Apelin receptor (APLNR) (APLNR)

The Apelin receptor (APLNR, also known as APJ) is a class A G protein-coupled receptor that binds endogenous peptide hormones apelin (APLN) and elabela (APELA/ELA), regulating cardiovascular function, fluid homeostasis, and angiogenesis. It activates G(i) signaling to inhibit adenylate cyclase and beta-arrestin pathways for receptor internalization, while also functioning as a mechanoreceptor in pathological cardiac hypertrophy. Expressed widely in the central nervous system, heart, lung, kidney, and vasculature, APLNR plays roles in embryonic development including gastrulation and heart morphogenesis, as well as adult processes like blood pressure control and tumor angiogenesis. Dysregulation links it to diseases such as heart failure, hypertension, diabetes, obesity, and cancers like hematologic cancer and cholangiocarcinoma. As a therapeutic target, synthetic agonists like azelaprag and antagonists like ML221 modulate its pathways, though challenges include HIV-1 coreceptor activity and impacts on metabolism or behavior.

Other names

APJAGTRL1Angiotensin receptor-like 1G-protein coupled receptor APJAPJRHG11msr/apj

G(i) protein pathway activation inhibiting adenylate cyclase, Beta-arrestin pathway promoting receptor internalization, Mechanoreceptor activation inducing cardiac hypertrophy (G-protein-independent)