- G-protein-coupled receptor allosterism: the promise and the problem(s).
G-protein-coupled receptor allosterism: the promise and the problem(s).
Biochemical Society transactions (2004-10-21)
A Christopoulos, L T May, V A Avlani, P M Sexton
PMID15494038
要旨
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.
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