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Page 1
Discovery of Small Molecule Kappa Opioid Receptor Agonist and Antagonist Chemotypes through a HTS and Hit Refinement Strategy.
Frankowski KJ, Hedrick MP, Gosalia P, Li K, Shi S, Whipple D, Ghosh P, Prisinzano TE, Schoenen FJ, Su Y, Vasile S, Sergienko E, Gray W, Hariharan S, Milan L, Heynen-Genel S, Mangravita-Novo A, Vicchiarelli M, Smith LH, Streicher JM, Caron MG, Barak LS, Bohn LM, Chung TD, Aubé J. Frankowski KJ, et al. Among authors: sergienko e. ACS Chem Neurosci. 2012 Mar 21;3(3):221-236. doi: 10.1021/cn200128x. Epub 2012 Jan 20. ACS Chem Neurosci. 2012. PMID: 22737280 Free PMC article.
Design of high-throughput screening assays and identification of a SUMO1-specific small molecule chemotype targeting the SUMO-interacting motif-binding surface.
Alontaga AY, Li Y, Chen CH, Ma CT, Malany S, Key DE, Sergienko E, Sun Q, Whipple DA, Matharu DS, Li B, Vega R, Li YJ, Schoenen FJ, Blagg BS, Chung TD, Chen Y. Alontaga AY, et al. Among authors: sergienko e. ACS Comb Sci. 2015 Apr 13;17(4):239-46. doi: 10.1021/co500181b. Epub 2015 Mar 23. ACS Comb Sci. 2015. PMID: 25719760 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.
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.
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.
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.
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.
133 results