Pharmacological development of G protein-coupled receptors allosteric modulation / 中国药理学通报

ABSTRACT

G protein-coupled receptors(GPCRs)mediate cell signaling transduction of most hormones and neurological transmitters and behave as the key targets for drug research and development.Recently,the evidence of allosteric modulation of GPCRs has been revealed.Allosteric modulators have the ability to selectively tune responses only in tissues in which the endogenous agonist exerts its physiological effects,and have the potential for greater receptor subtype selectivity.The GPCRs allosteric modulators have been found and some of them have been in clinical use.Under the strategy of allosterism on structure activity relationship and target directed screening,more and more GPCRs allosteric modulators will be developed in the future.