APELIN-36 (HUMAN)

Apelin-36(human) is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC50=8.61). Apelin-36 has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ[1][2][3][4].

HIV-1; HIV-2

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[1] Tatemoto K, Hosoya M, Habata Y, et al. Isolation and characterization of a novel endogenous peptide ligand for the human APJ receptor. Biochem Biophys Res Commun. 1998;251(2):471-476. DOI:10.1006/bbrc.1998.9489
[2] Medhurst AD, Jennings CA, Robbins MJ, et al. Pharmacological and immunohistochemical characterization of the APJ receptor and its endogenous ligand apelin. J Neurochem. 2003;84(5):1162-1172. DOI:10.1046/j.1471-4159.2003.01587.x
[3] Zou MX, Liu HY, Haraguchi Y, Soda Y, Tatemoto K, Hoshino H. Apelin peptides block the entry of human immunodeficiency virus (HIV). FEBS Lett. 2000;473(1):15-18. DOI:10.1016/s0014-5793(00)01487-3
[4] Galon-Tilleman H, Yang H, Bednarek MA, et al. Apelin-36 Modulates Blood Glucose and Body Weight Independently of Canonical APJ Receptor Signaling. J Biol Chem. 2017;292(5):1925-1933. DOI:10.1074/jbc.M116.748103