Detection of allosteric kinase inhibitors by displacement of active site probes

Journal of Biomolecular Screening

Volumn 17, Issue 6, 2012, Pages 813-821

  Lebakken, Connie S ^a   Reichling, Laurie J ^a   Ellefson, Jason M ^a   Riddle, Steven M ^a  

^a Life Technologies Corporation   (United States)

Author keywords

ABL; AKT; allosteric interactions; kinase inhibition; MEK; TR FRET

Indexed keywords

1,4 DIAMINO 1,4 BIS(2 AMINOPHENYLTHIO) 2,3 DICYANOBUTADIENE; 2 (2 AMINO 3 METHOXYPHENYL)CHROMONE; 2 (2 CHLORO 4 IODOANILINO) N CYCLOPROPYLMETHOXY 3,4 DIFLUOROBENZAMIDE; BCR ABL PROTEIN; FLUORESCENT DYE; MITOGEN ACTIVATED PROTEIN KINASE; MITOGEN ACTIVATED PROTEIN KINASE INHIBITOR; N (2,3 DIHYDROXYPROPOXY) 3,4 DIFLUORO 2 (2 FLUORO 4 IODOANILINO)BENZAMIDE; PHOSPHOTRANSFERASE INHIBITOR; SELUMETINIB; STAUROSPORINE; SUNITINIB;

ALLOSTERISM; ARTICLE; BINDING ASSAY; BINDING SITE; COMPETITIVE INHIBITION; CONTROLLED STUDY; DRUG BINDING; DRUG DETERMINATION; ENZYME ACTIVE SITE; FLUORESCENCE RESONANCE ENERGY TRANSFER; HUMAN; IC 50; PRIORITY JOURNAL; PROTEIN PHOSPHORYLATION;

ADENOSINE TRIPHOSPHATE; ALLOSTERIC REGULATION; BINDING, COMPETITIVE; CATALYTIC DOMAIN; DRUG EVALUATION, PRECLINICAL; FLUORESCENCE RESONANCE ENERGY TRANSFER; FUSION PROTEINS, BCR-ABL; HUMANS; INHIBITORY CONCENTRATION 50; MAP KINASE KINASE 1; PROTEIN BINDING; PROTEIN KINASE INHIBITORS; PROTEIN-TYROSINE KINASES;

EID: 84862236266     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057112439889     Document Type: Article

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