Literature DB >> 15304558

Allosteric modulators: the new generation of receptor antagonist.

Terry Kenakin1.   

Abstract

Allosteric antagonists modulate the affinity and/or efficacy of agonists for receptors. Although the manner in which this modulation can occur can mimic that of simple competitive antagonists, allosteric antagonists possess unique properties that can present seemingly capricious profiles of antagonism. These unique properties also offer potentially useful patterns for therapeutic utility. This review summarizes methods to detect allosteric antagonism and some special properties of these receptor modulators.

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Year:  2004        PMID： 15304558     DOI： 10.1124/mi.4.4.6

Source DB:  PubMed          Journal:  Mol Interv        ISSN： 1534-0384


  22 in total

Review 1.  Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery.

Authors:  Terry Kenakin; Laurence J Miller
Journal:  Pharmacol Rev       Date:  2010-04-14       Impact factor: 25.468

2.  Discovery of very late antigen-4 (VLA-4, alpha4beta1 integrin) allosteric antagonists.

Authors:  Alexandre Chigaev; Yang Wu; D Bart Williams; Yelena Smagley; Larry A Sklar
Journal:  J Biol Chem       Date:  2010-12-03       Impact factor: 5.157

3.  Structure-based ligand discovery targeting orthosteric and allosteric pockets of dopamine receptors.

Authors:  J Robert Lane; Pavel Chubukov; Wei Liu; Meritxell Canals; Vadim Cherezov; Ruben Abagyan; Raymond C Stevens; Vsevolod Katritch
Journal:  Mol Pharmacol       Date:  2013-09-10       Impact factor: 4.436

4.  Transmitted/founder and chronic HIV-1 envelope proteins are distinguished by differential utilization of CCR5.

Authors:  Zahra F Parker; Shilpa S Iyer; Craig B Wilen; Nicholas F Parrish; Kelechi C Chikere; Fang-Hua Lee; Chuka A Didigu; Reem Berro; Per Johan Klasse; Benhur Lee; John P Moore; George M Shaw; Beatrice H Hahn; Robert W Doms
Journal:  J Virol       Date:  2012-12-26       Impact factor: 5.103

Review 5.  Allosteric Modulation of GPCRs: New Insights and Potential Utility for Treatment of Schizophrenia and Other CNS Disorders.

Authors:  Daniel J Foster; P Jeffrey Conn
Journal:  Neuron       Date:  2017-05-03       Impact factor: 17.173

6.  A new small-molecule antagonist inhibits Graves' disease antibody activation of the TSH receptor.

Authors:  Susanne Neumann; Elena Eliseeva; Joshua G McCoy; Giorgio Napolitano; Cesidio Giuliani; Fabrizio Monaco; Wenwei Huang; Marvin C Gershengorn
Journal:  J Clin Endocrinol Metab       Date:  2010-12-01       Impact factor: 5.958

7.  Mutation-specific potency and efficacy of cystic fibrosis transmembrane conductance regulator chloride channel potentiators.

Authors:  Antonella Caputo; Alexandre Hinzpeter; Emanuela Caci; Nicoletta Pedemonte; Nicole Arous; Marco Di Duca; Olga Zegarra-Moran; Pascale Fanen; Luis J V Galietta
Journal:  J Pharmacol Exp Ther       Date:  2009-06-02       Impact factor: 4.030

Review 8.  Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders.

Authors:  P Jeffrey Conn; Craig W Lindsley; Jens Meiler; Colleen M Niswender
Journal:  Nat Rev Drug Discov       Date:  2014-09       Impact factor: 84.694

9.  Allosteric theory: taking therapeutic advantage of the malleable nature of GPCRs.

Authors:  Terry Kenakin
Journal:  Curr Neuropharmacol       Date:  2007-09       Impact factor: 7.363

10.  Influence of fluorophore and linker composition on the pharmacology of fluorescent adenosine A1 receptor ligands.

Authors:  Jillian G Baker; Richard Middleton; Luke Adams; Lauren T May; Stephen J Briddon; Barrie Kellam; Stephen J Hill
Journal:  Br J Pharmacol       Date:  2010-01-26       Impact factor: 8.739
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