Inhibition of c-kit receptor tyrosine kinase activity by STI 571, a selective tyrosine kinase inhibitor.

By M. Heinrich, D. Griffith, Brian J. Druker, C. Wait, Kristen A. Ott, A. J. Zigler. Blood, 2000

1,079 citations recorded by the source corpus.

Subfields: Genetics, Hematology, Immunology

View Paper: https://www.semanticscholar.org/paper/3d5788a8839695e794376eef165870ffbf14ab81

How researchers see this paper

The researchers whose trusted networks rank it highest, strongest advocate first. Every researcher gets a different order.

In Genetics

1. T. Hunter
2. Brian J. Druker
3. A. Hopkins

In Hematology

1. Brian J. Druker
2. T. Hunter
3. M. Heinrich
4. Christopher Corless
5. E. Scholar
6. A. Arora

In Immunology

1. T. Hunter

Citations in the corpus

• Oncogenic kinase signalling (2001, background): “41 ), which also inhibits Kit/SCFR and PDGFR-&beta”
• Efficacy and safety of imatinib mesylate in advanced gastrointestinal stromal tumors. (2002, background): “9,10,13 Subsequently, a single patient treated with imatinib for a chemotherapy-resistant metastatic gastrointestinal stromal tumor had a rapid, substantial, and durable response.”
• Clinical Pharmacokinetics of Imatinib (2005, background): “[6-9] KIT also plays a role in the CML is a haematological stem cell malignancy development of several human cancers, including caused by a reciprocal chromosomal translocation germ cell tumours, mast cell tumours, small-cell that generates the Philadelphia (Ph) chromosome.”
• Kinase mutations and imatinib response in patients with metastatic gastrointestinal stromal tumor. (2003, methodology): “Twenty-four hours after transfection, the cells were treated with control media or media containing various concentrations of imatinib for 90 minutes.(13) The cells were then collected, and protein lysates were prepared and analyzed for KIT or PDGFRA activation as previously described.”
• A quantitative analysis of kinase inhibitor selectivity (2008, background): “For example, the discovery that imatinib inhibits KIT in addition to ABL1 and the PDGF receptors first suggested the use of imatinib for the treatment of gastrointestinal stromal tumor”
• Role of Tyrosine Kinase Inhibitors in Cancer Therapy (2005, background): “It is also being studied in a phase III trial for imatinib-resistant GISTs.”
• The structure of Dasatinib (BMS-354825) bound to activated ABL kinase domain elucidates its inhibitory activity against imatinib-resistant ABL mutants. (2006, background): “Interestingly, imatinib, a potent KIT inhibitor and now the standard frontline therapy for advanced gastrointestinal stromal tumors (39, 40) binds to an inactive conformation of KIT (38).”
• How many drug targets are there? (2006, background): “(and which target association led to its first approval for chronic myeloid leukaemia), has subsequently been discovered to be have significant activity against several other clinically relevant kinases, such as c-KI”