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Assessment of Resistance to Tyrosine Kinase Inhibitors by an Interrogation of Signal Transduction Pathways by Antibody Arrays
Published on: September 19, 2018
Advances in studies of tyrosine kinase inhibitors and their acquired resistance
Qinlian Jiao1, Lei Bi2, Yidan Ren1
1International Biotechnology R&D Center, Shandong University School of Ocean, 180 Wenhua Xi Road, Weihai, Shandong, 264209, China.
Abstract:
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.
Insights
Protein tyrosine kinases (PTKs) are crucial in cell signaling and cancer. Tyrosine kinase inhibitors (TKIs) show promise in cancer treatment but acquired resistance remains a challenge.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- Protein tyrosine kinases (PTKs) are key enzymes in cellular signal transduction, regulating critical processes like cell growth and differentiation.
- Dysregulated PTK expression is implicated in various cancers, contributing to tumor invasion, metastasis, and angiogenesis.
- PTKs are established targets for anti-cancer drug development.
Purpose of the Study:
- To review the role of PTKs in cancer development.
- To outline the mechanisms of action for tyrosine kinase inhibitors (TKIs) in cancer therapy.
- To summarize acquired resistance mechanisms against TKIs.
Main Methods:
- Literature review of PTK function in cancer.
- Analysis of TKI therapeutic pathways.
- Examination of molecular mechanisms underlying TKI resistance.
Main Results:
- PTKs play a significant role in cancer cell proliferation and progression.
- TKIs effectively inhibit cancer cell growth by targeting PTK activity.
- Acquired resistance to TKIs is a major clinical limitation.
Conclusions:
- Understanding PTK signaling is vital for cancer therapy.
- TKIs represent a significant advancement in cancer treatment.
- Further research into TKI resistance mechanisms is necessary to improve patient outcomes.
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