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

doi:10.1021/acs.jmedchem.8b00251

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

Medicinal Chemistry

Research output: Contribution to journal › Article › peer-review

4 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 language	English (US)
Pages (from-to)	3738-3744
Number of pages	7
Journal	Journal of medicinal chemistry
Volume	61
Issue number	8
DOIs	https://doi.org/10.1021/acs.jmedchem.8b00251
State	Published - Apr 26 2018

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Publisher Copyright:
© 2018 American Chemical Society.

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10.1021/acs.jmedchem.8b00251

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6007841

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Ericson, M. D., Singh, A., Tala, S. R., Haslach, E. M., Dirain, M. L. S., Schaub, J. W., Flores, V., Eick, N., Lensing, C. J., Freeman, K. T., Smeester, B. A., Adank, D. N., Wilber, S. L., Speth, R., & Haskell-Luevano, C. (2018). Human β-Defensin 1 and β-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors. Journal of medicinal chemistry, 61(8), 3738-3744. https://doi.org/10.1021/acs.jmedchem.8b00251

Ericson, MD, Singh, A, Tala, SR, Haslach, EM, Dirain, MLS, Schaub, JW, Flores, V, Eick, N, Lensing, CJ, Freeman, KT, Smeester, BA, Adank, DN, Wilber, SL, Speth, R & Haskell-Luevano, C 2018, 'Human β-Defensin 1 and β-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors', Journal of medicinal chemistry, vol. 61, no. 8, pp. 3738-3744. https://doi.org/10.1021/acs.jmedchem.8b00251

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

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

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