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


ABSTRACT: ?-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 ?-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.

SUBMITTER: Ericson MD 

PROVIDER: S-EPMC6007841 | biostudies-literature | 2018 Apr

REPOSITORIES: biostudies-literature

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

Ericson Mark D MD   Singh Anamika A   Tala Srinivasa R SR   Haslach Erica M EM   Dirain Marvin L S MLS   Schaub Jay W JW   Flores Viktor V   Eick Natalie N   Lensing Cody J CJ   Freeman Katie T KT   Smeester Branden A BA   Adank Danielle N DN   Wilber Stacey L SL   Speth Robert R   Haskell-Luevano Carrie C  

Journal of medicinal chemistry 20180409 8


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. ...[more]

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