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Page 1
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.
Inhibition of hematopoietic protein tyrosine phosphatase augments and prolongs ERK1/2 and p38 activation.
Sergienko E, Xu J, Liu WH, Dahl R, Critton DA, Su Y, Brown BT, Chan X, Yang L, Bobkova EV, Vasile S, Yuan H, Rascon J, Colayco S, Sidique S, Cosford ND, Chung TD, Mustelin T, Page R, Lombroso PJ, Tautz L. Sergienko E, et al. ACS Chem Biol. 2012 Feb 17;7(2):367-77. doi: 10.1021/cb2004274. Epub 2011 Nov 17. ACS Chem Biol. 2012. PMID: 22070201 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: sergienko 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.
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.
Allosteric Inhibition of Ubiquitin-like Modifications by a Class of Inhibitor of SUMO-Activating Enzyme.
Li YJ, Du L, Wang J, Vega R, Lee TD, Miao Y, Aldana-Masangkay G, Samuels ER, Li B, Ouyang SX, Colayco SA, Bobkova EV, Divlianska DB, Sergienko E, Chung TDY, Fakih M, Chen Y. Li YJ, et al. Among authors: sergienko e. Cell Chem Biol. 2019 Feb 21;26(2):278-288.e6. doi: 10.1016/j.chembiol.2018.10.026. Epub 2018 Dec 20. Cell Chem Biol. 2019. PMID: 30581133 Free PMC article.
Discovery of 5-((5-chloro-2-methoxyphenyl)sulfonamido)nicotinamide (SBI-425), a potent and orally bioavailable tissue-nonspecific alkaline phosphatase (TNAP) inhibitor.
Pinkerton AB, Sergienko E, Bravo Y, Dahl R, Ma CT, Sun Q, Jackson MR, Cosford NDP, Millán JL. Pinkerton AB, et al. Among authors: sergienko e. Bioorg Med Chem Lett. 2018 Jan 1;28(1):31-34. doi: 10.1016/j.bmcl.2017.11.024. Epub 2017 Nov 11. Bioorg Med Chem Lett. 2018. PMID: 29174347 Free PMC article.
Identification of a selective inhibitor of murine intestinal alkaline phosphatase (ML260) by concurrent ultra-high throughput screening against human and mouse isozymes.
Ardecky RJ, Bobkova EV, Kiffer-Moreira T, Brown B, Ganji S, Zou J, Pass I, Narisawa S, Iano FG, Rosenstein C, Cheltsov A, Rascon J, Hedrick M, Gasior C, Forster A, Shi S, Dahl R, Vasile S, Su Y, Sergienko E, Chung TDY, Kaunitz J, Hoylaerts MF, Pinkerton AB, Millán JL. Ardecky RJ, et al. Among authors: sergienko e. Bioorg Med Chem Lett. 2014 Feb 1;24(3):1000-1004. doi: 10.1016/j.bmcl.2013.12.043. Epub 2013 Dec 19. Bioorg Med Chem Lett. 2014. PMID: 24412070 Free PMC article.
Optimization of a urea-containing series of nicotinamide phosphoribosyltransferase (NAMPT) activators.
Pinkerton AB, Sessions EH, Hershberger P, Maloney PR, Peddibhotla S, Hopf M, Sergienko E, Ma CT, Smith LH, Jackson MR, Tanaka J, Tsuji T, Akiu M, Cohen SE, Nakamura T, Gardell SJ. Pinkerton AB, et al. Among authors: sergienko e. Bioorg Med Chem Lett. 2021 Jun 1;41:128007. doi: 10.1016/j.bmcl.2021.128007. Epub 2021 Mar 31. Bioorg Med Chem Lett. 2021. PMID: 33798699
133 results