Human β-Defensin 1 and β-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors.

Autor: Ericson MD, Singh A; Departments of Medicinal Chemistry and Pharmacodynamics , University of Florida , Gainesville , Florida 32610 , United States., Tala SR; Departments of Medicinal Chemistry and Pharmacodynamics , University of Florida , Gainesville , Florida 32610 , United States., Haslach EM; Departments of Medicinal Chemistry and Pharmacodynamics , University of Florida , Gainesville , Florida 32610 , United States., Dirain MLS; Departments of Medicinal Chemistry and Pharmacodynamics , University of Florida , Gainesville , Florida 32610 , United States., Schaub JW; Departments of Medicinal Chemistry and Pharmacodynamics , University of Florida , Gainesville , Florida 32610 , United States., Flores V; Departments of Medicinal Chemistry and Pharmacodynamics , University of Florida , Gainesville , Florida 32610 , United States., Eick N; Departments of Medicinal Chemistry and Pharmacodynamics , University of Florida , Gainesville , Florida 32610 , United States., Lensing CJ, Freeman KT, Smeester BA, Adank DN, Wilber SL, Speth R; College of Pharmacy , Nova Southeastern University , Fort Lauderdale , Florida 33328 , United States.; Department of Pharmacology and Physiology , Georgetown University , Washington, D.C. 20057 , United States., Haskell-Luevano C; Departments of Medicinal Chemistry and Pharmacodynamics , University of Florida , Gainesville , Florida 32610 , United States.
Jazyk: angličtina
Zdroj: Journal of medicinal chemistry [J Med Chem] 2018 Apr 26; Vol. 61 (8), pp. 3738-3744. Date of Electronic Publication: 2018 Apr 09.
DOI: 10.1021/acs.jmedchem.8b00251
Abstrakt: β-Defensin 3 (BD3) was identified as a ligand for the melanocortin receptors (MCRs) in 2007, although the pharmacology activity of BD3 has not been clearly elucidated. Herein, it is demonstrated that human BD3 and mouse BD3 are full micromolar agonists at the MCRs. Furthermore, mouse β-defensin 1 (BD1) and human BD1 are also MCR micromolar agonists. This work identifies BD1 as an endogenous MCR ligand and clarifies the controversial role of BD3 as a micromolar agonist.
Databáze: MEDLINE
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