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Microwave-assisted solid-phase synthesis of side-chain to side-chain lactam-bridge cyclic peptides.

Tala SR, Schnell SM, Haskell-Luevano C. Tala SR, et al. Bioorg Med Chem Lett. 2015 Dec 15;25(24):5708-11. doi: 10.1016/j.bmcl.2015.10.095. Epub 2015 Oct 31. Bioorg Med Chem Lett. 2015. PMID: 26555357 Free PMC article.

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1,4-disubstituted-[1,2,3]triazolyl-containing analogues of MT-II: design, synthesis, conformational analysis, and biological activity.

Testa C, Scrima M, Grimaldi M, D'Ursi AM, Dirain ML, Lubin-Germain N, Singh A, Haskell-Luevano C, Chorev M, Rovero P, Papini AM. Testa C, et al. J Med Chem. 2014 Nov 26;57(22):9424-34. doi: 10.1021/jm501027w. Epub 2014 Nov 13. J Med Chem. 2014. PMID: 25347033 Free PMC article.

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A fragment of the Escherichia coli ClpB heat-shock protein is a micromolar melanocortin 1 receptor agonist.

Ericson MD, Schnell SM, Freeman KT, Haskell-Luevano C. Ericson MD, et al. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5306-8. doi: 10.1016/j.bmcl.2015.09.046. Epub 2015 Sep 21. Bioorg Med Chem Lett. 2015. PMID: 26433448 Free PMC article.

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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. 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.

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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.

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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.

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Synthesis and Structure-Activity Relationships of Substituted Urea Derivatives on Mouse Melanocortin Receptors.

Singh A, Kast J, Dirain ML, Huang H, Haskell-Luevano C. Singh A, et al. ACS Chem Neurosci. 2016 Feb 17;7(2):196-205. doi: 10.1021/acschemneuro.5b00273. Epub 2015 Dec 24. ACS Chem Neurosci. 2016. PMID: 26645732 Free PMC article.

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An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers.

Lensing CJ, Freeman KT, Schnell SM, Adank DN, Speth RC, Haskell-Luevano C. Lensing CJ, et al. J Med Chem. 2016 Apr 14;59(7):3112-28. doi: 10.1021/acs.jmedchem.5b01894. Epub 2016 Mar 29. J Med Chem. 2016. PMID: 26959173 Free PMC article.

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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.

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