Direct binding assay for the detection of type IV allosteric inhibitors of Abl

Journal of the American Chemical Society

Volumn 134, Issue 22, 2012, Pages 9138-9141

  Schneider, Ralf ^a   Becker, Christian ^b   Simard, Jeffrey R ^a,d   Getlik, Matthäus ^a,e   Bohlke, Nina ^a,f   Janning, Petra ^c   Rauh, Daniel ^a,b  

^a CHEMICAL GENOMICS CENTRE OF THE MAX PLANCK SOCIETY   (Germany)

^b TU DORTMUND UNIVERSITY   (Germany)

^c MAX PLANCK INSTITUTE OF MOLECULAR PHYSIOLOGY   (Germany)

^d AMGEN INC   (United States)

^e ONTARIO INSTITUTE FOR CANCER RESEARCH   (Canada)

^f TECHNISCHE UNIVERSITÄT BERLIN   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

ALLOSTERIC INHIBITOR; ALLOSTERIC SITE; BINDING ASSAYS; BREAKPOINT CLUSTER REGIONS; CELLULAR ENZYMES; CONSTITUTIVELY ACTIVES; FUSION PROTEINS; HIGH-THROUGHPUT SCREENING; IMATINIB; KINASE DOMAINS; POINT MUTATIONS; TYROSINE KINASE;

AMINO ACIDS;

ENZYMES;

ABELSON KINASE; ABELSON KINASE TYPE IV INHIBITOR; BCR ABL PROTEIN; DASATINIB; IMATINIB; MYRISTIC ACID; NILOTINIB; PHOSPHOTRANSFERASE INHIBITOR; UNCLASSIFIED DRUG;

ALLOSTERISM; ARTICLE; ASSAY; BINDING AFFINITY; CANCER PATIENT; CANCER RESISTANCE; CONFORMATIONAL TRANSITION; CRYSTAL STRUCTURE; DISSOCIATION CONSTANT; DRUG BINDING SITE; DRUG PROTEIN BINDING; HIGH THROUGHPUT SCREENING; HUMAN; LEUKEMIA; LIGAND BINDING; POINT MUTATION; PROTEIN DOMAIN; TANDEM MASS SPECTROMETRY;

MODELS, MOLECULAR; MOLECULAR STRUCTURE; PROTEIN KINASE INHIBITORS; PROTO-ONCOGENE PROTEINS C-ABL; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84861854598     PISSN: 00027863     EISSN: 15205126     Source Type: Journal    
DOI: 10.1021/ja303858w     Document Type: Article

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