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Updated: Jun 8, 2026

Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries
Published on: January 22, 2019
[Cytoplasmic kinase inhibitors]
1Division of Functional Genomics, Jichi Medical University.
Abstract:
Protein kinases play essential roles in the regulation of cell proliferation. Point mutations or/and fusions of protein kinases are frequently identified in human cancers, and targeting such activated kinases provides us with a chance to eradicate tumor cells. This was first proved by imatinib mesylate that inhibits ABL tyrosine kinase and, thereby, efficiently kills malignant cells in chronic myeloid leukemia. In addition, other clinical trials are ongoing for kinase inhibitors against EML4--ALK in lung cancer, JAK2 in myeloproliferative disorders and BRAF in malignant melanoma. Early reports indeed reveal that such targeting compounds are promising drugs for human cancers with activated kinases.
Insights
Targeting activated protein kinases, through mutations or fusions, offers a promising strategy for cancer treatment. Kinase inhibitors are being developed for various cancers, showing potential for tumor eradication.
Area of Science:
- Biochemistry
- Oncology
- Pharmacology
Background:
- Protein kinases regulate cell proliferation.
- Aberrant protein kinase activity (mutations/fusions) is common in human cancers.
- Targeting these kinases is a validated therapeutic strategy.
Purpose of the Study:
- To review the role of protein kinases in cancer.
- To highlight the therapeutic potential of kinase inhibitors.
- To discuss ongoing clinical trials for specific kinase inhibitors.
Main Methods:
- Literature review of protein kinase function in cancer.
- Analysis of clinical trial data for kinase inhibitors.
- Examination of specific examples like imatinib, EML4-ALK, JAK2, and BRAF inhibitors.
Main Results:
- Imatinib mesylate demonstrates efficacy against ABL tyrosine kinase in chronic myeloid leukemia.
- Clinical trials show promise for inhibitors targeting EML4-ALK, JAK2, and BRAF in various cancers.
- Activated kinases represent viable targets for novel cancer therapies.
Conclusions:
- Targeting activated protein kinases is a successful approach in cancer therapy.
- Kinase inhibitors are promising drugs for treating human cancers.
- Further development of kinase inhibitors holds significant therapeutic potential.
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