Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains

Journal of Medicinal Chemistry

Volumn 59, Issue 11, 2016, Pages 5391-5402

  Crawford, Terry D ^a   Tsui, Vickie ^a   Flynn, E Megan ^a   Wang, Shumei ^a   Taylor, Alexander M ^b   Côté, Alexandre ^b   Audia, James E ^b   Beresini, Maureen H ^a   Burdick, Daniel J ^a   Cummings, Richard ^b   Dakin, Les A ^b   Duplessis, Martin ^b   Good, Andrew C ^b   Hewitt, Michael C ^b   Huang, Hon Ren ^b   Jayaram, Hariharan ^b   Kiefer, James R ^a   Jiang, Ying ^c   Murray, Jeremy ^a   Nasveschuk, Christopher G ^b   Pardo, Eneida ^b   Poy, Florence ^b   Romero, F Anthony ^a   Tang, Yong ^b   Wang, Jian ^c   Xu, Zhaowu ^c   Zawadzke, Laura E ^b   Zhu, Xiaoyu ^c   Albrecht, Brian K ^b   Magnuson, Steven R ^a   Bellon, Steve ^b   Cochran, Andrea G ^a   more..

^a GENENTECH INC   (United States)

^b Department of Structural Biology   (United States)

^c WUXI APPTEC   (China)

Author keywords

[No Author keywords available]

Indexed keywords

2 (5 BROMO 2 METHOXY 3 NITRO 4 PYRIDYL) N,N DIMETHYLETHENAMINE; 2 METHOXY 4 METHYL 3 NITROPYRIDINE; 3 (6 ALLYL 7 OXO 1H PYRROLO[2,3 C]PYRIDIN 4 YL) N,N DIMETHYL BENZAMIDE; 3 (6 BUT 2 ENYL 7 OXO 1H PYRROLO[2,3 C]PYRIDIN 4 YL) N,N DIMETHYL BENZAMIDE; 3 (6 BUT 3 ENYL 7 OXO 1H PYRROLO[2,3 C]PYRIDIN 4 YL) N,N DIMETHYL BENZAMIDE; 3 (6 BUTYL 7 OXO 1H PYRROLO[2,3 C]PYRIDIN 4 YL) N,N DIMETHYLBENZAMIDE; 3 (6 ETHYL 7 OXO 1H PYRROLO[2,3 C]PYRIDIN 4 YL) N,N DIMETHYLBENZAMIDE; 3 (6 METHYL 7 OXO 1H PYRROLO[2,3 C]PYRIDIN 4 YL) N,N DIMETHYLBENZAMIDE; 3 (6 PROPYL 7 OXO 1H PYRROLO[2,3 C]PYRIDIN 4 YL) N,N DIMETHYLBENZAMIDE; 3 [6 (2 METHOXYETHYL) 7 OXO 1H PYRROLO[2,3 C]PYRIDIN 4 YL] N,N DIMETHYL BENZAMIDE; 4 BROMO 1 (PARA TOLYLSULFONYL) 6H PYRROLO[2,3 C]PYRIDIN 7 ONE; 4 BROMO 7 METHOXY 1 (PAARA TOLYLSULFONYL)PYRROLO[2,3 C]PYRIDINE; 4 BROMO 7 METHOXY 1H PYRROLO[2,3 C]PYRIDINE; 5 BROMO 2 METHOXY 4 METHYL 3 NITROPYRIDINE; 6 METHYL 4 BROMO 1 (PARA TOLYLSULFONYL)PYRROLO[2,3 C]PYRIDIN 7 ONE; BROMODOMAIN CONTAINING PROTEIN 4 INHIBITOR; BROMODOMAIN CONTAINING PROTEIN 9 INHIBITOR; BROMODOMAIN INHIBITOR; CAT EYE SYNDROME CRITICAL REGION PROTEIN 2 BROMODOMAIN INHIBITOR; PROTEIN INHIBITOR; TRANSCRIPTION FACTOR IID SUBUNIT 2 INHIBITOR; UNCLASSIFIED DRUG; WATER; 6-METHYL PYRROLOPYRIDONE; BRD4 PROTEIN, HUMAN; BRD9 PROTEIN, HUMAN; CECR2 PROTEIN, HUMAN; HISTONE ACETYLTRANSFERASE; LIGAND; NUCLEAR PROTEIN; PYRIDONE DERIVATIVE; PYRROLE DERIVATIVE; TAF2 PROTEIN, HUMAN; TATA BINDING PROTEIN ASSOCIATED FACTOR; TATA-BINDING PROTEIN ASSOCIATED FACTOR 250 KDA; TRANSCRIPTION FACTOR; TRANSCRIPTION FACTOR IID;

ARTICLE; CRYSTAL STRUCTURE; DRUG BINDING; DRUG CONFORMATION; HYDROPHOBICITY; LIPOPHILICITY; ANTAGONISTS AND INHIBITORS; BINDING SITE; CHEMISTRY; CONFORMATION; DOSE RESPONSE; DRUG EFFECTS; FLUORESCENCE RESONANCE ENERGY TRANSFER; FLUOROMETRY; HUMAN; METABOLISM; MOLECULAR MODEL; STRUCTURE ACTIVITY RELATION; SYNTHESIS;

BINDING SITES; DOSE-RESPONSE RELATIONSHIP, DRUG; FLUORESCENCE RESONANCE ENERGY TRANSFER; FLUOROMETRY; HISTONE ACETYLTRANSFERASES; HUMANS; LIGANDS; MODELS, MOLECULAR; MOLECULAR CONFORMATION; NUCLEAR PROTEINS; PYRIDONES; PYRROLES; STRUCTURE-ACTIVITY RELATIONSHIP; TATA-BINDING PROTEIN ASSOCIATED FACTORS; TRANSCRIPTION FACTOR TFIID; TRANSCRIPTION FACTORS; WATER;

EID: 84974653282     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.6b00264     Document Type: Article

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