title: [The pharmacological effect of allosteric regulation at GPCR heterodimer].
abstract: Traditionally GPCR can exist as monomer, and its function is linear. The signal is transduced when the ligand binds to the orthosteric site. It has been reported that GPCR can form homodimer or heterodimer. In the dimers, allosteric sites will form when ligand binds to one monomer and then regulates of another monomer. Therefore the signaling pathway and the function of the receptor will be changed. Compared to orthosteric agonists, allosteric modulators have a number of potential advantages, which make allosteric modulators as a drug discovery candidate for GPCR. Herein, we introduce the concept of allosteric regulation at GPCR dimers, and its impact on the function of the receptor. We also introduce the drug screening methods of allosteric regulator, and those will contribute to drug discovery for GPCR.
authors.affiliation: Qufu Normal University, Qufu 273165, China.
authors.forename: Ning
authors.initials: N
authors.lastname: Zhang
authors.forename: Jing
authors.initials: J
authors.lastname: Chen
authors.forename: Lei
authors.initials: L
authors.lastname: Gong
authors.forename: Lu-Lu
authors.initials: LL
authors.lastname: Liu
authors.forename: Bo
authors.initials: B
authors.lastname: Bai
mesh_terms: D000494:Allosteric Regulation / Q000187:drug effects; D000495:Allosteric Site; D000818:Animals; D019281:Dimerization; D058786:GABA-B Receptor Agonists / Q000494:pharmacology; D006801:Humans; D010636:Phenols / Q000494:pharmacology; D043562:Receptors, G-Protein-Coupled / Q000378:metabolism / Q000502:physiology*
chemical_list: C438607:2,6-di-tert-butyl-4-(3-hydroxy-2,2-dimethylpropyl)phenol; D058786:GABA-B Receptor Agonists; D010636:Phenols; D043562:Receptors, G-Protein-Coupled