Structure-Based Optimization of a Small Molecule Antagonist of the Interaction between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1)

Journal of Medicinal Chemistry

Volumn 59, Issue 6, 2016, Pages 2478-2496

  Getlik, Matthäus ^a   Smil, David ^b   Zepeda Velázquez, Carlos ^a   Bolshan, Yuri ^b   Poda, Gennady ^a,b   Wu, Hong ^b   Dong, Aiping ^b   Kuznetsova, Ekaterina ^b   Marcellus, Richard ^a   Senisterra, Guillermo ^b   Dombrovski, Ludmila ^b   Hajian, Taraneh ^b   Kiyota, Taira ^a   Schapira, Matthieu ^b   Arrowsmith, Cheryl H ^b   Brown, Peter J ^b   Vedadi, Masoud ^b   Al Awar, Rima ^a,b  

^a ONTARIO INSTITUTE FOR CANCER RESEARCH   (Canada)

^b UNIVERSITY OF TORONTO   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

BENZAMIDE DERIVATIVE; MIXED LINEAGE LEUKEMIA 1 PROTEIN; MIXED LINEAGE LEUKEMIA PROTEIN; MULTIPROTEIN COMPLEX; N [4 (4 METHYLPIPERAZIN 1 YL) 3' (MORPHOLINOMETHYL) [1,1 BIPHENYL] 3 YL] 6 OXO 4 (TRIFLUOROMETHYL) 1,6 DIHYDROPYRIDINE 3 CARBOXAMIDE; UNCLASSIFIED DRUG; WD REPEAT CONTAINING PROTEIN 5; ANTINEOPLASTIC AGENT; BIPHENYL DERIVATIVE; DIHYDROPYRIDINE DERIVATIVE; HISTONE LYSINE METHYLTRANSFERASE; MLL PROTEIN, HUMAN; MOLECULAR LIBRARY; OICR-9429; WDR5 PROTEIN, HUMAN;

ACUTE MYELOBLASTIC LEUKEMIA; ANIMAL EXPERIMENT; ARTICLE; BINDING AFFINITY; COMPUTER MODEL; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG ACTIVITY; DRUG ANTAGONISM; DRUG BINDING; DRUG BIOAVAILABILITY; DRUG PENETRATION; DRUG SYNTHESIS; HUMAN; HUMAN CELL; MOUSE; NONHUMAN; PROTEIN PROTEIN INTERACTION; STRUCTURE ACTIVITY RELATION; ANIMAL; ANTAGONISTS AND INHIBITORS; CHEMICAL STRUCTURE; DRUG DESIGN; DRUG EFFECTS; FEMALE; LEUKEMIA; MOLECULAR DOCKING; MOLECULAR LIBRARY; SCID MOUSE; SYNTHESIS; TUMOR CELL LINE; X RAY DIFFRACTION;

ANIMALS; ANTINEOPLASTIC AGENTS; BIPHENYL COMPOUNDS; CELL LINE, TUMOR; DIHYDROPYRIDINES; DRUG DESIGN; FEMALE; HISTONE-LYSINE N-METHYLTRANSFERASE; HUMANS; LEUKEMIA; MICE; MICE, SCID; MODELS, MOLECULAR; MOLECULAR DOCKING SIMULATION; MYELOID-LYMPHOID LEUKEMIA PROTEIN; SMALL MOLECULE LIBRARIES; STRUCTURE-ACTIVITY RELATIONSHIP; X-RAY DIFFRACTION;

EID: 84962205041     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.5b01630     Document Type: Article

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