Conformational Adaptation Drives Potent, Selective and Durable Inhibition of the Human Protein Methyltransferase DOT1L

Chemical Biology and Drug Design

Volumn 80, Issue 6, 2012, Pages 971-980

  Basavapathruni, Aravind ^a   Jin, Lei ^a   Daigle, Scott R ^a   Majer, Christina R A ^a   Therkelsen, Carly A ^a   Wigle, Tim J ^a   Kuntz, Kevin W ^a   Chesworth, Richard ^a   Pollock, Roy M ^a   Scott, Margaret P ^a   Moyer, Mikel P ^a   Richon, Victoria M ^a   Copeland, Robert A ^a   Olhava, Edward J ^a  

^a EPIZYME INC   (United States)

Author keywords

Conformational adaptation; DOT1L; Enzyme inhibition; Protein methyltransferase

Indexed keywords

AMINONUCLEOSIDE; ENZYME INHIBITOR; HISTONE H3; PROTEIN METHYLTRANSFERASE; PROTEIN METHYLTRANSFERASE DOT1L; S ADENOSYLHOMOCYSTEINE; UNCLASSIFIED DRUG;

ARTICLE; CATALYSIS; CELL KILLING; CHEMICAL STRUCTURE; CRYSTAL STRUCTURE; CRYSTALLOGRAPHY; ENZYME INHIBITOR COMPLEX; ENZYME METABOLISM; HUMAN; HUMAN CELL; IC 50; KINETICS; LEUKEMIA CELL; METHYLATION; PRIORITY JOURNAL; STRUCTURE ACTIVITY RELATION; THERMODYNAMICS;

BINDING SITES; CELL LINE, TUMOR; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; ENZYME INHIBITORS; HISTONES; HUMANS; KINETICS; METHYLATION; METHYLTRANSFERASES; MOLECULAR DOCKING SIMULATION; NUCLEOSIDES; PROTEIN BINDING; PROTEIN STRUCTURE, TERTIARY; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84868101932     PISSN: 17470277     EISSN: 17470285     Source Type: Journal    
DOI: 10.1111/cbdd.12050     Document Type: Article

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