Not all arrestins are created equal: Therapeutic implications of the functional diversity of the β-arrestins in the heart.

ABSTRACT: The two ubiquitous, outside the retina, G protein-coupled receptor (GPCR) adapter proteins, β-arrestin-1 and -2 (also known as arrestin-2 and -3, respectively), have three major functions in cells: GPCR desensitization, i.e., receptor decoupling from G-proteins; GPCR internalization via clathrin-coated pits; and signal transduction independently of or in parallel to G-proteins. Both β-arrestins are expressed in the heart and regulate a large number of cardiac GPCRs. The latter constitute the single most commonly targeted receptor class by Food and Drug Administration-approved cardiovascular drugs, with about one-third of all currently used in the clinic medications affecting GPCR function. Since β-arrestin-1 and -2 play important roles in signaling and function of several GPCRs, in particu

SUBMITTER: Lymperopoulos A 

PROVIDER: S-EPMC6391623 | biostudies-literature | 2019 Feb

REPOSITORIES: biostudies-literature