Dual kinase-bromodomain inhibitors for rationally designed polypharmacology

Nature Chemical Biology

Volumn 10, Issue 4, 2014, Pages 305-312

  Ciceri, Pietro ^a   Müller, Susanne ^b   O'Mahony, Alison ^a   Fedorov, Oleg ^b   Filippakopoulos, Panagis ^b   Hunt, Jeremy P ^a   Lasater, Elisabeth A ^c   Pallares, Gabriel ^a   Picaud, Sarah ^b   Wells, Christopher ^b   Martin, Sarah ^b   Wodicka, Lisa M ^a   Shah, Neil P ^c   Treiber, Daniel K ^a   Knapp, Stefan ^b  

^a DiscoveRx Corporation   (United States)

^b UNIVERSITY OF OXFORD   (United Kingdom)

^c UNIVERSITY OF CALIFORNIA   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 (8 CYCLOPENTYL 7 ETHYL 5,6,7,8 TETRAHYDRO 5 METHYL 6 OXO 2 PTERIDINYLAMINO) 3 METHOXY N (1 METHYL 4 PIPERIDINYL)BENZAMIDE; DUAL KINASE BROMODOMAIN INHIBITOR; FEDRATINIB; FLT3 LIGAND; JANUS KINASE 2 INHIBITOR; PHOSPHOTRANSFERASE; PHOSPHOTRANSFERASE INHIBITOR; POLO LIKE KINASE INHIBITOR; PROTEIN BRD4; UNCLASSIFIED DRUG;

ARTICLE; CARCINOGENESIS; CRYSTAL STRUCTURE; DRUG DESIGN; DRUG POTENCY; DRUG TARGETING; ENZYME INHIBITION; EPIGENETICS; HUMAN; HUMAN CELL; PRIORITY JOURNAL; PROTEIN DOMAIN; PROTEIN FAMILY; STRUCTURE ACTIVITY RELATION;

ANTINEOPLASTIC COMBINED CHEMOTHERAPY PROTOCOLS; BLOTTING, WESTERN; CALORIMETRY; CELL LINE, TUMOR; CRYSTALLIZATION; DRUG DESIGN; DRUG INTERACTIONS; DRUG SCREENING ASSAYS, ANTITUMOR; EPIGENESIS, GENETIC; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; NEOPLASMS; POLYPHARMACOLOGY; PROTEIN KINASE INHIBITORS; PROTO-ONCOGENE PROTEINS C-MYC; PTERIDINES; PYRROLIDINES; RECOMBINANT PROTEINS; SIGNAL TRANSDUCTION; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONAMIDES;

EID: 84896611007     PISSN: 15524450     EISSN: 15524469     Source Type: Journal    
DOI: 10.1038/nchembio.1471     Document Type: Article

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