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Page 1
Long residence time inhibition of EZH2 in activated polycomb repressive complex 2.
Van Aller GS, Pappalardi MB, Ott HM, Diaz E, Brandt M, Schwartz BJ, Miller WH, Dhanak D, McCabe MT, Verma SK, Creasy CL, Tummino PJ, Kruger RG. Van Aller GS, et al. Among authors: tummino pj. ACS Chem Biol. 2014 Mar 21;9(3):622-9. doi: 10.1021/cb4008748. Epub 2013 Dec 31. ACS Chem Biol. 2014. PMID: 24304166
Mutation of A677 in histone methyltransferase EZH2 in human B-cell lymphoma promotes hypertrimethylation of histone H3 on lysine 27 (H3K27).
McCabe MT, Graves AP, Ganji G, Diaz E, Halsey WS, Jiang Y, Smitheman KN, Ott HM, Pappalardi MB, Allen KE, Chen SB, Della Pietra A 3rd, Dul E, Hughes AM, Gilbert SA, Thrall SH, Tummino PJ, Kruger RG, Brandt M, Schwartz B, Creasy CL. McCabe MT, et al. Among authors: tummino pj. Proc Natl Acad Sci U S A. 2012 Feb 21;109(8):2989-94. doi: 10.1073/pnas.1116418109. Epub 2012 Feb 8. Proc Natl Acad Sci U S A. 2012. PMID: 22323599 Free PMC article.
Development and validation of reagents and assays for EZH2 peptide and nucleosome high-throughput screens.
Diaz E, Machutta CA, Chen S, Jiang Y, Nixon C, Hofmann G, Key D, Sweitzer S, Patel M, Wu Z, Creasy CL, Kruger RG, LaFrance L, Verma SK, Pappalardi MB, Le B, Van Aller GS, McCabe MT, Tummino PJ, Pope AJ, Thrall SH, Schwartz B, Brandt M. Diaz E, et al. Among authors: tummino pj. J Biomol Screen. 2012 Dec;17(10):1279-92. doi: 10.1177/1087057112453765. Epub 2012 Aug 17. J Biomol Screen. 2012. PMID: 22904200
EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations.
McCabe MT, Ott HM, Ganji G, Korenchuk S, Thompson C, Van Aller GS, Liu Y, Graves AP, Della Pietra A 3rd, Diaz E, LaFrance LV, Mellinger M, Duquenne C, Tian X, Kruger RG, McHugh CF, Brandt M, Miller WH, Dhanak D, Verma SK, Tummino PJ, Creasy CL. McCabe MT, et al. Among authors: tummino pj. Nature. 2012 Dec 6;492(7427):108-12. doi: 10.1038/nature11606. Epub 2012 Oct 10. Nature. 2012. PMID: 23051747
Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2.
Verma SK, Tian X, LaFrance LV, Duquenne C, Suarez DP, Newlander KA, Romeril SP, Burgess JL, Grant SW, Brackley JA, Graves AP, Scherzer DA, Shu A, Thompson C, Ott HM, Aller GS, Machutta CA, Diaz E, Jiang Y, Johnson NW, Knight SD, Kruger RG, McCabe MT, Dhanak D, Tummino PJ, Creasy CL, Miller WH. Verma SK, et al. Among authors: tummino pj. ACS Med Chem Lett. 2012 Oct 19;3(12):1091-6. doi: 10.1021/ml3003346. eCollection 2012 Dec 13. ACS Med Chem Lett. 2012. PMID: 24900432 Free PMC article.
A687V EZH2 is a driver of histone H3 lysine 27 (H3K27) hypertrimethylation.
Ott HM, Graves AP, Pappalardi MB, Huddleston M, Halsey WS, Hughes AM, Groy A, Dul E, Jiang Y, Bai Y, Annan R, Verma SK, Knight SD, Kruger RG, Dhanak D, Schwartz B, Tummino PJ, Creasy CL, McCabe MT. Ott HM, et al. Among authors: tummino pj. Mol Cancer Ther. 2014 Dec;13(12):3062-73. doi: 10.1158/1535-7163.MCT-13-0876. Epub 2014 Sep 24. Mol Cancer Ther. 2014. PMID: 25253781
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: tummino pj. Cancer Cell. 2015 Jul 13;28(1):57-69. doi: 10.1016/j.ccell.2015.06.002. Cancer Cell. 2015. PMID: 26175415 Free article.
Smyd3 regulates cancer cell phenotypes and catalyzes histone H4 lysine 5 methylation.
Van Aller GS, Reynoird N, Barbash O, Huddleston M, Liu S, Zmoos AF, McDevitt P, Sinnamon R, Le B, Mas G, Annan R, Sage J, Garcia BA, Tummino PJ, Gozani O, Kruger RG. Van Aller GS, et al. Among authors: tummino pj. Epigenetics. 2012 Apr;7(4):340-3. doi: 10.4161/epi.19506. Epub 2012 Apr 1. Epigenetics. 2012. PMID: 22419068 Free PMC article.
SMYD3 links lysine methylation of MAP3K2 to Ras-driven cancer.
Mazur PK, Reynoird N, Khatri P, Jansen PW, Wilkinson AW, Liu S, Barbash O, Van Aller GS, Huddleston M, Dhanak D, Tummino PJ, Kruger RG, Garcia BA, Butte AJ, Vermeulen M, Sage J, Gozani O. Mazur PK, et al. Among authors: tummino pj. Nature. 2014 Jun 12;510(7504):283-7. doi: 10.1038/nature13320. Epub 2014 May 21. Nature. 2014. PMID: 24847881 Free PMC article.
Small-Molecule Targets in Immuno-Oncology.
Dhanak D, Edwards JP, Nguyen A, Tummino PJ. Dhanak D, et al. Among authors: tummino pj. Cell Chem Biol. 2017 Sep 21;24(9):1148-1160. doi: 10.1016/j.chembiol.2017.08.019. Cell Chem Biol. 2017. PMID: 28938090 Free article. Review.
69 results