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Structure-activity relationships of peptides incorporating a bioactive reverse-turn heterocycle at the melanocortin receptors: identification of a 5800-fold mouse melanocortin-3 receptor (mMC3R) selective antagonist/partial agonist versus the mouse melanocortin-4 receptor (mMC4R).
Singh A, Dirain M, Witek R, Rocca JR, Edison AS, Haskell-Luevano C. Singh A, et al. J Med Chem. 2013 Apr 11;56(7):2747-63. doi: 10.1021/jm301253y. Epub 2013 Mar 25. J Med Chem. 2013. PMID: 23432160 Free PMC article.
Synthesis, biophysical, and pharmacological evaluation of the melanocortin agonist AST3-88: modifications of peptide backbone at Trp 7 position lead to a potent, selective, and stable ligand of the melanocortin 4 receptor (MC4R).
Singh A, Dirain ML, Wilczynski A, Chen C, Gosnell BA, Levine AS, Edison AS, Haskell-Luevano C. Singh A, et al. ACS Chem Neurosci. 2014 Oct 15;5(10):1020-31. doi: 10.1021/cn5000953. Epub 2014 Aug 26. ACS Chem Neurosci. 2014. PMID: 25141170 Free PMC article.
Human β-Defensin 1 and β-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors.
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. Ericson MD, et al. Among authors: singh a. J Med Chem. 2018 Apr 26;61(8):3738-3744. doi: 10.1021/acs.jmedchem.8b00251. Epub 2018 Apr 9. J Med Chem. 2018. PMID: 29578343 Free PMC article.
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