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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
Receptor tyrosine kinases: biological functions and anticancer targeted therapy
Nan Zhang1, Yongsheng Li1,2
1Chongqing University Cancer Hospital, School of Medicine Chongqing University Chongqing China.
Abstract:
Receptor tyrosine kinases (RTKs) are a class of protein kinases that play crucial roles in various cellular processes, including cell migration, morphological differentiation, cell growth, and angiogenesis. In humans, 58 RTKs have been identified and categorized into 20 distinct families based on the composition of their extracellular regions. RTKs are primarily activated by specific ligands that bind to their extracellular region. They not only regulate tumor transformation, proliferation, metastasis, drug resistance, and angiogenesis, but also initiate and maintain the self-renewal and cloning ability of cancer stem cells. Accurate diagnosis and grading of tumors with dysregulated RTKs are essential in clinical practice. There is a growing body of evidence supporting the benefits of RTKs-targeted therapies for cancer patients, and researchers are actively exploring new targets and developing targeted agents. However, further optimization of RTK inhibitors is necessary to effectively target the diverse RTK alterations observed in human cancers. This review provides insights into the classification, structure, activation mechanisms, and expression of RTKs in tumors. It also highlights the research advances in RTKs targeted anticancer therapy and emphasizes their significance in optimizing cancer diagnosis and treatment strategies.
Insights
Receptor tyrosine kinases (RTKs) are vital for cell functions and cancer development. Targeted therapies show promise, but optimizing RTK inhibitors is crucial for effective cancer treatment.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- Receptor tyrosine kinases (RTKs) are key regulators of cellular processes like growth and angiogenesis.
- Dysregulated RTKs are implicated in tumor progression, metastasis, and cancer stem cell self-renewal.
- Targeted therapies offer potential benefits for cancer patients with RTK alterations.
Purpose of the Study:
- To review the classification, structure, and activation mechanisms of RTKs.
- To highlight advances in RTK-targeted anticancer therapies.
- To emphasize the role of RTKs in cancer diagnosis and treatment optimization.
Main Methods:
- Literature review of RTK classification and function.
- Analysis of RTK roles in tumor biology.
- Summary of current RTK-targeted therapy research and development.
Main Results:
- 58 human RTKs exist in 20 families, activated by specific ligands.
- RTKs regulate critical cancer hallmarks, including proliferation and angiogenesis.
- RTK-targeted therapies are advancing, but inhibitor optimization is needed.
Conclusions:
- Understanding RTK biology is essential for cancer diagnosis and treatment.
- RTK-targeted therapies represent a significant advancement in oncology.
- Further research is needed to refine RTK inhibitors for diverse cancer alterations.
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