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Discovery of a β-Hairpin Octapeptide, c[Pro-Arg-Phe-Phe-Dap-Ala-Phe-DPro], Mimetic of Agouti-Related Protein(87-132) [AGRP(87-132)] with Equipotent Mouse Melanocortin-4 Receptor (mMC4R) Antagonist Pharmacology.
Ericson MD, Wilczynski A, Sorensen NB, Xiang Z, Haskell-Luevano C. Ericson MD, et al. Among authors: wilczynski a. J Med Chem. 2015 Jun 11;58(11):4638-47. doi: 10.1021/acs.jmedchem.5b00184. Epub 2015 Apr 21. J Med Chem. 2015. PMID: 25898270 Free PMC article.
Discovery of a ligand that compensates for decreased endogenous agonist potency of melanocortin-4 receptor polymorphisms identified in obese humans.
Haskell-Luevano C, Xiang Z, Wilczynski AM, Haskell KR, Andreasen AM, Litherland SA, Millard WJ, Pogozheva ID, Mosberg HI, Sorenson NB. Haskell-Luevano C, et al. Among authors: wilczynski am. Adv Exp Med Biol. 2009;611:509-10. doi: 10.1007/978-0-387-73657-0_221. Adv Exp Med Biol. 2009. PMID: 19400288 No abstract available.
Progress in the development of melanocortin receptor selective ligands.
Irani BG, Holder JR, Todorovic A, Wilczynski AM, Joseph CG, Wilson KR, Haskell-Luevano C. Irani BG, et al. Among authors: wilczynski am. Curr Pharm Des. 2004;10(28):3443-79. doi: 10.2174/1381612043382891. Curr Pharm Des. 2004. PMID: 15579046 Review.
Structural characterization and pharmacology of a potent (Cys101-Cys119, Cys110-Cys117) bicyclic agouti-related protein (AGRP) melanocortin receptor antagonist.
Wilczynski A, Wang XS, Bauzo RM, Xiang Z, Shaw AM, Millard WJ, Richards NG, Edison AS, Haskell-Luevano C. Wilczynski A, et al. J Med Chem. 2004 Nov 4;47(23):5662-73. doi: 10.1021/jm049620r. J Med Chem. 2004. PMID: 15509165
Herein, we report a bicyclic hAGRP analogue that, when compared to hAGRP(87-132), possesses equal binding affinity but is 80-fold less potent at the mouse MC4R. ...Those three docked mMC4R-bicyclic hAGRP family structures were compared with putative hAGRP(87-132) ligand-re …
Herein, we report a bicyclic hAGRP analogue that, when compared to hAGRP(87-132), possesses equal binding affinity but is 80-fold les …
Incorporation of a bioactive reverse-turn heterocycle into a peptide template using solid-phase synthesis to probe melanocortin receptor selectivity and ligand conformations by 2D 1H NMR.
Singh A, Wilczynski A, Holder JR, Witek RM, Dirain ML, Xiang Z, Edison AS, Haskell-Luevano C. Singh A, et al. Among authors: wilczynski a. J Med Chem. 2011 Mar 10;54(5):1379-90. doi: 10.1021/jm101425m. Epub 2011 Feb 9. J Med Chem. 2011. PMID: 21306168 Free PMC article.
36 results