The c-KIT mutation causing human mastocytosis is resistant to STI571 and other KIT kinase inhibitors; kinases with enzymatic site mutations show different inhibitor sensitivity profiles than wild-type kinases and those with regulatory-type mutations

Blood

Volumn 99, Issue 5, 2002, Pages 1741-1744

  Ma, Yongsheng ^a,b,c,d,e   Zeng, Shan ^a,b,c,d,e   Metcalfe, Dean D ^a,b,c,d,e   Akin, Cem ^a,b,c,d,e   Dimitrijevic, Sasa ^a,b,c,d,e   Butterfield, Joseph H ^a,b,c,d,e   McMahon, Gerald ^a,b,c,d,e   Jack Longley, B ^a,b,c,d,e  

^a Columbia University ^*  (United States)

^b NATIONAL INSTITUTE OF ALLERGY AND INFECTIOUS DISEASES   (United States)

^c NOVARTIS PHARMA AG   (Switzerland)

^d MAYO CLINIC   (United States)

^e SUGEN INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTINEOPLASTIC AGENT; ASPARTIC ACID; IMATINIB; PROTEIN KINASE INHIBITOR; STEM CELL FACTOR; SU 9529; UNCLASSIFIED DRUG; VALINE;

AMINO ACID SUBSTITUTION; ANIMAL CELL; APOPTOSIS; ARTICLE; CELL ACTIVATION; CELL PROLIFERATION; CONTROLLED STUDY; ENZYME ACTIVE SITE; ENZYME INHIBITION; ENZYME REGULATION; GASTROINTESTINAL TUMOR; GENE MUTATION; HUMAN; HUMAN CELL; MALIGNANT NEOPLASTIC DISEASE; MASTOCYTOSIS; NONHUMAN; ONCOGENE C KIT; PRIORITY JOURNAL; STROMA;

EID: 0036493872     PISSN: 00064971     EISSN: None     Source Type: Journal    
DOI: 10.1182/blood.V99.5.1741     Document Type: Article

References (19)

1. Human proto-oncogene c-kit: A new cell surface receptor tyrosine kinase for an unidentified ligand
2. Primary structure and functional expression of rat and human stem cell factor DNAs
3. The kit ligand, stem cell factor
4. Identification of mutations in the coding sequence of the proto-oncogene c-KIT in a human mast cell leukemia cell line causing ligand-independent activation of c-KIT product
5. Identification of a point mutation in the catalytic domain of the protooncogene c-kit in peripheral blood mononuclear cells of patients who have mastocytosis with an associated hematologic disorder
6. Somatic c-KIT activating mutation in urticaria pigmentosa and aggressive mastocytosis: Establishment of clonality in a human mast cell neoplasm
7. Activating and dominant inactivating c-KIT catalytic domain mutations in distinct clinical forms of human mastocytosis
8. Ligand-independent activation of c-kit receptor tyrosine kinase in a murine mastocytoma cell line p815 generated by a point mutation
9. Clustering of activating mutations in c-KIT's juxtamembrane coding region in canine mast cell neoplasms
10. Indolinone derivatives inhibit constitutively activated KIT mutants and kill neoplastic mast cells
11. Classes of c-KIT activating mutations: Proposed mechanisms of action and implications for disease classification and therapy
12. Gain-of-function mutations of c-kit in human gastrointestinal stromal tumors
13. Inhibition of spontaneous receptor phosphorylation by residues in a putative α-helix in the KIT intracellular juxtamembrane region
14. A proposed classification for mastocytosis incorporating molecular genetics
15. New approaches to therapy for mastocytosis: A case for treatment with kit kinase inhibitors
16. Establishment of an immature mast cell line from a patient with mast cell leukemia
17. Inhibition of the Abl protein-tyrosine kinase in vitro and in vivo by a 2-phenylaminopyrimidine derivative
18. Inhibition of c-kit receptor tyrosine kinase activity by STI 571, a selective tyrosine kinase inhibitor
19. Clinical resistance to STI-571 cancer therapy caused by BCR-ABL gene mutation or amplification