Author "Kristensen, Anders S."

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1. Historical Data Analysis for Extending Dynamic Line Ratings Across Power Transmission Systems [2018]

  • Viafora, Nicola, Moller, Jakob G., Olsen, Rasmus A., Kristensen, Anders S., and Holboll, Joachim
  • 2018 IEEE International Conference on Probabilistic Methods Applied to Power Systems (PMAPS) Probabilistic Methods Applied to Power Systems (PMAPS), 2018 IEEE International Conference on. :1-6 Jun, 2018

2. Identification and functional evaluation of GRIA1 missense and truncation variants in individuals with ID: An emerging neurodevelopmental syndrome [2022]

  • Ismail, Vardha, Zachariassen, Linda G., Godwin, Annie, Sahakian, Mane, Ellard, Sian, Stals, Karen L., Baple, Emma, Brown, Kate Tatton, Foulds, Nicola, Wheway, Gabrielle, Parker, Matthew O., Lyngby, Signe M., Pedersen, Miriam G., Desir, Julie, Bayat, Allan, Musgaard, Maria, Guille, Matthew, Kristensen, Anders S., and Baralle, Diana
  • American journal of human genetics. 109(7):1217-1241

3. Self-deployable drag sail folded nine times [2021]

  • Nikolajsen, Jan Á. and Kristensen, Anders S.
  • In Advances in Space Research 15 November 2021 68(10):4242-4251

4. Three-dimensional missense tolerance ratio analysis [2021]

  • Perszyk, Riley E., Kristensen, Anders S., Lyuboslavsky, Polina, and Traynelis, Stephen F.
  • Genome research. 31(8):1447-1461

5. Risk Mitigation of Poor Power Quality Issues of Standalone Wind Turbines: An Efficacy Study of Synchronous Reference Frame (SRF) Control [2020]

  • Mehmood, Saqib, Qureshi, Amin, and Kristensen, Anders S.
  • Energies. Sept 1, 2020, Vol. 13 Issue 17, p1gy, 14 p.

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7. Identification and functional evaluation of GRIA1 missense and truncation variants in patients with intellectual disability: an emerging neurodevelopmental phenotype [2022]

  • Ismail, Vardha, Zachariassen, Linda, Godwin, Annie, Sahakian, Mane, Ellard, Sian, Stals, Karen L, Tatton Brown, Kate, Foulds, Nicola, Wheway, Gabrielle, Parker, Matthew O., Lyngby, Signe M, Pedersen, Miriam G, Desir, Julie, Bayat, Allan, Lusgaard, Maria, Guille, Matthew, Kristensen, Anders S, and Baralle, Diana

8. Structural rearrangement of the intracellular domains during AMPA receptor activation [2016]

  • Zachariassen, Linda G., Katchan, Ljudmila, Jensen, Anna G., Pickering, Darryl S., Plested, Andrew J. R., and Kristensen, Anders S.
  • Proceedings of the National Academy of Sciences of the United States of America, 2016 Jul 01. 113(27), E3950-E3959.

9. Discovery of the First Highly Selective Antagonist of the GluK3 Kainate Receptor Subtype. [2022]

  • Chałupnik, Paulina, Vialko, Alina, Pickering, Darryl S., Hinkkanen, Markus, Donbosco, Stephanie, Møller, Thor C., Jensen, Anders A., Nielsen, Birgitte, Bay, Yasmin, Kristensen, Anders S., Johansen, Tommy N., Łątka, Kamil, Bajda, Marek, and Szymańska, Ewa
  • International Journal of Molecular Sciences; Aug2022, Vol. 23 Issue 15, p8797-8797, 16p
Subjects
GLUTAMATE receptors, CENTRAL nervous system, MOLECULAR dynamics, NEURAL transmission, MOLECULAR docking, and ION channels
Abstract
Kainate receptors belong to the family of glutamate receptors ion channels, which are responsible for the majority of rapid excitatory synaptic transmission in the central nervous system. The therapeutic potential of kainate receptors is still poorly understood, which is also due to the lack of potent and subunit-selective pharmacological tools. In search of selective ligands for the GluK3 kainate receptor subtype, a series of quinoxaline-2,3-dione analogues was synthesized and pharmacologically characterized at selected recombinant ionotropic glutamate receptors. Among them, compound 28 was found to be a competitive GluK3 antagonist with submicromolar affinity and unprecedented high binding selectivity, showing a 400-fold preference for GluK3 over other homomeric receptors GluK1, GluK2, GluK5 and GluA2. Furthermore, in functional assays performed for selected metabotropic glutamate receptor subtypes, 28 did not show agonist or antagonist activity. The molecular determinants underlying the observed affinity profile of 28 were analyzed using molecular docking and molecular dynamics simulations performed for individual GluK1 and GluK3 ligand-binding domains. [ABSTRACT FROM AUTHOR]

10. A high-affinity, dimeric inhibitor of PSD-95 bivalently interacts with PDZ1-2 and protects against ischemic brain damage [2012]

  • Bach, Anders, Clausen, Bettina H., Moller, Magda, Vestergaard, Bente, Chi, Celestine N., Round, Adam, Sorensen, Pernille L., Nissen, Klaus B., Kastrup, Jette S., Gajhede, Michael, Jemth, Per, Kristensen, Anders S., Lundström, Patrik, Lambertsen, Kate L., and Stromgaard, Kristian
  • Proceedings of the National Academy of Sciences of the United States of America. 109(9):3317-3322
Subjects
Medical and Health Sciences, Medicin och hälsovetenskap, drug discovery, ischemic stroke, and protein-protein interactions
Abstract
Inhibition of the ternary protein complex of the synaptic scaffolding protein postsynaptic density protein-95 (PSD-95), neuronal nitric oxide synthase (nNOS), and the N-methyl-D-aspartate (NMDA) receptor is a potential strategy for treating ischemic brain damage, but high-affinity inhibitors are lacking. Here we report the design and synthesis of a novel dimeric inhibitor, Tat-NPEG4(IETDV)(2) (Tat-N-dimer), which binds the tandem PDZ1-2 domain of PSD-95 with an unprecedented high affinity of 4.6 nM, and displays extensive protease-resistance as evaluated in vitro by stability-measurements in human blood plasma. X-ray crystallography, NMR, and small-angle X-ray scattering (SAXS) deduced a true bivalent interaction between dimeric inhibitor and PDZ1-2, and also provided a dynamic model of the conformational changes of PDZ1-2 induced by the dimeric inhibitor. A single intravenous injection of Tat-N-dimer (3 nmol/g) to mice subjected to focal cerebral ischemia reduces infarct volume with 40% and restores motor functions. Thus, Tat-N-dimer is a highly efficacious neuroprotective agent with therapeutic potential in stroke.

11. Interaction of Antidepressants with the Serotonin and Norepinephrine Transporters: MUTATIONAL STUDIES OF THE S1 SUBSTRATE BINDING POCKET [2012]

  • Sørensen, Lena, Andersen, Jacob, Thomsen, Mette, Hansen, Stinna M.R., Zhao, Xiaobei, Sandelin, Albin, Strømgaard, Kristian, and Kristensen, Anders S.
  • In Journal of Biological Chemistry 21 December 2012 287(52):43694-43707

12. Solid-Phase Synthesis and Biological Evaluation of Joro Spider Toxin-4 from Nephila clavata [2011]

  • BARSLUND, Anne F, POULSEN, Mette H, BACH, Tinna B, LUCAS, Simon, KRISTENSEN, Anders S, and STRØMGAARD, Kristian
  • Journal of natural products (Print). 74(3):483-486
Subjects
Pharmacology drugs, Pharmacologie, galénique, Sciences biologiques et medicales, Biological and medical sciences, Sciences medicales, Medical sciences, Toxicologie, Toxicology, Toxicologie des poisons d'origine animale. Antivenins, Animal poisons toxicology. Antivenoms, Arthropoda, Invertebrata, Activité biologique, Biological activity, Actividad biológica, Affinité, Affinity, Afinidad, Aminoamide, Aminoamida, Antagoniste, Antagonist, Antagonista, Arachnida, Araignée, Spider, Araña, Carboxamide, Carboxamida, Dipeptide, Dipeptides, Dipéptido, Diphénols, Diphenols, Difenoles, Guanidines, Guanidinas, In vitro, Peptide, Peptides, Péptido, Phase solide, Solid phase, Fase sólida, Récepteur glutamate, Glutamate receptor, Receptor glutámato, Récepteur ionotropique, Ionotropic receptor, Receptor ionotropico, Synthèse chimique, Chemical synthesis, Síntesis química, Toxique, Poison, Tóxico, Arginine dérivé, Asparaginamide dérivé, Nephila clavata, Ornithinamide dérivé, Pentane-1,5-diamine dérivé, and Toxine JSTX 4
Abstract
Polyamine toxins from orb weaver spiders are attractive pharmacological tools particularly for studies of ionotropic glutamate (iGlu) receptors in the brain. These polyamine toxins are biosynthesized in a combinatorial manner, providing a plethora of related, but structurally complex toxins to be exploited in biological studies. Here, we have used solid-phase synthetic methodology for the efficient synthesis of Joro spider toxin-4 (JSTX-4) (1) from Nephila clavata, providing sufficient amounts of the toxin for biological evaluation at iGlu receptor subtypes using electrophysiology. Biological evaluation revealed that JSTX-4 inhibits iGlu receptors only in high μM concentrations, thereby being substantially less potent than structurally related polyamine toxins.

13. Structure-activity relationship studies of citalopram derivatives: examining substituents conferring selectivity for the allosteric site in the 5-HT transporter [2016]

  • Larsen, M Andreas B, Plenge, Per, Andersen, Jacob, Eildal, Jonas NN, Kristensen, Anders S, Bogeso, Klaus P, Gether, Ulrik, Stromgaard, Kristian, Bang-Andersen, Benny, and Loland, Claus J
  • British Journal of Pharmacology. March, 2016, Vol. 173 Issue 5, p925, 12 p.

14. The Glutamate Receptor GluR5 Agonist (S)-2-Amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic Acid and the 8-Methyl Analogue: Synthesis, Molecular Pharmacology, and Biostructural Characterization [2009]

  • CLAUSEN, Rasmus P, NAUR, Peter, NIELSEN, Birgitte, PICKERING, Darryl S, BREHM, Lotte, GAJHEDE, Michael, KROGSGAARD-LARSEN, Povl, KASTRUP, Jette S, KRISTENSEN, Anders S, GREENWOOD, Jeremy R, STRANGE, Mette, BRAUNER-OSBORNE, Hans, JENSEN, Anders A, NIELSEN, Anne Sophie T, GENESER, Ulla, and RINGGAARD, Lone M
  • Journal of medicinal chemistry (Print). 52(15):4911-4922
Subjects
Pharmacology drugs, Pharmacologie, galénique, Sciences biologiques et medicales, Biological and medical sciences, Sciences medicales, Medical sciences, Pharmacologie. Traitements medicamenteux, Pharmacology. Drug treatments, Neuropharmacologie, Neuropharmacology, Neuromédiateurs. Neurotransmission. Récepteurs, Neurotransmitters. Neurotransmission. Receptors, Système glutamatergique (aspartate et autres aminoacides excitateurs), Glutamatergic system (aspartate and other excitatory aminoacids), Activité biologique, Biological activity, Actividad biológica, Agoniste, Agonist, Agonista, Diffraction RX, X ray diffraction, Difracción RX, Dérivé de l'acide propionique, Propionic acid derivatives, Propionico ácido derivado, Dérivé de l'isoxazole, Isoxazole derivatives, Electrophysiologie, Electrophysiology, Electrofisiología, In vitro, Mode liaison, Binding mode, Modo de enlace, Modèle moléculaire, Molecular model, Modelo molecular, Modélisation, Modeling, Modelización, Pharmacologie, Pharmacology, Farmacología, Récepteur glutamate, Glutamate receptor, Receptor glutámato, Récepteur kaïnate, Kainate receptor, Receptor kainato, Structure cristalline, Crystalline structure, Estructura cristalina, Structure moléculaire, Molecular structure, Estructura molecular, Synthèse chimique, Chemical synthesis, Síntesis química, Cyclohepta[d]isoxazole dérivé, Cycloheptaisoxazole, and Sous-unité GluR5
Abstract
The design, synthesis, and pharmacological characterization of a highly potent and selective glutamate GluR5 agonist is reported. (S)-2-Amino-3-((RS)-3-hydroxy-8-methyl-7,8-dihydro-6H-cyclohepta-[d]isoxazol-4-yl)propionic acid (5) is the 8-methyl analogue of (S)-2-amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic acid ((S)-4-AHCP, 4). Compound 5 displays an improved selectivity profile compared to 4. A versatile stereoselective synthetic route for this class of compounds is presented along with the characterization of the binding affinity of 5 to ionotropic glutamate receptors (iGluRs). Functional characterization of 5 at cloned iGluRs using a calcium imaging assay and voltage-clamp recordings show a different activation of GluR5 compared to (S)-glutamic acid (Glu), kainic acid (KA, 1), and (S)-2-amino-3-(3-hydroxy-5-tert-butyl-4-isoxazolyl)propionic acid ((S)-ATPA, 3) as previously demonstrated for 4. An X-ray crystallographic analysis of 4 and computational analyses of 4 and 5 bound to the GluR5 agonist binding domain (ABD) are presented, including a watermap analysis, which suggests that water molecules in the agonist binding site are important selectivity determinants.

15. From the Selective Serotonin Transporter Inhibitor Citalopram to the Selective Norepinephrine Transporter Inhibitor Talopram : Synthesis and Structure-Activity Relationship Studies [2008]

  • EILDAL, Jonas N. N, ANDERSEN, Jacob, KRISTENSEN, Anders S, JØRGENSEN, Anne Marie, BANG-ANDERSEN, Benny, JØRGENSEN, Morten, and STRØMGAARD, Kristian
  • Journal of medicinal chemistry (Print). 51(10):3045-3048
Subjects
Pharmacology drugs, Pharmacologie, galénique, Sciences biologiques et medicales, Biological and medical sciences, Sciences medicales, Medical sciences, Pharmacologie. Traitements medicamenteux, Pharmacology. Drug treatments, Neuropharmacologie, Neuropharmacology, Neuromédiateurs. Neurotransmission. Récepteurs, Neurotransmitters. Neurotransmission. Receptors, Système catécholaminergique, Catecholaminergic system, Système sérotoninergique, Serotoninergic system, Inhibiteur recapture, Reuptake inhibitor, Inhibidor recaptura, Amine biogène, Biogenic amine, Amina biógena, Amine tertiaire, Tertiary amine, Amina terciaria, Catécholamine, Catecholamine, Catecolamina, Citalopram, Fluor Composé organique, Fluorine Organic compounds, Fluor Compuesto orgánico, Neurotransmetteur, Neurotransmitter, Neurotransmisor, Nitrile, Nitrilo, Noradrénaline, Norepinephrine, Noradrenalina, Protéine transport, Carrier protein, Proteína transportador, Relation structure activité, Structure activity relation, Relación estructura actividad, Synthèse chimique, Chemical synthesis, Síntesis química, Sélectivité, Selectivity, Selectividad, Sérotonine, Serotonin, Serotonina, Talopram, Transport membranaire, Membrane transport, Transporte membranal, Transporteur de la sérotonine, Serotonin transporter, Transportador de la serotonina, Isobenzofurane dérivé, Isobenzofurane-5-carbonitrile(1,3-dihydro-1-[3-(diméthylamino)propyl]-1-[4-fluorophényl]), and Transporteur noradrénaline
Abstract
Citalopram and talopram are structurally closely related, but they have very distinct pharmacological profiles as selective inhibitors of the serotonin and norepinephrine transporters, respectively. A systematic structure-activity relationship study was performed, in which each of the four positions distinguishing the two compounds were varied. The inhibitory potencies of the resulting 16 compounds were tested at both serotonin and norepinephrine transporters. This showed that particularly two of the four positions are determinants for the biological activity.

16. Analogues of 3-Hydroxyisoxazole-Containing Glutamate Receptor Ligands Based on the 3-Hydroxypyrazole-Moiety: Design, Synthesis and Pharmacological Characterization [2014]

  • Jørgensen, Lars, Nielsen, Birgitte, Pickering, Darryl S., Kristensen, Anders S., Frydenvang, Karla, Madsen, Ulf, and Clausen, Rasmus P.
  • Neurochemical Research. October 2014 39(10):1895-1905

17. Inhibition of AMPA Receptors by Polyamine Toxins is Regulated by Agonist Efficacy and Stargazin [2014]

  • Poulsen, Mette H., Lucas, Simon, Strømgaard, Kristian, and Kristensen, Anders S.
  • Neurochemical Research. October 2014 39(10):1906-1913

18. Bioisosteric modifications of 2-arylureidobenzoic acids: Selective noncompetitive antagonists for the homomeric kainate receptor subtype GluR5 [2004]

  • VALGEIRSSON, Jon, NIELSEN, Elsebet O, PETERS, Dan, MATHIESEN, Claus, KRISTENSEN, Anders S, and MADSEN, Ulf
  • Journal of medicinal chemistry (Print). 47(27):6948-6957
Subjects
Pharmacology drugs, Pharmacologie, galénique, Sciences biologiques et medicales, Biological and medical sciences, Sciences medicales, Medical sciences, Pharmacologie. Traitements medicamenteux, Pharmacology. Drug treatments, Neuropharmacologie, Neuropharmacology, Neuromédiateurs. Neurotransmission. Récepteurs, Neurotransmitters. Neurotransmission. Receptors, Système glutamatergique (aspartate et autres aminoacides excitateurs), Glutamatergic system (aspartate and other excitatory aminoacids), Antagoniste, Antagonist, Antagonista, Benzoïque acide dérivé, Benzoic acid derivatives, Benzoico ácido derivado, Brome composé organique, Organic bromine compounds, Chlore composé organique, Organic chlorine compounds, Electrophysiologie, Electrophysiology, Electrofisiología, In vitro, Relation structure activité, Structure activity relation, Relación estructura actividad, Récepteur glutamate, Glutamate receptor, Receptor glutámato, Récepteur kaïnate, Kainate receptor, Receptor kainato, Synthèse chimique, Chemical synthesis, Síntesis química, Sélectivité, Selectivity, Selectividad, Tétrazole dérivé, Tetrazole derivatives, Tetrazol derivado, Urées, Ureas, Bioisostère, Sous unité GluR5, and Urée(1-[3-bromophényl]-3-[5-chloro-2-tétrazolylphényl])
Abstract
2-Arylureidobenzoic acids (AUBAs) have recently been presented as the first series of selective noncompetitive GluR5 antagonists. In this paper we have modified the acidic moiety of the AUBAs by introducing different acidic and neutral groups, and similarly, we have replaced the urea linker of the AUBAs with other structurally related linkers. Replacing the acid with neutral substituents led to inactive compounds in all instances, showing that an acidic moiety is necessary for activity. Replacing the carboxylic moiety in 2a with a sulfonic acid (5c) or a tetrazole ring (5d) improved the potency at GluR5 receptors (compounds 5c and 5d showed IC50 values of 1.5 and 2.0 μM, respectively, compared to compound 2a with IC50 = 4.8 μM). Compound 5c did not show improved in vivo activity in the ATPA rigidity test compared to 2a, whereas compound 5d was 4 times more potent than 2a. All compounds wherein the urea linker had been replaced showed lower or no activity. The results described extend the knowledge of structure-activity relationships for the AUBAs, and compound 5d may prove to be a good candidate for studying GluR5 receptors in vitro and in vivo.

19. Targeting Protein-Protein Interactions with Trimeric Ligands: High Affinity Inhibitors of the MAGUK Protein Family [2015]

  • Nissen, Klaus B., Haugaard-Kedstrom, Linda M., Wilbek, Theis S., Nielsen, Line S., Åberg, Emma, Kristensen, Anders S., Bach, Anders, Jemth, Per, and Stromgaard, Kristian
  • PLOS ONE. 10(2)
Subjects
Medical and Health Sciences, Basic Medicine, Microbiology in the medical area, Medicin och hälsovetenskap, Medicinska och farmaceutiska grundvetenskaper, Mikrobiologi inom det medicinska området, Medical Biotechnology, Medical Biotechnology (with a focus on Cell Biology (including Stem Cell Biology), Molecular Biology, Microbiology, Biochemistry or Biopharmacy), Medicinsk bioteknologi, Medicinsk bioteknologi (med inriktning mot cellbiologi (inklusive stamcellsbiologi), molekylärbiologi, mikrobiologi, and biokemi eller biofarmaci)
Abstract
PDZ domains in general, and those of PSD-95 in particular, are emerging as promising drug targets for diseases such as ischemic stroke. We have previously shown that dimeric ligands that simultaneously target PDZ1 and PDZ2 of PSD-95 are highly potent inhibitors of PSD-95. However, PSD-95 and the related MAGUK proteins contain three consecutive PDZ domains, hence we envisioned that targeting all three PDZ domains simultaneously would lead to more potent and potentially more specific interactions with the MAGUK proteins. Here we describe the design, synthesis and characterization of a series of trimeric ligands targeting all three PDZ domains of PSD-95 and the related MAGUK proteins, PSD93, SAP-97 and SAP-102. Using our dimeric ligands targeting the PDZ1-2 tandem as starting point, we designed novel trimeric ligands by introducing a PDZ3-binding peptide moiety via a cysteine-derivatized NPEG linker. The trimeric ligands generally displayed increased affinities compared to the dimeric ligands in fluorescence polarization binding experiments and optimized trimeric ligands showed low nanomolar inhibition towards the four MAGUK proteins, thus being the most potent inhibitors described. Kinetic experiments using stopped-flow spectrometry showed that the increase in affinity is caused by a decrease in the dissociation rate of the trimeric ligand as compared to the dimeric ligands, likely reflecting the lower probability of simultaneous dissociation of all three PDZ ligands. Thus, we have provided novel inhibitors of the MAGUK proteins with exceptionally high affinity, which can be used to further elucidate the therapeutic potential of these proteins.

20. Deciphering the Kinetic Binding Mechanism of Dimeric Ligands Using a Potent Plasma-stable Dimeric Inhibitor of Postsynaptic Density Protein-95 as an Example [2010]

  • Chi, Celestine N., Bach, Anders, Gottschalk, Marie, Kristensen, Anders S., Strømgaard, Kristian, and Jemth, Per
  • In Journal of Biological Chemistry 3 September 2010 285(36):28252-28260

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