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2021 2
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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. 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
Discovery of a Pan-Melanocortin Receptor Antagonist [Ac-DPhe(pI)-Arg-Nal(2')-Orn-NH2] at the MC1R, MC3R, MC4R, and MC5R that Mediates an Increased Feeding Response in Mice and a 40-Fold Selective MC1R Antagonist [Ac-DPhe(pI)-DArg-Nal(2')-Arg-NH2].
Ericson MD, Tran LT, Mathre SS, Freeman KT, Holdaway K, John K, Lunzer MM, Bouchard JL, Haskell-Luevano C. Ericson MD, et al. J Med Chem. 2023 Jun 22;66(12):8103-8117. doi: 10.1021/acs.jmedchem.3c00432. Epub 2023 Jun 12. J Med Chem. 2023. PMID: 37307241
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. 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.
Discovery of Nanomolar Melanocortin-3 Receptor (MC3R)-Selective Small Molecule Pyrrolidine Bis-Cyclic Guanidine Agonist Compounds Via a High-Throughput "Unbiased" Screening Campaign.
Doering SR, Freeman K, Debevec G, Geer P, Santos RG, Lavoi TM, Giulianotti MA, Pinilla C, Appel JR, Houghten RA, Ericson MD, Haskell-Luevano C. Doering SR, et al. J Med Chem. 2021 May 13;64(9):5577-5592. doi: 10.1021/acs.jmedchem.0c02041. Epub 2021 Apr 22. J Med Chem. 2021. PMID: 33886285 Free PMC article.