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A Direct in Vivo Comparison of the Melanocortin Monovalent Agonist Ac-His-DPhe-Arg-Trp-NH2 versus the Bivalent Agonist Ac-His-DPhe-Arg-Trp-PEDG20-His-DPhe-Arg-Trp-NH2: A Bivalent Advantage.
Lensing CJ, Adank DN, Wilber SL, Freeman KT, Schnell SM, Speth RC, Zarth AT, Haskell-Luevano C. Lensing CJ, et al. Among authors: freeman kt. ACS Chem Neurosci. 2017 Jun 21;8(6):1262-1278. doi: 10.1021/acschemneuro.6b00399. Epub 2017 Feb 16. ACS Chem Neurosci. 2017. PMID: 28128928 Free PMC article.
Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-Xaa1-Arg-(pI)DPhe-Xaa4-NH2.
Doering SR, Freeman KT, Schnell SM, Haslach EM, Dirain M, Debevec G, Geer P, Santos RG, Giulianotti MA, Pinilla C, Appel JR, Speth RC, Houghten RA, Haskell-Luevano C. Doering SR, et al. Among authors: freeman kt. J Med Chem. 2017 May 25;60(10):4342-4357. doi: 10.1021/acs.jmedchem.7b00301. Epub 2017 May 15. J Med Chem. 2017. PMID: 28453292 Free PMC article.
Structure-Activity Relationship Studies on a Macrocyclic Agouti-Related Protein (AGRP) Scaffold Reveal Agouti Signaling Protein (ASP) Residue Substitutions Maintain Melanocortin-4 Receptor Antagonist Potency and Result in Inverse Agonist Pharmacology at the Melanocortin-5 Receptor.
Ericson MD, Freeman KT, Schnell SM, Fleming KA, Haskell-Luevano C. Ericson MD, et al. Among authors: freeman kt. J Med Chem. 2017 Oct 12;60(19):8103-8114. doi: 10.1021/acs.jmedchem.7b00856. Epub 2017 Oct 4. J Med Chem. 2017. PMID: 28813605 Free PMC article.
Structure-Activity Relationship Studies of a Macrocyclic AGRP-Mimetic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-DPro] Yield Potent and Selective Melanocortin-4 Receptor Antagonists and Melanocortin-5 Receptor Inverse Agonists That Increase Food Intake in Mice.
Fleming KA, Ericson MD, Freeman KT, Adank DN, Lunzer MM, Wilber SL, Haskell-Luevano C. Fleming KA, et al. Among authors: freeman kt. ACS Chem Neurosci. 2018 May 16;9(5):1141-1151. doi: 10.1021/acschemneuro.7b00495. Epub 2018 Feb 13. ACS Chem Neurosci. 2018. PMID: 29363944 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: freeman kt. 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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