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Advances in studies of tyrosine kinase inhibitors and their acquired resistance

期刊

MOLECULAR CANCER
卷 17, 期 -, 页码 -

出版社

BMC
DOI: 10.1186/s12943-018-0801-5

关键词

Cancer; Protein tyrosine kinase; Tyrosine kinase inhibitors; Acquired resistance

资金

  1. China Post doctoral International Exchange Program, National Natural Science Foundation of China [81402193]
  2. Postdoctoral Innovation Project of Shandong Province [147751]
  3. Postdoctoral Science Foundation of China [2015 M570597]
  4. National Natural Science Foundation of China [81500029]
  5. Natural Science Foundation of Shandong Province [BS2015YY05]

向作者/读者索取更多资源

Protein tyrosine kinase (PTK) is one of the major signaling enzymes in the process of cell signal transduction, which catalyzes the transfer of ATP-gamma-phosphate to the tyrosine residues of the substrate protein, making it phosphorylation, regulating cell growth, differentiation, death and a series of physiological and biochemical processes. Abnormal expression of PTK usually leads to cell proliferation disorders, and is closely related to tumor invasion, metastasis and tumor angiogenesis. At present, a variety of PTKs have been used as targets in the screening of anti-tumor drugs. Tyrosine kinase inhibitors (TKIs) compete with ATP for the ATP binding site of PTK and reduce tyrosine kinase phosphorylation, thereby inhibiting cancer cell proliferation. TKI has made great progress in the treatment of cancer, but the attendant acquired acquired resistance is still inevitable, restricting the treatment of cancer. In this paper, we summarize the role of PTK in cancer, TKI treatment of tumor pathways and TKI acquired resistance mechanisms, which provide some reference for further research on TKI treatment of tumors.

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