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Book
online resource (xii, 252 pages) : illustrations (some color)
This book focuses on applications of compound library design and virtual screening to expand the bioactive chemical space, to target hopping of chemotypes to identify synergies within related drug discovery projects or to repurpose known drugs, to propose mechanism of action of compounds, or to identify off-target effects by cross-reactivity analysis. Both ligand-based and structure-based in silico approaches, as reviewed in this book, play important roles for all these applications. Computational chemogenomics is expected to increase the quality and productivity of drug discovery and lead.
This book focuses on applications of compound library design and virtual screening to expand the bioactive chemical space, to target hopping of chemotypes to identify synergies within related drug discovery projects or to repurpose known drugs, to propose mechanism of action of compounds, or to identify off-target effects by cross-reactivity analysis. Both ligand-based and structure-based in silico approaches, as reviewed in this book, play important roles for all these applications. Computational chemogenomics is expected to increase the quality and productivity of drug discovery and lead.
Medical Library (Lane)
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CRCNETBASE Unknown
Book
1 online resource (xxiv, 553 pages)
Book
1 online resource (366 pages) : illustrations.
Book
1 online resource.
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.
  • 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.
Book
1 online resource.
"A peptidomimetic is a small protein-like chain designed to mimic a peptide with adjusted molecular properties such as enhanced stability or biological activity. It is a very powerful approach for the generation of small-molecule-based drugs as enzyme inhibitors or receptor ligands.Peptidomimetics in Organic and Medicinal Chemistry outlines the concepts and synthetic strategies underlying the building of bioactive compounds of a peptidomimetic nature. Topics covered include the chemistry of unnatural amino acids, peptide- and scaffold-based peptidomimetics, amino acid-side chain isosteres, backbone isosteres, dipeptide isosteres, beta-turn peptidomimetics, proline-mimetics as turn inducers, cyclic scaffolds, amino acid surrogates, and scaffolds for combinatorial chemistry of peptidomimetics. Case studies in the hit-to-lead process, such as the development of integrin ligands and thrombin inhibitors, illustrate the successful application of peptidomimetics in drug discovery"-- Provided by publisher.
"Peptidomimetics in Organic and Medicinal Chemistry outlines the concepts and synthetic strategies underlying the building of bioactive compounds of a peptidomimetic nature"-- Provided by publisher.
"A peptidomimetic is a small protein-like chain designed to mimic a peptide with adjusted molecular properties such as enhanced stability or biological activity. It is a very powerful approach for the generation of small-molecule-based drugs as enzyme inhibitors or receptor ligands.Peptidomimetics in Organic and Medicinal Chemistry outlines the concepts and synthetic strategies underlying the building of bioactive compounds of a peptidomimetic nature. Topics covered include the chemistry of unnatural amino acids, peptide- and scaffold-based peptidomimetics, amino acid-side chain isosteres, backbone isosteres, dipeptide isosteres, beta-turn peptidomimetics, proline-mimetics as turn inducers, cyclic scaffolds, amino acid surrogates, and scaffolds for combinatorial chemistry of peptidomimetics. Case studies in the hit-to-lead process, such as the development of integrin ligands and thrombin inhibitors, illustrate the successful application of peptidomimetics in drug discovery"-- Provided by publisher.
"Peptidomimetics in Organic and Medicinal Chemistry outlines the concepts and synthetic strategies underlying the building of bioactive compounds of a peptidomimetic nature"-- Provided by publisher.
Book
1 online resource (xii, 176 pages) : illustrations (some color).
  • Getting started
  • Discovery and preclinical work
  • Preparing for the clinic
  • Transferring technology
  • Commercialization and entrepreneurship
  • Concluding thoughts.
Written by the founders of the SPARK program at Stanford University, this book is a practical guide designed for professors, students and clinicians at academic research institutions who are interested in learning more about the drug development process and how to help their discoveries become the novel drugs of the future. Often many potentially transformative basic science discoveries are not pursued because they are deemed "too early" to attract industry interest. There are simple, relatively cost-effective things that academic researchers can do to advance their findings to the point that they can be tested in the clinic or attract more industry interest.
  • Getting started
  • Discovery and preclinical work
  • Preparing for the clinic
  • Transferring technology
  • Commercialization and entrepreneurship
  • Concluding thoughts.
Written by the founders of the SPARK program at Stanford University, this book is a practical guide designed for professors, students and clinicians at academic research institutions who are interested in learning more about the drug development process and how to help their discoveries become the novel drugs of the future. Often many potentially transformative basic science discoveries are not pursued because they are deemed "too early" to attract industry interest. There are simple, relatively cost-effective things that academic researchers can do to advance their findings to the point that they can be tested in the clinic or attract more industry interest.
Book
xii, 176 pages
  • Getting started
  • Discovery and preclinical work
  • Preparing for the clinic
  • Transferring technology
  • Commercialization and entrepreneurship
  • Concluding thoughts.
Written by the founders of the SPARK program at Stanford University, this book is a practical guide designed for professors, students and clinicians at academic research institutions who are interested in learning more about the drug development process and how to help their discoveries become the novel drugs of the future. Often many potentially transformative basic science discoveries are not pursued because they are deemed "too early" to attract industry interest. There are simple, relatively cost-effective things that academic researchers can do to advance their findings to the point that they can be tested in the clinic or attract more industry interest.
  • Getting started
  • Discovery and preclinical work
  • Preparing for the clinic
  • Transferring technology
  • Commercialization and entrepreneurship
  • Concluding thoughts.
Written by the founders of the SPARK program at Stanford University, this book is a practical guide designed for professors, students and clinicians at academic research institutions who are interested in learning more about the drug development process and how to help their discoveries become the novel drugs of the future. Often many potentially transformative basic science discoveries are not pursued because they are deemed "too early" to attract industry interest. There are simple, relatively cost-effective things that academic researchers can do to advance their findings to the point that they can be tested in the clinic or attract more industry interest.
Medical Library (Lane)
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RM301.25 .P733 2014 Unknown
Book
1 online resource : text file, PDF
  • section I. A theory of evaluating drugs
  • section II. A theory of evidence in drug development
  • section III. Additional topics.
  • section I. A theory of evaluating drugs
  • section II. A theory of evidence in drug development
  • section III. Additional topics.
Book
online resource (xvi, 245 pages) : illustrations
  • Section I. A theory of evaluating drugs
  • section II. A theory of evidence in drug development
  • section III. Additional topics.
  • Section I. A theory of evaluating drugs
  • section II. A theory of evidence in drug development
  • section III. Additional topics.
Medical Library (Lane)
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CRCNETBASE Unknown
Book
online resource (viii, 198 pages) : illustrations (some color)
Medical Library (Lane)
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SPRINGER Unknown
Book
online resource (xii, 89 pages) : illustrations
  • Introduction
  • Application of prodrug chemistry to GLP-1
  • Experimental procedures
  • Characterization of prodrugs
  • Conclusion
  • Appendix I. Schematic synthesis of longer acting prodrugs
  • Appendix II: Structure of peptides in Table A.1
  • Appendix III: Structure of peptides in table A.2
  • Appendix IV: Structure of peptides in table A.3
  • Appendix V: Structure of peptides in table A.4 Appendix VI: Structure of peptides in table A.5
  • Appendix VII. Structure of peptides in table A.6
  • Appendix VIII: Acylataion of HO-His7, GLP(8-37)
  • Appendix IX: A note on nomenclature.
  • Introduction
  • Application of prodrug chemistry to GLP-1
  • Experimental procedures
  • Characterization of prodrugs
  • Conclusion
  • Appendix I. Schematic synthesis of longer acting prodrugs
  • Appendix II: Structure of peptides in Table A.1
  • Appendix III: Structure of peptides in table A.2
  • Appendix IV: Structure of peptides in table A.3
  • Appendix V: Structure of peptides in table A.4 Appendix VI: Structure of peptides in table A.5
  • Appendix VII. Structure of peptides in table A.6
  • Appendix VIII: Acylataion of HO-His7, GLP(8-37)
  • Appendix IX: A note on nomenclature.
Medical Library (Lane)
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SPRINGER Unknown
Book
1 online resource.
  • Introduction
  • Application of prodrug chemistry to GLP-1
  • Experimental procedures
  • Characterization of prodrugs
  • Conclusion
  • Appendix I. Schematic synthesis of longer acting prodrugs
  • Appendix II: Structure of peptides in Table A.1
  • Appendix III: Structure of peptides in table A.2
  • Appendix IV: Structure of peptides in table A.3
  • Appendix V: Structure of peptides in table A.4 Appendix VI: Structure of peptides in table A.5
  • Appendix VII. Structure of peptides in table A.6
  • Appendix VIII: Acylataion of HO-His7, GLP(8-37)
  • Appendix IX: A note on nomenclature.
  • Introduction
  • Application of prodrug chemistry to GLP-1
  • Experimental procedures
  • Characterization of prodrugs
  • Conclusion
  • Appendix I. Schematic synthesis of longer acting prodrugs
  • Appendix II: Structure of peptides in Table A.1
  • Appendix III: Structure of peptides in table A.2
  • Appendix IV: Structure of peptides in table A.3
  • Appendix V: Structure of peptides in table A.4 Appendix VI: Structure of peptides in table A.5
  • Appendix VII. Structure of peptides in table A.6
  • Appendix VIII: Acylataion of HO-His7, GLP(8-37)
  • Appendix IX: A note on nomenclature.
Book
online resource (xv, 306 pages) : illustrations
  • Omics & microarrays revisited
  • The commercial microarrays
  • Supports & surface chemistries
  • The arraying processes
  • Gene expression microarray-based applications
  • Protein microarray applications
  • Multiplex assays.
  • Omics & microarrays revisited
  • The commercial microarrays
  • Supports & surface chemistries
  • The arraying processes
  • Gene expression microarray-based applications
  • Protein microarray applications
  • Multiplex assays.
Medical Library (Lane)
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CRCNETBASE Unknown
Book
online resource (ix, 293 pages) : color illustrations
  • Introduction / Linda O. Narhi
  • High-Throughput Biophysical Approaches to Therapeutic Protein Development / Feng He, Vladimir I. Razinkov
  • Techniques for Higher-Order Structure Determination / James Kranz, Fatma AlAzzam, Atul Saluja
  • Biophysical Techniques for Protein Size Distribution Analysis / Ziping Wei, Alla Polozova
  • Qualification of Biophysical Methods for the Analysis of Protein Therapeutics / Yijia Jiang, Cynthia Li, John Gabrielson
  • Application of Biophysics to the Early Developability Assessment of Therapeutic Candidates and Its Application to Enhance Developability Properties / Hasige Sathish, Nicolas Angell, David Lowe
  • Application of Biophysics in Formulation, Process, and Product Characterization: Selected Case Studies / Satish K. Singh, Qin Zou, Min Huang
  • Biophysical Analysis in Support of Development of Protein Pharmaceuticals / Sreedhara Alavattam, Barthelemy Demeule
  • Case Studies Applying Biophysical Techniques to Better Characterize Protein Aggregates and Particulates of Varying Size / Tingting Wang, Sangeeta B. Joshi
  • Investigation of Nonconformance During Protein Therapeutic Manufacturing / Zai-Qing Wen, Gianni Torraca, Guiyang Li
  • Higher-Order Structure and Protein Aggregate Characterization of Protein Therapeutics: Perspectives from Good Manufacturing Practices and Regulatory Guidance / Evi B. Struble, John F. Cipollo.
This book can be used to provide insight into this important application of biophysics for those who are planning a career in protein therapeutic development, and for those outside this area who are interested in understanding it better. The initial chapters describe the underlying theory, and strengths and weaknesses of the different techniques commonly used during therapeutic development. The majority of the chapters discuss the applications of these techniques, including case studies, across the product lifecycle from early discovery, where the focus is on identifying targets, and screening for potential drug product candidates, through expression and purification, large scale production, formulation development, lot-to-lot comparability studies, and commercial support including investigations.
  • Introduction / Linda O. Narhi
  • High-Throughput Biophysical Approaches to Therapeutic Protein Development / Feng He, Vladimir I. Razinkov
  • Techniques for Higher-Order Structure Determination / James Kranz, Fatma AlAzzam, Atul Saluja
  • Biophysical Techniques for Protein Size Distribution Analysis / Ziping Wei, Alla Polozova
  • Qualification of Biophysical Methods for the Analysis of Protein Therapeutics / Yijia Jiang, Cynthia Li, John Gabrielson
  • Application of Biophysics to the Early Developability Assessment of Therapeutic Candidates and Its Application to Enhance Developability Properties / Hasige Sathish, Nicolas Angell, David Lowe
  • Application of Biophysics in Formulation, Process, and Product Characterization: Selected Case Studies / Satish K. Singh, Qin Zou, Min Huang
  • Biophysical Analysis in Support of Development of Protein Pharmaceuticals / Sreedhara Alavattam, Barthelemy Demeule
  • Case Studies Applying Biophysical Techniques to Better Characterize Protein Aggregates and Particulates of Varying Size / Tingting Wang, Sangeeta B. Joshi
  • Investigation of Nonconformance During Protein Therapeutic Manufacturing / Zai-Qing Wen, Gianni Torraca, Guiyang Li
  • Higher-Order Structure and Protein Aggregate Characterization of Protein Therapeutics: Perspectives from Good Manufacturing Practices and Regulatory Guidance / Evi B. Struble, John F. Cipollo.
This book can be used to provide insight into this important application of biophysics for those who are planning a career in protein therapeutic development, and for those outside this area who are interested in understanding it better. The initial chapters describe the underlying theory, and strengths and weaknesses of the different techniques commonly used during therapeutic development. The majority of the chapters discuss the applications of these techniques, including case studies, across the product lifecycle from early discovery, where the focus is on identifying targets, and screening for potential drug product candidates, through expression and purification, large scale production, formulation development, lot-to-lot comparability studies, and commercial support including investigations.
Medical Library (Lane)
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Medical Library (Lane) Status
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SPRINGER Unknown
Book
1 online resource (xxvi, 698 pages)
  • Introduction to biopharmaceuticals
  • Distinctions of biologic versus small molecule platforms in drug development
  • Financing biologic drug development
  • Application of biotechnology in drug discovery and early development
  • Large-scale production of recombinant proteins
  • Clinical pharmacology, toxicology, and therapeutic dosage & response
  • Clinical evaluation and regulatory approval & enforcement of biopharmaceuticals
  • Pharmacoeconomics and drug pricing / Garrison
  • Antibodies and derivatives
  • Hematopoietic growth and coagulation factors
  • Cytokines and interferons
  • Hormones
  • Enzymes
  • Vaccines / Hu, Ho
  • Other biopharmaceutical products
  • Advances in personalized medicine : pharmacogenetics in drug therapy
  • Gene and cell therapy
  • Pharmacoeconomics, outcome, and health technology assessment research in drug development
  • Summary and future prospects.
  • Introduction to biopharmaceuticals
  • Distinctions of biologic versus small molecule platforms in drug development
  • Financing biologic drug development
  • Application of biotechnology in drug discovery and early development
  • Large-scale production of recombinant proteins
  • Clinical pharmacology, toxicology, and therapeutic dosage & response
  • Clinical evaluation and regulatory approval & enforcement of biopharmaceuticals
  • Pharmacoeconomics and drug pricing / Garrison
  • Antibodies and derivatives
  • Hematopoietic growth and coagulation factors
  • Cytokines and interferons
  • Hormones
  • Enzymes
  • Vaccines / Hu, Ho
  • Other biopharmaceutical products
  • Advances in personalized medicine : pharmacogenetics in drug therapy
  • Gene and cell therapy
  • Pharmacoeconomics, outcome, and health technology assessment research in drug development
  • Summary and future prospects.
Book
1 online resource (720 pages) : color illustrations
  • Part I. Fundamentalsin Drug Research
  • 1. Drug Research Yesterday, Today and Tomorrow
  • 2. The Role of Serendipityin Drug Research
  • 3. Classical Drug Research
  • 4. ProteinLigand Interactionsas the Basis for Drug Action
  • 5. Optical Activity and Biological Effects
  • Part II. Discovery and Optimizationof Lead Compounds
  • 6. Screeningfor Lead Structures
  • 7. Screening Technologies for LeadDiscovery
  • 8. Optimizationof Lead Structures
  • 9. Designingprodrugs
  • 10. Peptidomimetics
  • Part III. Experimental and Theoretical Methods
  • 11. Combinatorics: Chemistry With Big Numbers
  • 12. Gene Technology in drug research
  • 13. Experimental Methods of Structure Determination
  • 14. The Spatial Structure of Biomolecules
  • 15. Molecular Modelling
  • 16. Conformational Analysis
  • Part IV. StructureActivity Relationships and Design Approaches
  • 17.Pharmacophore Hypothesis and Molecular Comparisons
  • 18. Quantitative StructureActivityRelationships
  • 19. From in vitro to in vivo:Optimization of ADME-Tox Properties
  • 20. ProteinModeling and Structure-BasedDrug Design
  • 21. ACase Study: Structure-Based Inhibtor Design for tRNA-Guanine Transglycosylase
  • Part V. Drugs and drug action: Successes of stucture-based design
  • 22. Howdrugs act: Concepts for therapy
  • 23. Inhibitors of hydrolases With an acyl-enzymeintermediate
  • 24. Asparticprotease inhibitors
  • 25. Inhibitorsof hydrolysing metalloenzymes
  • 26. Inhibitorsof transferases
  • 27. Inhibitors ofoxidoreductases
  • 28. Agonists and antagonistsof nuclear receptors
  • 29. Agonists and antagonists of membrane-bound
  • 30. Ligands forchannels, pores and transporters
  • 31. Ligands for surfacereceptors
  • 32. Biologicals: Peptides, proteins, nucleotidesand macrolides as drugs.
Unique work on structure-based drug design, covering multiple aspects of drug discovery and development. Fully colored, many images, computer animations of 3D structures (these only in electronic form). Makes the spatial aspects of interacting molecules clear to the reader, covers multiple applications and methods in drug design. Structures by mode of action, no therapeutic areas. Of high relevance for academia and industrial research. Focus on gene technology in drug design, omics-technologies computational methods experimental techniques of structure determinationmultiple examples on mode of action of current drugs, ADME-tox properties in drug development, QSAR methods, combinatorial chemistry, biologicals, ribosome, targeting protein-protein interfaces.
  • Part I. Fundamentalsin Drug Research
  • 1. Drug Research Yesterday, Today and Tomorrow
  • 2. The Role of Serendipityin Drug Research
  • 3. Classical Drug Research
  • 4. ProteinLigand Interactionsas the Basis for Drug Action
  • 5. Optical Activity and Biological Effects
  • Part II. Discovery and Optimizationof Lead Compounds
  • 6. Screeningfor Lead Structures
  • 7. Screening Technologies for LeadDiscovery
  • 8. Optimizationof Lead Structures
  • 9. Designingprodrugs
  • 10. Peptidomimetics
  • Part III. Experimental and Theoretical Methods
  • 11. Combinatorics: Chemistry With Big Numbers
  • 12. Gene Technology in drug research
  • 13. Experimental Methods of Structure Determination
  • 14. The Spatial Structure of Biomolecules
  • 15. Molecular Modelling
  • 16. Conformational Analysis
  • Part IV. StructureActivity Relationships and Design Approaches
  • 17.Pharmacophore Hypothesis and Molecular Comparisons
  • 18. Quantitative StructureActivityRelationships
  • 19. From in vitro to in vivo:Optimization of ADME-Tox Properties
  • 20. ProteinModeling and Structure-BasedDrug Design
  • 21. ACase Study: Structure-Based Inhibtor Design for tRNA-Guanine Transglycosylase
  • Part V. Drugs and drug action: Successes of stucture-based design
  • 22. Howdrugs act: Concepts for therapy
  • 23. Inhibitors of hydrolases With an acyl-enzymeintermediate
  • 24. Asparticprotease inhibitors
  • 25. Inhibitorsof hydrolysing metalloenzymes
  • 26. Inhibitorsof transferases
  • 27. Inhibitors ofoxidoreductases
  • 28. Agonists and antagonistsof nuclear receptors
  • 29. Agonists and antagonists of membrane-bound
  • 30. Ligands forchannels, pores and transporters
  • 31. Ligands for surfacereceptors
  • 32. Biologicals: Peptides, proteins, nucleotidesand macrolides as drugs.
Unique work on structure-based drug design, covering multiple aspects of drug discovery and development. Fully colored, many images, computer animations of 3D structures (these only in electronic form). Makes the spatial aspects of interacting molecules clear to the reader, covers multiple applications and methods in drug design. Structures by mode of action, no therapeutic areas. Of high relevance for academia and industrial research. Focus on gene technology in drug design, omics-technologies computational methods experimental techniques of structure determinationmultiple examples on mode of action of current drugs, ADME-tox properties in drug development, QSAR methods, combinatorial chemistry, biologicals, ribosome, targeting protein-protein interfaces.
Book
1 online resource : ill.
Book
1 online resource.
  • Basic principles of preformulation studies
  • Ionisation constants
  • Partitioning affinity
  • Solubility
  • Dissolution
  • Salt selection
  • Physical form I : crystalline materials
  • Physical form II : amorphous materials
  • Stability assessment
  • Particle properties
  • Powder properties.
  • Basic principles of preformulation studies
  • Ionisation constants
  • Partitioning affinity
  • Solubility
  • Dissolution
  • Salt selection
  • Physical form I : crystalline materials
  • Physical form II : amorphous materials
  • Stability assessment
  • Particle properties
  • Powder properties.
dx.doi.org Wiley Online Library

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