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Discovery of a Plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase inhibitor (R,Z)-N-((1-ethylpyrrolidin-2-yl)methyl)-2-(2-fluorobenzylidene)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]thiazine-6-carboxamide (ML276) that reduces parasite growth in vitro.
Preuss J, Maloney P, Peddibhotla S, Hedrick MP, Hershberger P, Gosalia P, Milewski M, Li YL, Sugarman E, Hood B, Suyama E, Nguyen K, Vasile S, Sergienko E, Mangravita-Novo A, Vicchiarelli M, McAnally D, Smith LH, Roth GP, Diwan J, Chung TD, Jortzik E, Rahlfs S, Becker K, Pinkerton AB, Bode L. Preuss J, et al. Among authors: suyama e. J Med Chem. 2012 Aug 23;55(16):7262-72. doi: 10.1021/jm300833h. Epub 2012 Aug 6. J Med Chem. 2012. PMID: 22813531 Free PMC article.
Discovery of ML314, a Brain Penetrant Non-Peptidic β-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor.
Peddibhotla S, Hedrick MP, Hershberger P, Maloney PR, Li Y, Milewski M, Gosalia P, Gray W, Mehta A, Sugarman E, Hood B, Suyama E, Nguyen K, Heynen-Genel S, Vasile S, Salaniwal S, Stonich D, Su Y, Mangravita-Novo A, Vicchiarelli M, Roth GP, Smith LH, Chung TD, Hanson GR, Thomas JB, Caron MG, Barak LS, Pinkerton AB. Peddibhotla S, et al. Among authors: suyama e. ACS Med Chem Lett. 2013 Jul 20;4(9):846-851. doi: 10.1021/ml400176n. ACS Med Chem Lett. 2013. PMID: 24611085 Free PMC article.
Discovery of 4-oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate (ML221) as a functional antagonist of the apelin (APJ) receptor.
Maloney PR, Khan P, Hedrick M, Gosalia P, Milewski M, Li L, Roth GP, Sergienko E, Suyama E, Sugarman E, Nguyen K, Mehta A, Vasile S, Su Y, Stonich D, Nguyen H, Zeng FY, Novo AM, Vicchiarelli M, Diwan J, Chung TD, Smith LH, Pinkerton AB. Maloney PR, et al. Among authors: suyama e. Bioorg Med Chem Lett. 2012 Nov 1;22(21):6656-60. doi: 10.1016/j.bmcl.2012.08.105. Epub 2012 Sep 7. Bioorg Med Chem Lett. 2012. PMID: 23010269 Free PMC article.
Capzimin is a potent and specific inhibitor of proteasome isopeptidase Rpn11.
Li J, Yakushi T, Parlati F, Mackinnon AL, Perez C, Ma Y, Carter KP, Colayco S, Magnuson G, Brown B, Nguyen K, Vasile S, Suyama E, Smith LH, Sergienko E, Pinkerton AB, Chung TDY, Palmer AE, Pass I, Hess S, Cohen SM, Deshaies RJ. Li J, et al. Among authors: suyama e. Nat Chem Biol. 2017 May;13(5):486-493. doi: 10.1038/nchembio.2326. Epub 2017 Feb 28. Nat Chem Biol. 2017. PMID: 28244987 Free PMC article.
Identification of Inhibitors of NOD1-Induced Nuclear Factor-κB Activation.
Khan PM, Correa RG, Divlianska DB, Peddibhotla S, Sessions EH, Magnuson G, Brown B, Suyama E, Yuan H, Mangravita-Novo A, Vicchiarelli M, Su Y, Vasile S, Smith LH, Diaz PW, Reed JC, Roth GP. Khan PM, et al. Among authors: suyama e. ACS Med Chem Lett. 2011 Oct 13;2(10):780-785. doi: 10.1021/ml200158b. Epub 2011 Aug 5. ACS Med Chem Lett. 2011. PMID: 22003428 Free PMC article.
Development and use of a high-throughput screen to identify novel modulators of the corticotropin releasing factor binding protein.
Haass-Koffler CL, Francis TC, Gandhi P, Patel R, Naemuddin M, Nielsen CK, Bartlett SE, Bonci A, Vasile S, Hood BL, Suyama E, Hedrick MP, Smith LH, Limpert AS, Roberto M, Cosford NDP, Sheffler DJ. Haass-Koffler CL, et al. Among authors: suyama e. SLAS Discov. 2022 Dec;27(8):448-459. doi: 10.1016/j.slasd.2022.09.005. Epub 2022 Oct 7. SLAS Discov. 2022. PMID: 36210051 Free PMC article.
Identification of Inhibitors of triacylglyceride accumulation in muscle cells: comparing HTS results from 1536-well plate-based and high-content platforms.
Sugarman E, Koo A, Suyama E, Ruidiaz ME, Heynen-Genel S, Nguyen KH, Vasile S, Soundarapandian MM, Vega RB, Kelly DP, Smith LH, Malany S. Sugarman E, et al. Among authors: suyama e. J Biomol Screen. 2014 Jan;19(1):77-87. doi: 10.1177/1087057113501198. Epub 2013 Aug 29. J Biomol Screen. 2014. PMID: 23989452 Free PMC article.
58 results