Allosteric modulation and functional selectivity of G protein-coupled receptors.
Agonists of a single G protein-coupled receptor (GPCR) may activate distinct signaling pathways. Functional selectivity, an emerging concept with therapeutic relevance for GPCRs, may be due to conformational selection or stabilization with respect to particular agonists, receptor dimerization, variable expression levels of GPCRs and downstream signaling molecules, and allosteric modulation. Allosteric modulators may have potential advantages over orthosteric ligands, including greater selectivity and safety. This review focuses on functional selectivity resulting from allosteric modulation.
Zhan-Guo
ZG
Gao
Kenneth A
KA
Jacobson
D000494:Allosteric Regulation; D000818:Animals; D006801:Humans; D043562:Receptors, G-Protein-Coupled / Q000819:agonists* / Q000737:chemistry
D043562:Receptors, G-Protein-Coupled