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High-throughput screening for small-molecule inhibitors of plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase.
Preuss J, Hedrick M, Sergienko E, Pinkerton A, Mangravita-Novo A, Smith L, Marx C, Fischer E, Jortzik E, Rahlfs S, Becker K, Bode L. Preuss J, et al. Among authors: sergienko e. J Biomol Screen. 2012 Jul;17(6):738-51. doi: 10.1177/1087057112442382. Epub 2012 Apr 11. J Biomol Screen. 2012. PMID: 22496096 Free PMC article.
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: sergienko 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.
Potent, selective, and orally available benzoisothiazolone phosphomannose isomerase inhibitors as probes for congenital disorder of glycosylation Ia.
Dahl R, Bravo Y, Sharma V, Ichikawa M, Dhanya RP, Hedrick M, Brown B, Rascon J, Vicchiarelli M, Mangravita-Novo A, Yang L, Stonich D, Su Y, Smith LH, Sergienko E, Freeze HH, Cosford ND. Dahl R, et al. Among authors: sergienko e. J Med Chem. 2011 May 26;54(10):3661-8. doi: 10.1021/jm101401a. Epub 2011 May 3. J Med Chem. 2011. PMID: 21539312 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: sergienko 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.
133 results