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Updated: May 23, 2026

Assessment of Resistance to Tyrosine Kinase Inhibitors by an Interrogation of Signal Transduction Pathways by Antibody Arrays
Published on: September 19, 2018
Targeting of EPH receptor tyrosine kinases for anticancer therapy
Eva Nievergall1, Thomas Saunders, Martin Lackmann
1Department of Biochemistry and Molecular Biology, Monash University, Victoria, Australia.
Abstract:
Intense research over the past 15 years has demonstrated Eph receptors and their cell surface ephrin ligands to be one of the most prevalent and complex cell-cell communication systems; this system guides cell positioning and orchestrates tissue patterning in multicellular organisms by coordinating synchronised cell-cell adhesion or segregation of interacting cells. The expression of many Eph and ephrin family members together with their embryonic patterning functions often re-emerge during oncogenesis and have generated considerable interest as targets for anticancer therapies. The first generation of monoclonal antibodies, kinase inhibitors, and vaccines suggests considerable promise in preclinical and early clinical development, but there is little doubt that successful clinical use will rely on a comprehensive understanding of the complex and sometimes puzzling activities of Eph receptors during tumor progression.
Insights
Eph receptors and ephrin ligands are key to cell communication and tissue development. Their re-emergence in cancer offers potential anticancer therapy targets, but requires deeper understanding of their tumor progression roles.
Area of Science:
- Cellular and Molecular Biology
- Developmental Biology
- Oncology
Background:
- Eph receptors and ephrin ligands form a prevalent cell-cell communication system.
- This system is crucial for guiding cell positioning and tissue patterning in multicellular organisms.
- Their functions in embryonic development are often reactivated during oncogenesis.
Purpose of the Study:
- To explore the role of Eph receptors and ephrin ligands in oncogenesis.
- To evaluate their potential as targets for anticancer therapies.
- To understand the complex activities of Eph receptors during tumor progression.
Main Methods:
- Review of extensive research over the past 15 years.
- Analysis of preclinical and early clinical development data.
- Examination of the expression patterns of Eph and ephrin family members in cancer.
Main Results:
- Eph/ephrin signaling is implicated in coordinating cell adhesion and segregation.
- Re-emerged embryonic patterning functions of Eph/ephrin are observed in cancer.
- First-generation therapies (antibodies, inhibitors, vaccines) show preclinical promise.
Conclusions:
- Eph receptors and ephrin ligands are critical regulators of cell communication and tissue development.
- Their reactivation in cancer presents promising therapeutic opportunities.
- Comprehensive understanding of Eph receptor activity in tumors is essential for successful clinical application.
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