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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
Tyrosine kinase inhibitors for solid tumors in the past 20 years (2001-2020)
Liling Huang1, Shiyu Jiang1, Yuankai Shi2
1Department of Medical Oncology, National Cancer Center/National Clinical Research Center for Cancer/Cancer Hospital, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing Key Laboratory of Clinical Study On Anticancer Molecular Targeted Drugs, No. 17 Panjiayuan Nanli, Chaoyang District, Beijing, 100021, China.
Abstract:
Tyrosine kinases are implicated in tumorigenesis and progression, and have emerged as major targets for drug discovery. Tyrosine kinase inhibitors (TKIs) inhibit corresponding kinases from phosphorylating tyrosine residues of their substrates and then block the activation of downstream signaling pathways. Over the past 20 years, multiple robust and well-tolerated TKIs with single or multiple targets including EGFR, ALK, ROS1, HER2, NTRK, VEGFR, RET, MET, MEK, FGFR, PDGFR, and KIT have been developed, contributing to the realization of precision cancer medicine based on individual patient's genetic alteration features. TKIs have dramatically improved patients' survival and quality of life, and shifted treatment paradigm of various solid tumors. In this article, we summarized the developing history of TKIs for treatment of solid tumors, aiming to provide up-to-date evidence for clinical decision-making and insight for future studies.
Insights
Tyrosine kinase inhibitors (TKIs) have revolutionized cancer treatment by targeting specific genetic alterations in solid tumors. These targeted therapies have significantly improved patient survival and quality of life.
Area of Science:
- Oncology
- Pharmacology
- Molecular Biology
Background:
- Tyrosine kinases play a crucial role in cancer development and progression.
- Targeting these kinases is a key strategy in modern cancer drug discovery.
- Tyrosine kinase inhibitors (TKIs) block specific signaling pathways involved in tumorigenesis.
Purpose of the Study:
- To summarize the historical development of TKIs for solid tumor treatment.
- To provide an overview of TKIs targeting various kinases like EGFR, ALK, and VEGFR.
- To offer insights for clinical decision-making and future research in precision cancer medicine.
Main Methods:
- Review of the literature on TKIs and their clinical applications.
- Analysis of the development and targets of various TKIs over the past 20 years.
- Synthesis of evidence regarding the impact of TKIs on solid tumor treatment paradigms.
Main Results:
- Development of numerous single and multi-targeted TKIs (e.g., EGFR, ALK, VEGFR, MET).
- TKIs have enabled precision cancer medicine based on genetic alterations.
- Significant improvements in patient survival and quality of life observed with TKI therapy.
Conclusions:
- TKIs have transformed the treatment landscape for various solid tumors.
- The development of TKIs represents a major advancement in targeted cancer therapy.
- Continued research into TKIs is essential for further optimizing cancer treatment strategies.
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