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Article

Allosteric modulation of G protein-coupled receptors: a pharmacological perspective.

Neuropharmacology - 1 Jan 2011

Keov Peter, Sexton Patrick M, Christopoulos Arthur

Abstract excerpt

G protein-coupled receptor (GPCR)-based drug discovery has traditionally focused on targeting the orthosteric site for the endogenous agonist. However, many GPCRs possess allosteric sites that offer enormous potential for greater selectivity in drug action. The complex behaviors ascribed to allosteric ligands also present challenges to those interested in preclinical lead discovery. These challenges include the...

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PMID: 20637785
DOI: 10.1016/j.neuropharm.2010.07.010

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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