Literature DB >> 16580596

Keynote review: allosterism in membrane receptors.

Zhan-Guo Gao1, Kenneth A Jacobson.   

Abstract

Allosteric modulation of membrane receptors has been intensively studied in the past three decades and is now considered to be an important indirect mechanism for the control of receptor function. The allosteric site on the GABA(A) receptor is the target for the most widely prescribed sleep medicines, the benzodiazepines. Cinacalcet, an allosteric enhancer of the calcium-sensing receptor, is used to treat secondary hyperparathyroidism. Allosteric ligands might be especially valuable to control receptors for which the design of selective orthosteric agonists or antagonists has been elusive, such as muscarinic acetylcholine receptors.

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Year:  2006        PMID： 16580596     DOI： 10.1016/S1359-6446(05)03689-5

Source DB:  PubMed          Journal:  Drug Discov Today        ISSN： 1359-6446            Impact factor:   7.851


  21 in total

Review 1.  The significance of G protein-coupled receptor crystallography for drug discovery.

Authors:  John A Salon; David T Lodowski; Krzysztof Palczewski
Journal:  Pharmacol Rev       Date:  2011-12       Impact factor: 25.468

2.  An HSV vector system for selection of ligand-gated ion channel modulators.

Authors:  Rahul Srinivasan; Shaohua Huang; Suchita Chaudhry; Adrian Sculptoreanu; David Krisky; Michael Cascio; Peter A Friedman; William C de Groat; Darren Wolfe; Joseph C Glorioso
Journal:  Nat Methods       Date:  2007-08-05       Impact factor: 28.547

3.  The different ways through which specificity works in orthosteric and allosteric drugs.

Authors:  Ruth Nussinov; Chung-Jung Tsai
Journal:  Curr Pharm Des       Date:  2012       Impact factor: 3.116

4.  Structure-activity relationships of new 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric enhancers of the A3 adenosine receptor.

Authors:  Anikó Göblyös; Zhan-Guo Gao; Johannes Brussee; Roberto Connestari; Sabrina Neves Santiago; Kai Ye; Adriaan P Ijzerman; Kenneth A Jacobson
Journal:  J Med Chem       Date:  2006-06-01       Impact factor: 7.446

5.  Coarse-grained free energy functions for studying protein conformational changes: a double-well network model.

Authors:  Jhih-Wei Chu; Gregory A Voth
Journal:  Biophys J       Date:  2007-08-17       Impact factor: 4.033

6.  Protection from myocardial ischemia/reperfusion injury by a positive allosteric modulator of the A₃ adenosine receptor.

Authors:  Lili Du; Zhan-Guo Gao; Kasem Nithipatikom; Adriaan P Ijzerman; Jacobus P D van Veldhoven; Kenneth A Jacobson; Garrett J Gross; John A Auchampach
Journal:  J Pharmacol Exp Ther       Date:  2011-10-19       Impact factor: 4.030

Review 7.  Rational design of dualsteric GPCR ligands: quests and promise.

Authors:  Klaus Mohr; Christian Tränkle; Evi Kostenis; Elisabetta Barocelli; Marco De Amici; Ulrike Holzgrabe
Journal:  Br J Pharmacol       Date:  2010-02-05       Impact factor: 8.739

Review 8.  Activation and regulation of purinergic P2X receptor channels.

Authors:  Claudio Coddou; Zonghe Yan; Tomas Obsil; J Pablo Huidobro-Toro; Stanko S Stojilkovic
Journal:  Pharmacol Rev       Date:  2011-07-07       Impact factor: 25.468

9.  Functionally biased modulation of A(3) adenosine receptor agonist efficacy and potency by imidazoquinolinamine allosteric enhancers.

Authors:  Zhan-Guo Gao; Dennis Verzijl; Annelien Zweemer; Kai Ye; Anikó Göblyös; Adriaan P Ijzerman; Kenneth A Jacobson
Journal:  Biochem Pharmacol       Date:  2011-06-21       Impact factor: 5.858

10.  The role of a sodium ion binding site in the allosteric modulation of the A(2A) adenosine G protein-coupled receptor.

Authors:  Hugo Gutiérrez-de-Terán; Arnault Massink; David Rodríguez; Wei Liu; Gye Won Han; Jeremiah S Joseph; Ilia Katritch; Laura H Heitman; Lizi Xia; Adriaan P Ijzerman; Vadim Cherezov; Vsevolod Katritch; Raymond C Stevens
Journal:  Structure       Date:  2013-11-07       Impact factor: 5.006
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