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The melanocortin pathway and energy homeostasis: From discovery to obesity therapy.
Yeo GSH, Chao DHM, Siegert AM, Koerperich ZM, Ericson MD, Simonds SE, Larson CM, Luquet S, Clarke I, Sharma S, Clément K, Cowley MA, Haskell-Luevano C, Van Der Ploeg L, Adan RAH. Yeo GSH, et al. Among authors: koerperich zm. Mol Metab. 2021 Jun;48:101206. doi: 10.1016/j.molmet.2021.101206. Epub 2021 Mar 6. Mol Metab. 2021. PMID: 33684608 Free PMC article. Review.
Functional Mixture-Based Positional Scan Identifies a Library of Antagonist Tetrapeptide Sequences (LAtTeS) with Nanomolar Potency for the Melanocortin-4 Receptor and Equipotent with the Endogenous AGRP(86-132) Antagonist.
Ericson MD, Doering SR, Larson CM, Freeman KT, LaVoi TM, Donow HM, Santos RG, Cho RH, Koerperich ZM, Giulianotti MA, Pinilla C, Houghten RA, Haskell-Luevano C. Ericson MD, et al. Among authors: koerperich zm. J Med Chem. 2021 Oct 14;64(19):14860-14875. doi: 10.1021/acs.jmedchem.1c01417. Epub 2021 Sep 30. J Med Chem. 2021. PMID: 34592820 Free PMC article.
Incorporation of Agouti-Related Protein (AgRP) Human Single Nucleotide Polymorphisms (SNPs) in the AgRP-Derived Macrocyclic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-dPro] Decreases Melanocortin-4 Receptor Antagonist Potency and Results in the Discovery of Melanocortin-5 Receptor Antagonists.
Koerperich ZM, Ericson MD, Freeman KT, Speth RC, Pogozheva ID, Mosberg HI, Haskell-Luevano C. Koerperich ZM, et al. J Med Chem. 2020 Mar 12;63(5):2194-2208. doi: 10.1021/acs.jmedchem.9b00860. Epub 2020 Jan 6. J Med Chem. 2020. PMID: 31845801 Free PMC article.
Incorporation of Three Extracyclic Arginine Residues into a Melanocortin Macrocyclic Agonist (c[Pro-His-DPhe-Arg-Trp-Dap-Lys(Arg-Arg-Arg-Ac)-DPro]) Decreases Food Intake When Administered Intrathecally or Subcutaneously Compared to a Macrocyclic Ligand Lacking Extracyclic Arginine Residues (c[Pro-His-DPhe-Arg-Trp-Dap-Ala-DPro)].
Ericson MD, Freeman KT, Larson CM, Bouchard JL, John K, Lunzer MM, Koerperich ZM, Haskell-Luevano C. Ericson MD, et al. Among authors: koerperich zm. ACS Pharmacol Transl Sci. 2024 Apr 2;7(4):1114-1125. doi: 10.1021/acsptsci.4c00011. eCollection 2024 Apr 12. ACS Pharmacol Transl Sci. 2024. PMID: 38633589
Arg-Phe-Phe d-Amino Acid Stereochemistry Scan in the Macrocyclic Agouti-Related Protein Antagonist Scaffold c[Pro-Arg-Phe-Phe-Xxx-Ala-Phe-DPro] Results in Unanticipated Melanocortin-1 Receptor Agonist Profiles.
Ericson MD, Koerperich ZM, Freeman KT, Fleming KA, Haskell-Luevano C. Ericson MD, et al. Among authors: koerperich zm. ACS Chem Neurosci. 2018 Dec 19;9(12):3015-3023. doi: 10.1021/acschemneuro.8b00218. Epub 2018 Jul 20. ACS Chem Neurosci. 2018. PMID: 29924583 Free PMC article.