Discovery of epigenetic regulator i-bet762: Lead optimization to afford a clinical candidate inhibitor of the bet bromodomains

Journal of Medicinal Chemistry

Volumn 56, Issue 19, 2013, Pages 7501-7515

  Mirguet, Olivier ^a,c   Gosmini, Romain ^a,d   Toum, Jéroîme ^a   Clément, Catherine A ^a   Barnathan, Mélanie ^a   Brusq, Jean Marie ^a   Mordaunt, Jacqueline E ^b   Grimes, Richard M ^b   Crowe, Miriam ^b   Pineau, Olivier ^a   Ajakane, Myriam ^a   Daugan, Alain ^a   Jeffrey, Phillip ^b   Cutler, Leanne ^b   Haynes, Andrea C ^b   Smithers, Nicholas N ^b   Chung, Chun Wa ^b   Bamborough, Paul ^b   Uings, Iain J ^b   Lewis, Antonia ^b   Witherington, Jason ^b   Parr, Nigel ^b   Prinjha, Rab K ^b   Nicodème, Edwige ^a   more..

^a GLAXOSMITHKLINE   (France)

^b GLAXOSMITHKLINE   (United Kingdom)

^c INSTITUT DE RECHERCHES INTERNATIONALES SERVIER   (France)

^d Galapagos SASU   (France)

Author keywords

[No Author keywords available]

Indexed keywords

APOLIPOPROTEIN A1; BENZODIAZEPINE RECEPTOR BLOCKING AGENT; I BET 762; NUCLEAR PROTEIN; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BROMO AND EXTRA C TERMINAL DOMAIN; DRUG SYNTHESIS; EPIGENETICS; HUMAN; HUMAN CELL; MOUSE; NONHUMAN; PROTEIN DOMAIN; RAT; STRUCTURE ACTIVITY RELATION; TESTIS CARCINOMA;

ANIMALS; ANTI-INFLAMMATORY AGENTS; ANTINEOPLASTIC AGENTS; APOLIPOPROTEIN A-I; BENZODIAZEPINES; DOGS; EPIGENESIS, GENETIC; HUMANS; MACACA FASCICULARIS; MICE; MODELS, MOLECULAR; NUCLEAR PROTEINS; PERMEABILITY; PROTEIN STRUCTURE, TERTIARY; RATS; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSCRIPTION FACTORS;

EID: 84885675970     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm401088k     Document Type: Article

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