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

Mark D. Ericson, Anamika Singh, Srinivasa R. Tala, Erica M. Haslach, Marvin L.S. Dirain, Jay W. Schaub, Viktor Flores, Natalie Eick, Cody J. Lensing, Katie T. Freeman, Branden A. Smeester, Danielle N. Adank, Stacey L. Wilber, Robert Speth, Carrie Haskell-Luevano

Research output: Contribution to journalArticlepeer-review

2 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)3738-3744
Number of pages7
JournalJournal of medicinal chemistry
Volume61
Issue number8
DOIs
StatePublished - Apr 26 2018

Bibliographical note

Funding Information:
This work has been supported in part by NIH Grants R01DK097838, RO1DK064250, R01DK091906, and R01DK108893 (C.H.-L.) and an NIH Postdoctoral Fellowship F32DK108402 (M.D.E.). The Haskell-Luevano laboratory is the recipient of a 2017 Wallin Neuroscience Discovery Fund Award through the University of Minnesota.

Publisher Copyright:
© 2018 American Chemical Society.

Copyright:
Copyright 2019 Elsevier B.V., All rights reserved.

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