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2013 1
2014 3
2015 4
2016 2
2022 0
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Page 1
Identification of tetrapeptides from a mixture based positional scanning library that can restore nM full agonist function of the L106P, I69T, I102S, A219V, C271Y, and C271R human melanocortin-4 polymorphic receptors (hMC4Rs).
Haslach EM, Huang H, Dirain M, Debevec G, Geer P, Santos RG, Giulianotti MA, Pinilla C, Appel JR, Doering SR, Walters MA, Houghten RA, Haskell-Luevano C. Haslach EM, et al. J Med Chem. 2014 Jun 12;57(11):4615-28. doi: 10.1021/jm500064t. Epub 2014 May 14. J Med Chem. 2014. PMID: 24517312 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.
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.