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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: giulianotti ma. 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.
Identification of a small molecule inhibitor of the aminoglycoside 6'-N-acetyltransferase type Ib [AAC(6')-Ib] using mixture-based combinatorial libraries.
Tran T, Chiem K, Jani S, Arivett BA, Lin DL, Lad R, Jimenez V, Farone MB, Debevec G, Santos R, Giulianotti M, Pinilla C, Tolmasky ME. Tran T, et al. Among authors: giulianotti m. Int J Antimicrob Agents. 2018 May;51(5):752-761. doi: 10.1016/j.ijantimicag.2018.01.019. Epub 2018 Feb 2. Int J Antimicrob Agents. 2018. PMID: 29410367 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. Among authors: giulianotti ma. 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.
Inhibition of Aminoglycoside 6'-N-acetyltransferase Type Ib (AAC(6')-Ib): Structure-Activity Relationship of Substituted Pyrrolidine Pentamine Derivatives as Inhibitors.
Rocha K, Magallon J, Reeves C, Phan K, Vu P, Oakley-Havens CL, Kwan S, Ramirez MS, LaVoi T, Donow H, Chapagain P, Santos R, Pinilla C, Giulianotti MA, Tolmasky ME. Rocha K, et al. Among authors: giulianotti ma. Biomedicines. 2021 Sep 14;9(9):1218. doi: 10.3390/biomedicines9091218. Biomedicines. 2021. PMID: 34572404 Free PMC article.
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: giulianotti ma. 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.
The Parallel Structure-Activity Relationship Screening of Three Compounds Identifies the Common Agonist Pharmacophore of Pyrrolidine Bis-Cyclic Guanidine Melanocortin-3 Receptor (MC3R) Small-Molecule Ligands.
Ericson MD, Freeman KT, LaVoi TM, Donow HM, Santos RG, Giulianotti MA, Pinilla C, Houghten RA, Haskell-Luevano C. Ericson MD, et al. Among authors: giulianotti ma. Int J Mol Sci. 2023 Jun 14;24(12):10145. doi: 10.3390/ijms241210145. Int J Mol Sci. 2023. PMID: 37373293 Free PMC article.
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. Among authors: giulianotti ma. 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.
83 results