Advances in studies of tyrosine kinase inhibitors and their acquired resistance

• Published in: Molecular cancer Vol. 17; no. 1; pp. 36 - 12
• Main Authors: Jiao, Qinlian, Bi, Lei, Ren, Yidan, Song, Shuliang, Wang, Qin, Wang, Yun-shan
• Format: Journal Article
• Language: English
• Published: England BioMed Central Ltd 19.02.2018; BioMed Central; BMC
• Subjects: Acquired resistance; Analysis; Animals; Cancer; Care and treatment; Cell Line, Tumor; Cell proliferation; Cell Proliferation - drug effects; Diagnosis; Drug resistance; Humans; Neoplasms - drug therapy; Neoplasms - metabolism; Physiological aspects; Protein Kinase Inhibitors - pharmacology; Protein Kinase Inhibitors - therapeutic use; Protein tyrosine kinase; Protein-Tyrosine Kinases - antagonists & inhibitors; Protein-Tyrosine Kinases - metabolism; Review; Signal Transduction - drug effects; Tyrosine; Tyrosine kinase inhibitors; Protein tyrosine kinase; Acquired resistance; Tyrosine kinase inhibitors; Cancer
• ISSN: 1476-4598; 1476-4598
• DOI: 10.1186/s12943-018-0801-5

Protein tyrosine kinase (PTK) is one of the major signaling enzymes in the process of cell signal transduction, which catalyzes the transfer of ATP-γ-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.