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Targeting receptor tyrosine kinase EphB4 in cancer therapy

Yinnan Chen1, Hongmei Zhang2, Yanmin Zhang3

  • 1School of Molecular Sciences, Arizona State University, Tempe, AZ 85287, USA.

Seminars in Cancer Biology
|October 11, 2017
PubMed

Insights

EphB4 receptor tyrosine kinase plays a dual role in cancer, promoting growth and metastasis. Inhibitors targeting EphB4 show promise as a challenging yet valuable anticancer therapy.

Area of Science:

  • Cell signaling
  • Molecular biology
  • Oncology

Background:

  • Eph receptors and ephrin ligands form a critical cell communication system.
  • Eph receptors exhibit both tumor-suppressing and tumor-promoting roles in cancer.
  • The EphB4 receptor tyrosine kinase is implicated in tumor angiogenesis, growth, and metastasis.

Purpose of the Study:

  • To review the structure and function of the EphB4 receptor.
  • To analyze EphB4's potential as an anticancer therapeutic target.
  • To summarize inhibitors targeting EphB4 kinase activity.

Main Methods:

  • Literature review of studies on EphB4 structure, function, and inhibition.
  • Analysis of EphB4's role in carcinogenesis and therapeutic potential.
  • Summary of preclinical and clinical data on EphB4 inhibitors.

Main Results:

  • EphB4 signaling is crucial in cancer progression.
  • Numerous compounds targeting EphB4 have been developed.
  • Several selective EphB4 inhibitors have advanced to clinical trials.

Conclusions:

  • EphB4 is a significant target in cancer therapy.
  • Targeting EphB4 presents therapeutic opportunities.
  • EphB4 inhibition is a promising, albeit challenging, anticancer strategy.
Keywords:
Cancer therapyDrug targetEphB4 receptorEphrin signalingReceptor tyrosine kinases

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