G-protein-coupled receptor allosterism: the promise and the problem(s)

Arthur Christopoulos, L T May, Vimesh Ashvinkumar Avlani, Patrick M Sexton

Research output: Contribution to journalArticleOther

41 Citations (Scopus)

Abstract

Allosteric modulators of G-protein-coupled receptors interact with binding sites that are topographically distinct from the orthosteric site recognized by the receptor s endogenous agonist. Allosteric ligands offer a number of advantages over orthosteric drugs, including the potential for greater receptor subtype selectivity and a more physiological regulation of receptor activity. However, the manifestations of allosterism at G-protein-coupled receptors are quite varied, and significant challenges remain for the optimization of screening methods to ensure the routine detection and validation of allosteric ligands.
Original languageEnglish
Pages (from-to)873 - 877
Number of pages5
JournalBiochemical Society Transactions
Volume32
Issue numberPt 5
Publication statusPublished - 2004
Externally publishedYes

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