Structure-guided DOT1L probe optimization by label-free ligand displacement

ACS Chemical Biology

Volumn 10, Issue 3, 2015, Pages 667-674

  Yi, Joanna S ^a,b   Federation, Alexander J ^a   Qi, Jun ^a   Dhe Paganon, Sirano ^a   Hadler, Michael ^c   Xu, Xiang ^b   St Pierre, Roodolph ^a   Varca, Anthony C ^a   Wu, Lei ^d   Marineau, Jason J ^a   Smith, William B ^a   Souza, Amanda ^a   Chory, Emma J ^a   Armstrong, Scott A ^c   Bradner, James E ^a,b  

^a DANA FARBER CANCER INSTITUTE   (United States)

^b HARVARD MEDICAL SCHOOL   (United States)

^c MEMORIAL SLOAN KETTERING CANCER CENTER   (United States)

^d Shanghai ChemPartner Co Ltd   (China)

Author keywords

[No Author keywords available]

Indexed keywords

ANTILEUKEMIC AGENT; DOT1L INHIBITOR; S ADENOSYLMETHIONINE; UNCLASSIFIED DRUG; ADENOSINE; ANTINEOPLASTIC AGENT; CARBANILAMIDE DERIVATIVE; DOT1L PROTEIN, HUMAN; ENZYME INHIBITOR; EPZ004777; HISTONE; HYBRID PROTEIN; LIGAND; METHYLTRANSFERASE; MOLECULAR LIBRARY;

ACUTE LEUKEMIA; ANISOTROPY; ARTICLE; CELL PROLIFERATION; CHEMOLUMINESCENCE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DOSE RESPONSE; HIGH THROUGHPUT SCREENING; IC50; ISOTHERMAL TITRATION CALORIMETRY; LIGAND BINDING; MOLECULAR RECOGNITION; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN PURIFICATION; ANALOGS AND DERIVATIVES; ANTAGONISTS AND INHIBITORS; CHEMICAL STRUCTURE; CHEMISTRY; DRUG EFFECTS; ENZYMOLOGY; EPITHELIUM CELL; GENE EXPRESSION REGULATION; GENETICS; HUMAN; METABOLISM; METHYLATION; MOLECULAR LIBRARY; PATHOLOGY; PHARMACOLOGY; STRUCTURE ACTIVITY RELATION; SYNTHESIS; TUMOR CELL LINE;

ADENOSINE; ANTINEOPLASTIC AGENTS; CELL LINE, TUMOR; ENZYME INHIBITORS; EPITHELIAL CELLS; GENE EXPRESSION REGULATION, NEOPLASTIC; HIGH-THROUGHPUT SCREENING ASSAYS; HISTONES; HUMANS; LIGANDS; METHYLATION; METHYLTRANSFERASES; MODELS, MOLECULAR; PHENYLUREA COMPOUNDS; RECOMBINANT FUSION PROTEINS; S-ADENOSYLMETHIONINE; SMALL MOLECULE LIBRARIES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84925620054     PISSN: 15548929     EISSN: 15548937     Source Type: Journal    
DOI: 10.1021/cb500796d     Document Type: Article

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