β-arrestins and biased signalling in gonadotropin receptors.

β-arrestins and biased signalling in gonadotropin receptors. Minerva Ginecol. 2018 Jul 10;: Authors: De Pascali F, Reiter E Abstract Gonadotropin receptors include the follicle stimulating hormone receptor (FSHR) and the luteinizing hormone/choriogonadotropin receptor (LHCGR), both belong to the G protein- coupled receptor (GPCR) superfamily and being essential to reproduction. FSHR is activated by follicle stimulating hormone (FSH) while LHCGR is activated by either luteinizing hormone (LH) or choriogonadotropin (CG). Upon ligand binding, gonadotropin receptors undergo conformational changes that leads to the activation of the heterotrimeric G protein, resulting in the production of different second messengers. Gonadotropin receptors can also recruit and bind β-arrestins. This particular class of scaffold proteins were initially identified to mediate GPCRs desensitization and recycling, but it is now well established that β-arrestins can also initiate Gs- independent signalling by assembling signalling modules. Furthermore, new advances in structural biology and biophysical techniques has revealed novel activation mechanisms in the way β-arrestins and G proteins control signalling in time and space. The ability of different ligands to preferentially elicit G- or β-arrestin-mediated signalling is known as functional selectivity or biased signalling. This new concept has switched the view of pharmacology efficacy from monodimenti...
Source: Minerva Ginecologica - Category: OBGYN Tags: Minerva Ginecol Source Type: research