Identification of potent, selective, cell-Active inhibitors of the histone lysine methyltransferase EZH2

ACS Medicinal Chemistry Letters

Volumn 3, Issue 12, 2012, Pages 1091-1096

  Verma, Sharad K ^a   Tian, Xinrong ^a   Lafrance, Louis V ^a   Duquenne, Céline ^a   Suarez, Dominic P ^a   Newlander, Kenneth A ^a   Romeril, Stuart P ^a   Burgess, Joelle L ^a   Grant, Seth W ^a   Brackley, James A ^a   Graves, Alan P ^b   Scherzer, Daryl A ^a   Shu, Art ^a   Thompson, Christine ^a   Ott, Heidi M ^a   Van Aller, Glenn S ^a   MacHutta, Carl A ^b   Diaz, Elsie ^b   Jiang, Yong ^b   Johnson, Neil W ^a   Knight, Steven D ^a   Kruger, Ryan G ^a   McCabe, Michael T ^a   Dhanak, Dashyant ^a   Tummino, Peter J ^a   Creasy, Caretha L ^a   Miller, William H ^a   more..

^a Oncology Research and Development   (United States)

^b GLAXOSMITHKLINE   (United States)

Author keywords

Epigenetics; EZH2; H3K27me3; methyltransferase; PRC2; SAM competitive inhibitor

Indexed keywords

GSK 343; GSK 926; HISTONE H3; HISTONE LYSINE METHYLTRANSFERASE INHIBITOR; S ADENOSYLMETHIONINE; TRANSCRIPTION FACTOR EZH2; UNCLASSIFIED DRUG;

ARTICLE; BREAST CANCER; CANCER GROWTH; COMPETITIVE INHIBITION; DRUG IDENTIFICATION; DRUG POTENCY; DRUG SELECTIVITY; ENZYME INHIBITION; GENE EXPRESSION REGULATION; GENE TARGETING; HUMAN; PRIORITY JOURNAL;

EID: 84871248432     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/ml3003346     Document Type: Article

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