Human β-Defensin 1 and β-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors
| Autor: | Katie T. Freeman, Jay W. Schaub, Stacey L. Wilber, Carrie Haskell-Luevano, Cody J. Lensing, Marvin L. Dirain, Srinivasa R. Tala, Viktor Flores, Mark D. Ericson, Erica M. Haslach, Branden A. Smeester, Robert C. Speth, Natalie Eick, Anamika Singh, Danielle N. Adank |
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| Rok vydání: | 2018 |
| Předmět: |
Male
0301 basic medicine Agonist beta-Defensins medicine.drug_class Endogeny Ligands Article 03 medical and health sciences 0302 clinical medicine Drug Discovery Cyclic AMP medicine Animals Humans Amino Acid Sequence Receptor Defensin integumentary system Chemistry Receptors Melanocortin Ligand (biochemistry) Cell biology Mice Inbred C57BL 030104 developmental biology Molecular Medicine Melanocortin hormones hormone substitutes and hormone antagonists 030217 neurology & neurosurgery Function (biology) |
| Zdroj: | Journal of Medicinal Chemistry. 61:3738-3744 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/acs.jmedchem.8b00251 |
| Popis: | 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: | OpenAIRE |
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