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Discovery of Protease-Activated Receptor 4 (PAR4)-Tethered Ligand Antagonists Using Ultralarge Virtual Screening.
Smith ST, Cassada JB, Von Bredow L, Erreger K, Webb EM, Trombley TA, Kalbfleisch JJ, Bender BJ, Zagol-Ikapitte I, Kramlinger VM, Bouchard JL, Mitchell SG, Tretbar M, Shoichet BK, Lindsley CW, Meiler J, Hamm HE. Smith ST, et al. Among authors: bouchard jl. ACS Pharmacol Transl Sci. 2024 Mar 21;7(4):1086-1100. doi: 10.1021/acsptsci.3c00378. eCollection 2024 Apr 12. ACS Pharmacol Transl Sci. 2024. PMID: 38633591
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. Among authors: bouchard jl. 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
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: bouchard jl. 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