receptor (AhR) activators / Guochun He ... [et al.]
  • In vitro CYP induction using human hepatocytes / Monica Singer, Carlo Sensenhauser, and Shannon Dallas
  • Assessment of CYP3A4 time-dependent inhibition in plated and suspended human hepatocytes / J. George Zhang and David M. Stresser
  • Evaluation of time-dependent CYP3A4 inhibition using human hepatocytes / Yuan Chen and Adrian J. Fretland
  • Rapidly distinguishing reversible and time-dependent CYP450 inhibition using human liver microsomes, co-incubation, and continuous fluorometric Kinetic analyses / Gary W. Caldwell and Zhengyin Yan
  • Identification of time-dependent CYP inhibitors using human liver microsomes (HLM) / Kevin J. Coe, Judith Skaptason, and Tatiana Koudriakova
  • CYP time-dependent inhibition (TDI) using an IC50 shift assay with stable isotopic labeled substrate Probes to facilitate liquid chromatography/mass spectrometry analyses / Gary W. Caldwell and Zhengyin Yan
  • Screening for p-glycoprotein (Pgp) substrates and inhibitors / Qing Wang and Tina M. Sauerwald
  • In vitro characterization of intestinal transporter, breast cancer resistance protein (BCRP) / Chris Bode and Li-Bin Li
  • In vitro characterization of intestinal and hepatic transporters : MRP2 / Ravindra Varma Alluri ... [et al.]
  • In vitro characterization of hepatic transporters OATP1B1 and OATP1B3 / Blair Miezeiewski and Allison McLaughlin
  • In vitro characterization of renal transporters OAT1, OAT3, and OCT2 / Ying Wang and Nicole Behler
  • General guidelines for setting up an in vitro LC/MS/MS assay / John A. Masucci and Gary W. Caldwell
  • Metabolite identification in drug discovery / Wing W. Lam ... [et al.]
  • Drug, lipid, and acylcarnitine profiling using dried blood spot (DBS) technology in drug discovery / Wensheng Lang, Jenson Qi, and Gary W. Caldwell
  • In vitro trapping and screening of reactive metabolites using liquid chromatography-mass spectrometry / Zhengyin Yan and Gary W. Caldwell
  • Quantitative assessment of reactive metabolites / Jie Chen ... [et al.]
  • In vitro assessment of the reactivity of acyl glucuronides / Rongfang Fran Xu ... [et at.]
  • In vitro comet assay for testing genotoxicity of chemicals / Haixia Lin, Nan Mei, and Mugimane G. Manjanatha
  • Assessing DNA damage using a reporter gene system / Michael Biss and Wei Xiao
  • Improved AMES test for genotoxicity assessment of drugs : preincubation assay using a low concentration of dimethyl sulfoxide / Atsushi Hakura
  • Methods for using the mouse lymphoma assay to screen for chemical mutagenicity and photo-mutagenicity / Nan Mei, Xiaoqing Guo, and Martha M. Moore.
Thoroughly revised and updated, Optimization in Drug Discovery: In Vitro Methods, Second Edition presents a wide spectrum of in vitro assays including formulation, plasma binding, absorption and permeability, cytochrome P450 (CYP) and UDP-glucuronosyltransferases (UGT) metabolism, CYP inhibition and induction, drug transporters, drug-drug interactions via assessment of reactive metabolites, genotoxicity, and chemical and photo-mutagenicity assays. Written for the Methods in Pharmacology and Toxicology series, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible protocols, and tips on troubleshooting and avoiding known pitfalls. Expert authors have developed and utilized these in vitro assays to achieve drug-like characteristics in addition to efficacy properties and good safety profiles of drug candidates. Comprehensive and up-to-date, Optimization in Drug Discovery: In Vitro Methods, Second Edition aims to guide researchers down the difficult path to successful drug discovery and development.
  • Small molecule formulation screening strategies in drug discovery / Gary W. Caldwell ... [et al.]
  • Assessment of drug plasma protein binding in drug discovery / Dennis Kalamaridis and Nayan Patel
  • Drug partition in red blood cells / Dennis Kalamaridis and Karen DiLoreto
  • Permeability assessment using 5-day cultured caco-2 cell monolayers / Gary W. Caldwell ... [et al.]
  • In situ single pass perfused rat intestinal model / Maria Markowska and L. Mark Kao
  • Metabolic stability assessed by liver microsomes and hepatocytes / Kevin J. Coe and Tatiana Koudriakova
  • Metabolic assessment in alamethicin-activated liver microsomes : co-activating CYPs and UGTs / Gary W. Caldwell and Zhengyin Yan
  • Phenotyping UDP-glucuronosyltransferases (UGTs) involved in human drug metabolism : an update / Michael H. Court
  • In vitro CYP/FMO reaction phenotyping / Carlo Sensenhauser
  • Human pregnane X receptor (hPXR) activation assay in stable cell lines / Judy L. Raucy
  • Characterization of constitutive androstane receptor (CAR) activation / Caitlin Lynch, Haishan Li, and Hongbing Wang
  • DNA binding (gel retardation assay) analysis for Identification of aryl hydrocarbon (Ah) receptor agonists and antagonists / Anatoly A. Soshilov and Michael S. Denison
  • Cell-based assays for identification of aryl hydrocarbon receptor (AhR) activators / Guochun He ... [et al.]
  • In vitro CYP induction using human hepatocytes / Monica Singer, Carlo Sensenhauser, and Shannon Dallas
  • Assessment of CYP3A4 time-dependent inhibition in plated and suspended human hepatocytes / J. George Zhang and David M. Stresser
  • Evaluation of time-dependent CYP3A4 inhibition using human hepatocytes / Yuan Chen and Adrian J. Fretland
  • Rapidly distinguishing reversible and time-dependent CYP450 inhibition using human liver microsomes, co-incubation, and continuous fluorometric Kinetic analyses / Gary W. Caldwell and Zhengyin Yan
  • Identification of time-dependent CYP inhibitors using human liver microsomes (HLM) / Kevin J. Coe, Judith Skaptason, and Tatiana Koudriakova
  • CYP time-dependent inhibition (TDI) using an IC50 shift assay with stable isotopic labeled substrate Probes to facilitate liquid chromatography/mass spectrometry analyses / Gary W. Caldwell and Zhengyin Yan
  • Screening for p-glycoprotein (Pgp) substrates and inhibitors / Qing Wang and Tina M. Sauerwald
  • In vitro characterization of intestinal transporter, breast cancer resistance protein (BCRP) / Chris Bode and Li-Bin Li
  • In vitro characterization of intestinal and hepatic transporters : MRP2 / Ravindra Varma Alluri ... [et al.]
  • In vitro characterization of hepatic transporters OATP1B1 and OATP1B3 / Blair Miezeiewski and Allison McLaughlin
  • In vitro characterization of renal transporters OAT1, OAT3, and OCT2 / Ying Wang and Nicole Behler
  • General guidelines for setting up an in vitro LC/MS/MS assay / John A. Masucci and Gary W. Caldwell
  • Metabolite identification in drug discovery / Wing W. Lam ... [et al.]
  • Drug, lipid, and acylcarnitine profiling using dried blood spot (DBS) technology in drug discovery / Wensheng Lang, Jenson Qi, and Gary W. Caldwell
  • In vitro trapping and screening of reactive metabolites using liquid chromatography-mass spectrometry / Zhengyin Yan and Gary W. Caldwell
  • Quantitative assessment of reactive metabolites / Jie Chen ... [et al.]
  • In vitro assessment of the reactivity of acyl glucuronides / Rongfang Fran Xu ... [et at.]
  • In vitro comet assay for testing genotoxicity of chemicals / Haixia Lin, Nan Mei, and Mugimane G. Manjanatha
  • Assessing DNA damage using a reporter gene system / Michael Biss and Wei Xiao
  • Improved AMES test for genotoxicity assessment of drugs : preincubation assay using a low concentration of dimethyl sulfoxide / Atsushi Hakura
  • Methods for using the mouse lymphoma assay to screen for chemical mutagenicity and photo-mutagenicity / Nan Mei, Xiaoqing Guo, and Martha M. Moore.
Thoroughly revised and updated, Optimization in Drug Discovery: In Vitro Methods, Second Edition presents a wide spectrum of in vitro assays including formulation, plasma binding, absorption and permeability, cytochrome P450 (CYP) and UDP-glucuronosyltransferases (UGT) metabolism, CYP inhibition and induction, drug transporters, drug-drug interactions via assessment of reactive metabolites, genotoxicity, and chemical and photo-mutagenicity assays. Written for the Methods in Pharmacology and Toxicology series, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible protocols, and tips on troubleshooting and avoiding known pitfalls. Expert authors have developed and utilized these in vitro assays to achieve drug-like characteristics in addition to efficacy properties and good safety profiles of drug candidates. Comprehensive and up-to-date, Optimization in Drug Discovery: In Vitro Methods, Second Edition aims to guide researchers down the difficult path to successful drug discovery and development.
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Book
1 online resource.
  • Introduction
  • Lead discovery and lead modification
  • Receptors
  • Enzymes
  • Enzyme inhibition and inactivation
  • Dna-interactive agents
  • Drug resistance and drug synergism
  • Drug metabolism
  • Prodrugs and drug delivery systems.
The Organic Chemistry of Drug Design and Drug Action, Third Edition, represents a unique approach to medicinal chemistry based on physical organic chemical principles and reaction mechanisms that rationalize drug action, which allows the reader to extrapolate those core principles and mechanisms to many related classes of drug molecules. This new edition reflects significant changes in the process of drug design over the last decade. It preserves the successful approach of the previous editions while including significant changes in format and coverage. New to this edition: * Updates to all chapters, including new examples and references* Chapter 1 (Introduction): Completely rewritten and expanded as an overview of topics discussed in detail throughout the book* Chapter 2 (Lead Discovery and Lead Modification): Sections on sources of compounds for screening including library collections, virtual screening, and computational methods, as well as hit-to-lead and scaffold hopping; expanded sections on sources of lead compounds, fragment-based lead discovery, and molecular graphics; and deemphasized solid-phase synthesis and combinatorial chemistry* Chapter 3 (Receptors): Drug-receptor interactions, cation-? and halogen bonding; atropisomers; case history of the insomnia drug suvorexant* Chapter 4 (Enzymes): Expanded sections on enzyme catalysis in drug discovery and enzyme synthesis* Chapter 5 (Enzyme Inhibition and Inactivation): New case histories: * for competitive inhibition, the epidermal growth factor receptor tyrosine kinase inhibitor, erlotinib and Abelson kinase inhibitor, imatinib* for transition state analogue inhibition, the purine nucleoside phosphorylase inhibitors, forodesine and DADMe-ImmH, as well as the mechanism of the multisubstrate analog inhibitor isoniazid* for slow, tight-binding inhibition, the dipeptidyl peptidase-4 inhibitor, saxagliptin* Chapter 7 (Drug Resistance and Drug Synergism): This new chapter includes topics taken from two chapters in the previous edition, with many new examples* Chapter 8 (Drug Metabolism): Discussions of toxicophores and reactive metabolites* Chapter 9 (Prodrugs and Drug Delivery Systems): Discussion of antibody-drug conjugates.
(source: Nielsen Book Data)
  • Introduction
  • Lead discovery and lead modification
  • Receptors
  • Enzymes
  • Enzyme inhibition and inactivation
  • Dna-interactive agents
  • Drug resistance and drug synergism
  • Drug metabolism
  • Prodrugs and drug delivery systems.
The Organic Chemistry of Drug Design and Drug Action, Third Edition, represents a unique approach to medicinal chemistry based on physical organic chemical principles and reaction mechanisms that rationalize drug action, which allows the reader to extrapolate those core principles and mechanisms to many related classes of drug molecules. This new edition reflects significant changes in the process of drug design over the last decade. It preserves the successful approach of the previous editions while including significant changes in format and coverage. New to this edition: * Updates to all chapters, including new examples and references* Chapter 1 (Introduction): Completely rewritten and expanded as an overview of topics discussed in detail throughout the book* Chapter 2 (Lead Discovery and Lead Modification): Sections on sources of compounds for screening including library collections, virtual screening, and computational methods, as well as hit-to-lead and scaffold hopping; expanded sections on sources of lead compounds, fragment-based lead discovery, and molecular graphics; and deemphasized solid-phase synthesis and combinatorial chemistry* Chapter 3 (Receptors): Drug-receptor interactions, cation-? and halogen bonding; atropisomers; case history of the insomnia drug suvorexant* Chapter 4 (Enzymes): Expanded sections on enzyme catalysis in drug discovery and enzyme synthesis* Chapter 5 (Enzyme Inhibition and Inactivation): New case histories: * for competitive inhibition, the epidermal growth factor receptor tyrosine kinase inhibitor, erlotinib and Abelson kinase inhibitor, imatinib* for transition state analogue inhibition, the purine nucleoside phosphorylase inhibitors, forodesine and DADMe-ImmH, as well as the mechanism of the multisubstrate analog inhibitor isoniazid* for slow, tight-binding inhibition, the dipeptidyl peptidase-4 inhibitor, saxagliptin* Chapter 7 (Drug Resistance and Drug Synergism): This new chapter includes topics taken from two chapters in the previous edition, with many new examples* Chapter 8 (Drug Metabolism): Discussions of toxicophores and reactive metabolites* Chapter 9 (Prodrugs and Drug Delivery Systems): Discussion of antibody-drug conjugates.
(source: Nielsen Book Data)

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