Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review

Functional antagonists of the Apelin (APJ) receptor

In: Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010.
[updated ].
Free Books & Documents
Review

Functional antagonists of the Apelin (APJ) receptor

Patrick R. Maloney et al.
Free Books & Documents

Excerpt

The recently discovered apelin receptor (APJ, AGTRL-1, APLNR) system has emerged as a critical mediator of cardiovascular homeostasis and is involved in the pathogenesis of hypertension, heart failure, atherosclerosis, and other cardiovascular diseases. We disclose the first discovery and characterization of a potent (1.7 – 2.2 μM), kojic acid based small molecule APJ functional antagonist in cell-based assays that is >37 fold selective over the closely related angiotensin II type 1 (AT1) receptor, derived from an high throughput screening (HTS) of the ~330,600 compound MLSMR collection. This antagonist showed no significant binding activity against 29 other GPCRs, except to the κ-opioid receptor (<50%I at 10 μM). The synthetic methodology, development of structure-activity relationship (SAR), and initial in vitro pharmacologic characterization are also presented. This probe molecule provides a useful tool compound for investigators interested in understanding apelin receptor pharmacology and function.

PubMed Disclaimer

References

    1. De Falco M, De Luca L, Onori N, Cavallotti I, Artigiano F, Esposito V, De Luca B, Laforgia V, Groeger AM, De Luca A. Apelin expression in normal human tissues. In Vivo. 2002;16:333–336. - PubMed
    1. Kleinz MJ, Davenport AP. Immunocytochemical localization of the endogenous vasoactive peptide apelin to human vascular and endocardial endothelial cells. Regul Pept. 2004;118:119–125. - PubMed
    1. Kleinz MJ, Skepper JN, Davenport AP. Immunocytochemical localization of the apelin receptor, APJ, to human cardiomyocytes, vascular smooth muscle and endothelial cells. Regul Pept. 2005;126:233–240. - PubMed
    1. Quazi R, Palaniswamy C, Frishman WH. The emerging role of apelin in cardiovascular disease and health. Cardiol Rev. 2009;17:283–286. - PubMed
    1. Sorli SC, van den Berghe L, Masri B, Knibiehler B, Audigier Y. Therapeutic potential of interfering with apelin signaling. Drug Discov Today. 2006;11:1100–1106. - PubMed

LinkOut - more resources