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An Alternative Approach to ChIP-Seq Normalization Enables Detection of Genome-Wide Changes in Histone H3 Lysine 27 Trimethylation upon EZH2 Inhibition.
Egan B, Yuan CC, Craske ML, Labhart P, Guler GD, Arnott D, Maile TM, Busby J, Henry C, Kelly TK, Tindell CA, Jhunjhunwala S, Zhao F, Hatton C, Bryant BM, Classon M, Trojer P. Egan B, et al. Among authors: classon m. PLoS One. 2016 Nov 22;11(11):e0166438. doi: 10.1371/journal.pone.0166438. eCollection 2016. PLoS One. 2016. PMID: 27875550 Free PMC article.
An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells.
Vinogradova M, Gehling VS, Gustafson A, Arora S, Tindell CA, Wilson C, Williamson KE, Guler GD, Gangurde P, Manieri W, Busby J, Flynn EM, Lan F, Kim HJ, Odate S, Cochran AG, Liu Y, Wongchenko M, Yang Y, Cheung TK, Maile TM, Lau T, Costa M, Hegde GV, Jackson E, Pitti R, Arnott D, Bailey C, Bellon S, Cummings RT, Albrecht BK, Harmange JC, Kiefer JR, Trojer P, Classon M. Vinogradova M, et al. Among authors: classon m. Nat Chem Biol. 2016 Jul;12(7):531-8. doi: 10.1038/nchembio.2085. Epub 2016 May 23. Nat Chem Biol. 2016. PMID: 27214401
Repression of Stress-Induced LINE-1 Expression Protects Cancer Cell Subpopulations from Lethal Drug Exposure.
Guler GD, Tindell CA, Pitti R, Wilson C, Nichols K, KaiWai Cheung T, Kim HJ, Wongchenko M, Yan Y, Haley B, Cuellar T, Webster J, Alag N, Hegde G, Jackson E, Nance TL, Giresi PG, Chen KB, Liu J, Jhunjhunwala S, Settleman J, Stephan JP, Arnott D, Classon M. Guler GD, et al. Among authors: classon m. Cancer Cell. 2017 Aug 14;32(2):221-237.e13. doi: 10.1016/j.ccell.2017.07.002. Epub 2017 Aug 3. Cancer Cell. 2017. PMID: 28781121 Free article.
From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors.
Liang J, Labadie S, Zhang B, Ortwine DF, Patel S, Vinogradova M, Kiefer JR, Mauer T, Gehling VS, Harmange JC, Cummings R, Lai T, Liao J, Zheng X, Liu Y, Gustafson A, Van der Porten E, Mao W, Liederer BM, Deshmukh G, An L, Ran Y, Classon M, Trojer P, Dragovich PS, Murray L. Liang J, et al. Among authors: classon m. Bioorg Med Chem Lett. 2017 Jul 1;27(13):2974-2981. doi: 10.1016/j.bmcl.2017.05.016. Epub 2017 May 5. Bioorg Med Chem Lett. 2017. PMID: 28512031
Lead optimization of a pyrazolo[1,5-a]pyrimidin-7(4H)-one scaffold to identify potent, selective and orally bioavailable KDM5 inhibitors suitable for in vivo biological studies.
Liang J, Zhang B, Labadie S, Ortwine DF, Vinogradova M, Kiefer JR, Gehling VS, Harmange JC, Cummings R, Lai T, Liao J, Zheng X, Liu Y, Gustafson A, Van der Porten E, Mao W, Liederer BM, Deshmukh G, Classon M, Trojer P, Dragovich PS, Murray L. Liang J, et al. Among authors: classon m. Bioorg Med Chem Lett. 2016 Aug 15;26(16):4036-41. doi: 10.1016/j.bmcl.2016.06.078. Epub 2016 Jun 29. Bioorg Med Chem Lett. 2016. PMID: 27406798
Silencing of retrotransposons by SETDB1 inhibits the interferon response in acute myeloid leukemia.
Cuellar TL, Herzner AM, Zhang X, Goyal Y, Watanabe C, Friedman BA, Janakiraman V, Durinck S, Stinson J, Arnott D, Cheung TK, Chaudhuri S, Modrusan Z, Doerr JM, Classon M, Haley B. Cuellar TL, et al. Among authors: classon m. J Cell Biol. 2017 Nov 6;216(11):3535-3549. doi: 10.1083/jcb.201612160. Epub 2017 Sep 8. J Cell Biol. 2017. PMID: 28887438 Free PMC article.
48 results