Literature DB >> 20558186

Binding site and ligand flexibility revealed by high resolution crystal structures of GluK1 competitive antagonists.

Gregory M Alushin1, David Jane, Mark L Mayer.   

Abstract

The availability of crystal structures for the ligand binding domains of ionotropic glutamate receptors, combined with their key role in synaptic function in the normal and diseased brain, offers a unique selection of targets for pharmaceutical research compared to other drug targets for which the atomic structure of the ligand binding site is not known. Currently only a few antagonist structures have been solved, and these reveal ligand specific conformational changes that hinder rational drug design. Here we report high resolution crystal structures for three kainate receptor GluK1 antagonist complexes which reveal new and unexpected modes of binding, highlighting the continued need for experimentally determined receptor-ligand complexes.
Copyright © 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20558186      PMCID： PMC2976827          DOI： 10.1016/j.neuropharm.2010.06.002

Source DB:  PubMed          Journal:  Neuropharmacology        ISSN： 0028-3908            Impact factor:   5.250


  50 in total

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4.  Abnormal glutamate receptor expression in the medial temporal lobe in schizophrenia and mood disorders.

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Journal:  Neuropsychopharmacology       Date:  2007-02-14       Impact factor: 7.853

5.  A hippocampal GluR5 kainate receptor regulating inhibitory synaptic transmission.

Authors:  V R Clarke; B A Ballyk; K H Hoo; A Mandelzys; A Pellizzari; C P Bath; J Thomas; E F Sharpe; C H Davies; P L Ornstein; D D Schoepp; R K Kamboj; G L Collingridge; D Lodge; D Bleakman
Journal:  Nature       Date:  1997-10-09       Impact factor: 49.962

6.  Full domain closure of the ligand-binding core of the ionotropic glutamate receptor iGluR5 induced by the high affinity agonist dysiherbaine and the functional antagonist 8,9-dideoxyneodysiherbaine.

Authors:  Karla Frydenvang; L Leanne Lash; Peter Naur; Pekka A Postila; Darryl S Pickering; Caleb M Smith; Michael Gajhede; Makoto Sasaki; Ryuichi Sakai; Olli T Pentikaïnen; Geoffrey T Swanson; Jette S Kastrup
Journal:  J Biol Chem       Date:  2009-03-18       Impact factor: 5.157

7.  PHENIX: a comprehensive Python-based system for macromolecular structure solution.

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Journal:  Acta Crystallogr D Biol Crystallogr       Date:  2010-01-22

8.  6-substituted decahydroisoquinoline-3-carboxylic acids as potent and selective conformationally constrained NMDA receptor antagonists.

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Journal:  J Med Chem       Date:  1992-09-18       Impact factor: 7.446

9.  Partial agonism and antagonism of the ionotropic glutamate receptor iGLuR5: structures of the ligand-binding core in complex with domoic acid and 2-amino-3-[5-tert-butyl-3-(phosphonomethoxy)-4-isoxazolyl]propionic acid.

Authors:  Helle Hald; Peter Naur; Darryl S Pickering; Desiree Sprogøe; Ulf Madsen; Daniel B Timmermann; Philip K Ahring; Tommy Liljefors; Arne Schousboe; Jan Egebjerg; Michael Gajhede; Jette Sandholm Kastrup
Journal:  J Biol Chem       Date:  2007-06-20       Impact factor: 5.157

10.  Mechanisms of activation, inhibition and specificity: crystal structures of the NMDA receptor NR1 ligand-binding core.

Authors:  Hiroyasu Furukawa; Eric Gouaux
Journal:  EMBO J       Date:  2003-06-16       Impact factor: 11.598
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  10 in total

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Journal:  Proc Natl Acad Sci U S A       Date:  2013-03-25       Impact factor: 11.205

Review 2.  Structure and mechanism of glutamate receptor ion channel assembly, activation and modulation.

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Journal:  Curr Opin Neurobiol       Date:  2011-02-23       Impact factor: 6.627

Review 3.  The Challenge of Interpreting Glutamate-Receptor Ion-Channel Structures.

Authors:  Mark L Mayer
Journal:  Biophys J       Date:  2017-08-24       Impact factor: 4.033

4.  Piperazine-2,3-dicarboxylic acid derivatives as dual antagonists of NMDA and GluK1-containing kainate receptors.

Authors:  Mark W Irvine; Blaise M Costa; Daniel Dlaboga; Georgia R Culley; Richard Hulse; Caroline L Scholefield; Palmi Atlason; Guangyu Fang; Richard Eaves; Richard Morley; Maria B Mayo-Martin; Mascia Amici; Zuner A Bortolotto; Lucy Donaldson; Graham L Collingridge; Elek Molnár; Daniel T Monaghan; David E Jane
Journal:  J Med Chem       Date:  2011-12-14       Impact factor: 7.446

5.  Novel Functional Properties of Drosophila CNS Glutamate Receptors.

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6.  Mapping the ligand binding sites of kainate receptors: molecular determinants of subunit-selective binding of the antagonist [3H]UBP310.

Authors:  Palmi T Atlason; Caroline L Scholefield; Richard J Eaves; M Belen Mayo-Martin; David E Jane; Elek Molnár
Journal:  Mol Pharmacol       Date:  2010-09-13       Impact factor: 4.436

Review 7.  Structure, Function, and Regulation of the Kainate Receptor.

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Review 8.  Structure, Function, and Pharmacology of Glutamate Receptor Ion Channels.

Authors:  Kasper B Hansen; Lonnie P Wollmuth; Derek Bowie; Hiro Furukawa; Frank S Menniti; Alexander I Sobolevsky; Geoffrey T Swanson; Sharon A Swanger; Ingo H Greger; Terunaga Nakagawa; Chris J McBain; Vasanthi Jayaraman; Chian-Ming Low; Mark L Dell'Acqua; Jeffrey S Diamond; Chad R Camp; Riley E Perszyk; Hongjie Yuan; Stephen F Traynelis
Journal:  Pharmacol Rev       Date:  2021-10       Impact factor: 18.923

9.  Structural mechanism of glutamate receptor activation and desensitization.

Authors:  Joel R Meyerson; Janesh Kumar; Sagar Chittori; Prashant Rao; Jason Pierson; Alberto Bartesaghi; Mark L Mayer; Sriram Subramaniam
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10.  Structural basis of kainate subtype glutamate receptor desensitization.

Authors:  Joel R Meyerson; Sagar Chittori; Alan Merk; Prashant Rao; Tae Hee Han; Mihaela Serpe; Mark L Mayer; Sriram Subramaniam
Journal:  Nature       Date:  2016-08-31       Impact factor: 49.962
  10 in total

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