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A cellular target engagement assay for the characterization of SHP2 (PTPN11) phosphatase inhibitors.
Romero C, Lambert LJ, Sheffler DJ, De Backer LJS, Raveendra-Panickar D, Celeridad M, Grotegut S, Rodiles S, Holleran J, Sergienko E, Pasquale EB, Cosford NDP, Tautz L. Romero C, et al. Among authors: sergienko e. J Biol Chem. 2020 Feb 28;295(9):2601-2613. doi: 10.1074/jbc.RA119.010838. Epub 2020 Jan 17. J Biol Chem. 2020. PMID: 31953320 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 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.
Design, synthesis and evaluation of benzoisothiazolones as selective inhibitors of PHOSPHO1.
Bravo Y, Teriete P, Dhanya RP, Dahl R, Lee PS, Kiffer-Moreira T, Ganji SR, Sergienko E, Smith LH, Farquharson C, Millán JL, Cosford ND. Bravo Y, et al. Among authors: sergienko e. Bioorg Med Chem Lett. 2014 Sep 1;24(17):4308-11. doi: 10.1016/j.bmcl.2014.07.013. Epub 2014 Jul 15. Bioorg Med Chem Lett. 2014. PMID: 25124115 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.
Inhibition of the Hematopoietic Protein Tyrosine Phosphatase by Phenoxyacetic Acids.
Bobkova EV, Liu WH, Colayco S, Rascon J, Vasile S, Gasior C, Critton DA, Chan X, Dahl R, Su Y, Sergienko E, Chung TD, Mustelin T, Page R, Tautz L. Bobkova EV, et al. Among authors: sergienko e. ACS Med Chem Lett. 2011 Feb;2(2):113-118. doi: 10.1021/ml100103p. ACS Med Chem Lett. 2011. PMID: 21503265 Free PMC article.
129 results