Inhibitors that stabilize a closed RAF kinase domain conformation induce dimerization

Nature Chemical Biology

Volumn 9, Issue 7, 2013, Pages 428-436

  Lavoie, Hugo ^a   Thevakumaran, Neroshan ^b,c   Gavory, Gwenaëlle ^a   Li, John J ^b,c   Padeganeh, Abbas ^a   Guiral, Sébastien ^a   Duchaine, Jean ^a   Mao, Daniel Y L ^b,d   Bouvier, Michel ^a,e   Sicheri, Frank ^b,c   Therrien, Marc ^a,e  

^a INSTITUTE FOR RESEARCH IN IMMUNOLOGY AND CANCER   (Canada)

^b MOUNT SINAI HOSPITAL   (Canada)

^c UNIVERSITY OF TORONTO   (Canada)

^d RYERSON UNIVERSITY   (Canada)

^e UNIVERSITÉ DE MONTRÉAL   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

2 [4 (1 HYDROXYIMINO 5 INDANYL) 3 (4 PYRIDINYL) 1H PYRAZOL 1 YL]ETHANOL; 2 [4 (2 DIMETHYLAMINOETHOXY)PHENYL] 4 (1 HYDROXYIMINO 5 INDANYL) 5 (4 PYRIDINYL) 1H IMIDAZOLE; 4 (4 FLUOROPHENYL) 2 (4 HYDROXYPHENYL) 5 (4 PYRIDYL)IMIDAZOLE; 4 (4 FLUOROPHENYL) 2 (4 METHYLSULFINYLPHENYL) 5 (4 PYRIDYL)IMIDAZOLE; A RAF KINASE; ADENOSINE TRIPHOSPHATE; AZ 628; B RAF KINASE; C RAF KINASE; DASATINIB; DIMER; DORAMAPIMOD; IMATINIB; K RAS PROTEIN; L 779450; MITOGEN ACTIVATED PROTEIN KINASE; N [3 (5 CHLORO 1H PYRROLO[2,3 B]PYRIDINE 3 CARBONYL) 2,4 DIFLUOROPHENYL]PROPANESULFONAMIDE; NILOTINIB; PROTEIN 14 3 3; PROTEIN SERINE THREONINE KINASE INHIBITOR; RAF PROTEIN; SORAFENIB; TIVOZANIB; UNCLASSIFIED DRUG;

ALLOSTERISM; ARTICLE; BINDING AFFINITY; BIOLUMINESCENCE RESONANCE ENERGY TRANSFER; CONTROLLED STUDY; CRYSTAL STRUCTURE; CRYSTALLOGRAPHY; DIMERIZATION; ENZYME ACTIVATION; ENZYME ACTIVITY; ENZYME CONFORMATION; ENZYME INHIBITION; ENZYMIC BIOSENSOR; HUMAN; HUMAN CELL; PRIORITY JOURNAL; PROTEIN DOMAIN; PROTEIN EXPRESSION; TITRIMETRY; TRANSACTIVATION; WILD TYPE;

BIOSENSING TECHNIQUES; CRYSTALLIZATION; DIMERIZATION; DNA, COMPLEMENTARY; ENERGY TRANSFER; HEK293 CELLS; HUMANS; LUMINESCENCE; MUTATION; NEOPLASMS; PROTEIN KINASE INHIBITORS; PROTEIN STRUCTURE, TERTIARY; PROTO-ONCOGENE PROTEINS C-RAF; TIME FACTORS; ULTRACENTRIFUGATION;

EID: 84879422871     PISSN: 15524450     EISSN: 15524469     Source Type: Journal    
DOI: 10.1038/nchembio.1257     Document Type: Article

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