Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFRα, Kit, and Src kinases: Novel type II inhibitor of gatekeeper mutants

Blood

Volumn 115, Issue 21, 2010, Pages 4206-4216

  Weisberg, Ellen ^a   Choi, Hwan Geun ^b   Ray, Arghya ^a   Barrett, Rosemary ^a   Zhang, Jianming ^b   Sim, Taebo ^b   Zhou, Wenjun ^b   Seeliger, Markus ^c   Cameron, Michael ^d   Azam, Mohammed ^e   Fletcher, Jonathan A ^f   Debiec Rychter, Maria ^g   Mayeda, Mark ^f   Moreno, Daisy ^a   Kung, Andrew L ^a   Janne, Pasi Antero ^a   Khosravi Far, Roya ^b   Melo, Junia V ^h   Manley, Paul W ⁱ   Adamia, Sophia ^a   Wu, Catherine ^a   Gray, Nathanael ^a,b   Griffin, James D ^a   more..

^a DANA FARBER CANCER INSTITUTE   (United States)

^b HARVARD MEDICAL SCHOOL   (United States)

^c UNIVERSITY OF CALIFORNIA   (United States)

^d SCRIPPS RESEARCH INSTITUTE   (United States)

^e CINCINNATI CHILDREN'S HOSPITAL MEDICAL CENTER   (United States)

^f BRIGHAM AND WOMEN S HOSPITAL   (United States)

^g UNIVERSITY OF LEUVEN   (Belgium)

^h INSTITUTE OF MEDICAL AND VETERINARY SCIENCE   (Australia)

ⁱ NOVARTIS PHARMA AG   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

BCR ABL PROTEIN; HG 78501; IMATINIB; NILOTINIB; PLATELET DERIVED GROWTH FACTOR ALPHA RECEPTOR; PROTEIN KINASE; PROTEIN TYROSINE KINASE; PROTEIN TYROSINE KINASE INHIBITOR; STEM CELL FACTOR; THREONINE; UNCLASSIFIED DRUG; ANTINEOPLASTIC AGENT; MUTANT PROTEIN; PIPERAZINE DERIVATIVE; PROTEIN KINASE INHIBITOR; PYRIMIDINE DERIVATIVE; STEM CELL FACTOR RECEPTOR;

ANIMAL EXPERIMENT; ANIMAL MODEL; APOPTOSIS; ARTICLE; CELL CYCLE PROGRESSION; CELL PROLIFERATION; CHRONIC MYELOID LEUKEMIA; CONTROLLED STUDY; CRYSTALLIZATION; DRUG BIOAVAILABILITY; DRUG EFFECT; DRUG HALF LIFE; DRUG POTENCY; DRUG SYNTHESIS; ENZYME ACTIVITY; ENZYME INHIBITION; GASTROINTESTINAL STROMAL TUMOR; GENE MUTATION; HUMAN; HUMAN CELL; HYPEREOSINOPHILIC SYNDROME; IN VIVO STUDY; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN PHOSPHORYLATION; WILD TYPE; AMINO ACID SUBSTITUTION; ANIMAL; CHEMICAL STRUCTURE; CHEMISTRY; DRUG ANTAGONISM; DRUG DEVELOPMENT; DRUG RESISTANCE; GENETICS; IN VITRO STUDY; MISSENSE MUTATION; TUMOR CELL LINE;

AMINO ACID SUBSTITUTION; ANIMALS; ANTINEOPLASTIC AGENTS; CELL LINE, TUMOR; DRUG DISCOVERY; DRUG RESISTANCE, NEOPLASM; FUSION PROTEINS, BCR-ABL; HUMANS; MOLECULAR STRUCTURE; MUTANT PROTEINS; MUTATION, MISSENSE; PIPERAZINES; PROTEIN KINASE INHIBITORS; PROTO-ONCOGENE PROTEINS C-KIT; PYRIMIDINES; RECEPTOR, PLATELET-DERIVED GROWTH FACTOR ALPHA; SRC-FAMILY KINASES; THREONINE;

EID: 77953636478     PISSN: 00064971     EISSN: 15280020     Source Type: Journal    
DOI: 10.1182/blood-2009-11-251751     Document Type: Article

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