Apelin/APJ system: a novel promising therapy target for thrombotic diseases

摘要

APJ,which was initially identified as a gene with closest homology to the angiotensin Ⅱ type 1 receptor,is a seven transmembrane G protein-coupled receptor.Apelin is an endogenous ligand of the APJ originally isolated from bovine stomach extracts.There are several isoforms of apelin.Apelin preproproteins contain 77 amino-acid residues,which can be cleaved to form shorter bioactive isoforms,including apelin-36,apelin-17,apelin-13,apelin-12,and so on.Apelin/APJ receptor is extensively distributed in the central nervous system and peripheral tissues.Apelin/APJ system involves in a wide range of physiological and pathological functions.For example,apelin lowers blood pressure via a NO/cGMP-dependent mechanism.Apelin-13 maintains the Ca2+ transient against ischemia/reperfusion in cardiomyocytes.Furthermore,apelin-13 promotes cell prolifera tion and angiogenesis via PI3K/AKT activation [1,2].