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3,202 results

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Page 1
Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia.
Pappalardi MB, Keenan K, Cockerill M, Kellner WA, Stowell A, Sherk C, Wong K, Pathuri S, Briand J, Steidel M, Chapman P, Groy A, Wiseman AK, McHugh CF, Campobasso N, Graves AP, Fairweather E, Werner T, Raoof A, Butlin RJ, Rueda L, Horton JR, Fosbenner DT, Zhang C, Handler JL, Muliaditan M, Mebrahtu M, Jaworski JP, McNulty DE, Burt C, Eberl HC, Taylor AN, Ho T, Merrihew S, Foley SW, Rutkowska A, Li M, Romeril SP, Goldberg K, Zhang X, Kershaw CS, Bantscheff M, Jurewicz AJ, Minthorn E, Grandi P, Patel M, Benowitz AB, Mohammad HP, Gilmartin AG, Prinjha RK, Ogilvie D, Carpenter C, Heerding D, Baylin SB, Jones PA, Cheng X, King BW, Luengo JI, Jordan AM, Waddell I, Kruger RG, McCabe MT. Pappalardi MB, et al. Among authors: ho t. Nat Cancer. 2021 Oct;2(10):1002-1017. Epub 2021 Sep 27. Nat Cancer. 2021. PMID: 34790902 Free PMC article.
A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC.
Mohammad HP, Smitheman KN, Kamat CD, Soong D, Federowicz KE, Van Aller GS, Schneck JL, Carson JD, Liu Y, Butticello M, Bonnette WG, Gorman SA, Degenhardt Y, Bai Y, McCabe MT, Pappalardi MB, Kasparec J, Tian X, McNulty KC, Rouse M, McDevitt P, Ho T, Crouthamel M, Hart TK, Concha NO, McHugh CF, Miller WH, Dhanak D, Tummino PJ, Carpenter CL, Johnson NW, Hann CL, Kruger RG. Mohammad HP, et al. Among authors: ho t. Cancer Cell. 2015 Jul 13;28(1):57-69. doi: 10.1016/j.ccell.2015.06.002. Cancer Cell. 2015. PMID: 26175415 Free article.
A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models.
Chan-Penebre E, Kuplast KG, Majer CR, Boriack-Sjodin PA, Wigle TJ, Johnston LD, Rioux N, Munchhof MJ, Jin L, Jacques SL, West KA, Lingaraj T, Stickland K, Ribich SA, Raimondi A, Scott MP, Waters NJ, Pollock RM, Smith JJ, Barbash O, Pappalardi M, Ho TF, Nurse K, Oza KP, Gallagher KT, Kruger R, Moyer MP, Copeland RA, Chesworth R, Duncan KW. Chan-Penebre E, et al. Among authors: ho tf. Nat Chem Biol. 2015 Jun;11(6):432-7. doi: 10.1038/nchembio.1810. Epub 2015 Apr 27. Nat Chem Biol. 2015. PMID: 25915199
A High-Throughput Dose-Response Cellular Thermal Shift Assay for Rapid Screening of Drug Target Engagement in Living Cells, Exemplified Using SMYD3 and IDO1.
McNulty DE, Bonnette WG, Qi H, Wang L, Ho TF, Waszkiewicz A, Kallal LA, Nagarajan RP, Stern M, Quinn AM, Creasy CL, Su DS, Graves AP, Annan RS, Sweitzer SM, Holbert MA. McNulty DE, et al. SLAS Discov. 2018 Jan;23(1):34-46. doi: 10.1177/2472555217732014. Epub 2017 Sep 28. SLAS Discov. 2018. PMID: 28957646 Free article.
A high-throughput screen measuring ubiquitination of p53 by human mdm2.
Murray MF, Jurewicz AJ, Martin JD, Ho TF, Zhang H, Johanson KO, Kirkpatrick RB, Ma J, Lor LA, Thrall SH, Schwartz B. Murray MF, et al. J Biomol Screen. 2007 Dec;12(8):1050-8. doi: 10.1177/1087057107308556. Epub 2007 Nov 7. J Biomol Screen. 2007. PMID: 17989425
Structure-guided optimization of small molecule c-Abl activators.
Hong X, Cao P, Washio Y, Simpson G, Campobasso N, Yang J, Borthwick J, Burton G, Chabanet J, Bertrand S, Evans H, Young RJ, Qu J, Li H, Cottom J, Ward P, Zhang H, Ho T, Qin D, Christensen S, Head MS. Hong X, et al. Among authors: ho t. J Comput Aided Mol Des. 2014 Feb;28(2):75-87. doi: 10.1007/s10822-014-9731-5. Epub 2014 Feb 27. J Comput Aided Mol Des. 2014. PMID: 24573412 Free PMC article.
Discovery and characterization of a cell-permeable, small-molecule c-Abl kinase activator that binds to the myristoyl binding site.
Yang J, Campobasso N, Biju MP, Fisher K, Pan XQ, Cottom J, Galbraith S, Ho T, Zhang H, Hong X, Ward P, Hofmann G, Siegfried B, Zappacosta F, Washio Y, Cao P, Qu J, Bertrand S, Wang DY, Head MS, Li H, Moores S, Lai Z, Johanson K, Burton G, Erickson-Miller C, Simpson G, Tummino P, Copeland RA, Oliff A. Yang J, et al. Among authors: ho t. Chem Biol. 2011 Feb 25;18(2):177-86. doi: 10.1016/j.chembiol.2010.12.013. Chem Biol. 2011. PMID: 21338916
Baculovirus production of fully-active phosphoinositide 3-kinase alpha as a p85alpha-p110alpha fusion for X-ray crystallographic analysis with ATP competitive enzyme inhibitors.
Sinnamon RH, McDevitt P, Pietrak BL, Leydon VR, Xue Y, Lehr R, Qi H, Burns M, Elkins P, Ward P, Vincentini G, Fisher D, Grimes M, Brandt M, Auger KR, Ho T, Johanson K, Jones CS, Schwartz B, Sweitzer TD, Kirkpatrick RB. Sinnamon RH, et al. Among authors: ho t. Protein Expr Purif. 2010 Oct;73(2):167-76. doi: 10.1016/j.pep.2010.05.002. Epub 2010 May 10. Protein Expr Purif. 2010. PMID: 20457255
3,202 results