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Updated: Aug 21, 2026

A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors
Published on: December 7, 2014
[Imatinib--a new perspective in the treatment of tumors]
Abstract:
Among novel promising approaches to anticancer therapy belongs the targeting inhibition of signal transduction. This review outlines present-day experiences with imatinib (Glivec), a potent inhibitor of the tyrosine kinases bcr-abl, c-kit and platelet-derived growth factor receptor kinase. Due to inhibition of bcr-abl tyroxine kinase, imatinib has rapidly become the standard therapy for chronic myelocytic leukemia; inhibition of c-kit receptor explains its effectivity in the treatment of patients with gastrointestinal stromal tumors. Another known target of imatinib is tyrosine kinase of PDGFR, which is activated in numerous malignancies, particularly in dermatofibrosarcoma protuberans. Discovery of the novel fusion gene in hypereosinophilic syndrome (FIPILI-PFGFRA, whose product is an imatinib sensitive protein kinase) permitted to treat successfully this event. Possible combination of imatinib with conventional chemotherapeutic drugs and other key signal transduction inhibitors are mentioned.
Insights
Imatinib effectively targets specific tyrosine kinases, revolutionizing treatment for chronic myelocytic leukemia and gastrointestinal stromal tumors. This targeted therapy also shows promise for other malignancies and hypereosinophilic syndrome.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Context:
- Signal transduction pathways are crucial in cancer development.
- Targeted therapies offer novel anticancer strategies.
- Imatinib (Glivec) is a key tyrosine kinase inhibitor.
Purpose:
- To review current therapeutic experiences with imatinib.
- To highlight imatinib's mechanisms of action and clinical applications.
- To discuss potential combination therapies involving imatinib.
Summary:
- Imatinib inhibits bcr-abl tyrosine kinase, establishing it as standard therapy for chronic myelocytic leukemia.
- Inhibition of c-kit receptor by imatinib is effective in treating gastrointestinal stromal tumors.
- Imatinib targets platelet-derived growth factor receptor (PDGFR) kinase, relevant in various malignancies like dermatofibrosarcoma protuberans and FIPILI-PFGFRA-driven hypereosinophilic syndrome.
Impact:
- Imatinib has transformed the treatment landscape for specific leukemias and tumors.
- Targeted inhibition of signal transduction pathways represents a significant advancement in cancer therapy.
- Further research into imatinib combinations may enhance treatment efficacy.
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