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2009 1
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Page 1
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.
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. 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.
SAR Studies of Exosite-Binding Substrate-Selective Inhibitors of A Disintegrin And Metalloprotease 17 (ADAM17) and Application as Selective in Vitro Probes.
Knapinska AM, Dreymuller D, Ludwig A, Smith L, Golubkov V, Sohail A, Fridman R, Giulianotti M, LaVoi TM, Houghten RA, Fields GB, Minond D. Knapinska AM, et al. J Med Chem. 2015 Aug 13;58(15):5808-24. doi: 10.1021/acs.jmedchem.5b00354. Epub 2015 Aug 4. J Med Chem. 2015. PMID: 26192023 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. 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.
27 results