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

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

  • J Med Chem. 2018 Apr 26;61(8):3738-3744. doi: 10.1021/acs.jmedchem.8b00251.
Mark D Ericson,  Anamika Singh 1,  Srinivasa R Tala 1,  Erica M Haslach 1,  Marvin L S Dirain 1,  Jay W Schaub 1,  Viktor Flores 1,  Natalie Eick 1,  Cody J Lensing,  Katie T Freeman,  Branden A Smeester,  Danielle N Adank,  Stacey L Wilber,  Robert Speth 2 3,  Carrie Haskell-Luevano 1
Affiliations

Affiliations

  • 1 Departments of Medicinal Chemistry and Pharmacodynamics , University of Florida , Gainesville , Florida 32610 , United States.
  • 2 College of Pharmacy , Nova Southeastern University , Fort Lauderdale , Florida 33328 , United States.
  • 3 Department of Pharmacology and Physiology , Georgetown University , Washington, D.C. 20057 , United States.
PMID: 29578343 DOI: 10.1021/acs.jmedchem.8b00251
Abstract

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.

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