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Updated: Aug 23, 2026

Assessment of Resistance to Tyrosine Kinase Inhibitors by an Interrogation of Signal Transduction Pathways by Antibody Arrays
Published on: September 19, 2018
Receptor tyrosine kinase inhibitors as anti-angiogenic agents
Dong Wook Kim1, Bo Lu, Dennis E Hallahan
1Department of Radiation Oncology, Vanderbilt-Ingram Cancer Center, 1301 22nd Avenue South, Nashville, TN 37232-5671, USA.
Abstract:
Receptor tyrosine kinases (RTKs) and their ligands have been implicated in angiogenesis and current data suggest that they are potential cancer therapeutic targets. Split-kinase domain RTKs, including receptors for vascular endothelial growth factor receptor, platelet-derived growth factor and fibroblast growth factor, have important roles in tumor angiogenesis. RTK inhibitors targeting tumor microvasculature have shown promising results in preclinical studies, and use of these compounds as single agents, or in combination with other cytotoxic therapies, including radiation, is an area of active clinical investigation. Preclinical and clinical data from representative anti-angiogenic RTK inhibitors will be discussed in this review.
Insights
Receptor tyrosine kinases (RTKs) are key targets for anti-angiogenesis cancer therapies. Inhibitors targeting RTKs show promise in preclinical studies and are under active clinical investigation for cancer treatment.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Receptor tyrosine kinases (RTKs) and their ligands play crucial roles in angiogenesis.
- Dysregulated angiogenesis is a hallmark of cancer, making RTKs potential therapeutic targets.
Purpose of the Study:
- To review the role of split-kinase domain RTKs in tumor angiogenesis.
- To discuss the preclinical and clinical data of anti-angiogenic RTK inhibitors.
Main Methods:
- Review of preclinical and clinical studies on RTK inhibitors.
- Focus on split-kinase domain RTKs, including VEGFR, PDGFR, and FGFR.
Main Results:
- RTK inhibitors targeting tumor microvasculature demonstrate promising preclinical results.
- RTK inhibitors are being investigated as single agents and in combination therapies.
Conclusions:
- Split-kinase domain RTKs are important targets for anti-angiogenic cancer therapy.
- RTK inhibitors represent a promising therapeutic strategy for various cancers.
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