Molecular basis of β-arrestin coupling to formoterol-bound β₁-adrenoceptor.

ABSTRACT: The β₁-adrenoceptor (β₁AR) is a G-protein-coupled receptor (GPCR) that couples¹ to the heterotrimeric G protein G_s. G-protein-mediated signalling is terminated by phosphorylation of the C terminus of the receptor by GPCR kinases (GRKs) and by coupling of β-arrestin 1 (βarr1, also known as arrestin 2), which displaces G_s and induces signalling through the MAP kinase pathway². The ability of synthetic agonists to induce signalling preferentially through either G proteins or arrestins-known as biased agonism³-is important in drug development, because the therapeutic effect may arise from only one signalling cascade, whereas the other pathway may mediate undesirable side effects⁴. To understand the molecula

SUBMITTER: Lee Y 

PROVIDER: S-EPMC7115876 | biostudies-literature | 2020 Jul

REPOSITORIES: biostudies-literature