Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor

Journal of Medicinal Chemistry

Volumn 59, Issue 4, 2016, Pages 1440-1454

  Palmer, Wylie S ^a   Poncet Montange, Guillaume ^a   Liu, Gang ^a   Petrocchi, Alessia ^a   Reyna, Naphtali ^a   Subramanian, Govindan ^a   Theroff, Jay ^a   Yau, Anne ^a   Kost Alimova, Maria ^a   Bardenhagen, Jennifer P ^a   Leo, Elisabetta ^a   Shepard, Hannah E ^a   Tieu, Trang N ^a   Shi, Xi ^a   Zhan, Yanai ^a   Zhao, Shuping ^a   Barton, Michelle C ^a   Draetta, Giulio ^a   Toniatti, Carlo ^a   Jones, Philip ^a   Geck Do, Mary ^a   Andersen, Jannik N ^a   more..

^a UNIVERSITY OF TEXAS   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BROMODOMAIN AND PHD FINGER CONTAINING PROTEIN 1; BROMODOMAIN INHIBITOR; HISTONE ACETYLTRANSFERASE; IACS 9571; MONOCYTIC LEUKEMIA ZINC FINGER PROTEIN; N N DIMETHYLBENZIMIDAZOLONE BROMODOMAIN INHIBITOR; SULFONAMIDE; TRIPARTITE MOTIF CONTAINING PROTEIN 24; UNCLASSIFIED DRUG; ZINC FINGER PROTEIN; BENZIMIDAZOLE DERIVATIVE; BENZIMIDAZOLONE; BRPF1 PROTEIN, HUMAN; CARRIER PROTEIN; NUCLEAR PROTEIN; PROTEIN BINDING; SIGNAL TRANSDUCING ADAPTOR PROTEIN; TRIM24 PROTEIN, HUMAN;

ARTICLE; CANCER PROGNOSIS; CHROMOSOME REARRANGEMENT; CRYSTAL STRUCTURE; DRUG DESIGN; DRUG STRUCTURE; GENE; GENE EXPRESSION; HUMAN; IN VITRO STUDY; IN VIVO STUDY; LEUKEMIA; X RAY; ANIMAL; ANTAGONISTS AND INHIBITORS; CHEMISTRY; FEMALE; METABOLISM; METHYLATION; MOLECULAR DOCKING; MOUSE;

ADAPTOR PROTEINS, SIGNAL TRANSDUCING; ANIMALS; BENZIMIDAZOLES; CARRIER PROTEINS; DRUG DESIGN; FEMALE; HUMANS; METHYLATION; MICE; MOLECULAR DOCKING SIMULATION; NUCLEAR PROTEINS; PROTEIN BINDING;

EID: 84959366723     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.5b00405     Document Type: Article

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