Targeting EphA2 in cancer

J Hematol Oncol. 2020 Aug 18;13(1):114. doi: 10.1186/s13045-020-00944-9.

Abstract

Eph receptors and the corresponding Eph receptor-interacting (ephrin) ligands jointly constitute a critical cell signaling network that has multiple functions. The tyrosine kinase EphA2, which belongs to the family of Eph receptors, is highly produced in tumor tissues, while found at relatively low levels in most normal adult tissues, indicating its potential application in cancer treatment. After 30 years of investigation, a large amount of data regarding EphA2 functions have been compiled. Meanwhile, several compounds targeting EphA2 have been evaluated and tested in clinical studies, albeit with limited clinical success. The present review briefly describes the contribution of EphA2-ephrin A1 signaling axis to carcinogenesis. In addition, the roles of EphA2 in resistance to molecular-targeted agents were examined. In particular, we focused on EphA2's potential as a target for cancer treatment to provide insights into the application of EphA2 targeting in anticancer strategies. Overall, EphA2 represents a potential target for treating malignant tumors.

Keywords: Cancer; EphA2 receptor; Ephrin A1; Target; Therapy.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / therapeutic use*
  • Cancer Vaccines
  • Clinical Trials as Topic
  • Combined Modality Therapy
  • Dendritic Cells / immunology
  • Drug Delivery Systems
  • Enzyme Induction / drug effects
  • Ephrin-A1 / physiology
  • Ephrin-A2 / antagonists & inhibitors*
  • Ephrin-A2 / physiology
  • Humans
  • Immunoconjugates / therapeutic use
  • Immunoglobulin Fc Fragments / immunology
  • Immunotherapy, Adoptive
  • Mice
  • Mice, Nude
  • Molecular Targeted Therapy*
  • Nanocapsules
  • Neoplasm Proteins / antagonists & inhibitors*
  • Neoplasm Proteins / physiology
  • Neoplasms / drug therapy*
  • Neoplasms / enzymology
  • Neoplasms / therapy
  • Protein Kinase Inhibitors / therapeutic use*
  • RNA Interference
  • RNA, Small Interfering / genetics
  • RNA, Small Interfering / therapeutic use
  • Receptor, EphA2
  • Recombinant Fusion Proteins / metabolism
  • Substrate Specificity
  • Xenograft Model Antitumor Assays

Substances

  • Antineoplastic Agents
  • Cancer Vaccines
  • EFNA1 protein, human
  • EPHA2 protein, human
  • Ephrin-A1
  • Ephrin-A2
  • Immunoconjugates
  • Immunoglobulin Fc Fragments
  • Nanocapsules
  • Neoplasm Proteins
  • Protein Kinase Inhibitors
  • RNA, Small Interfering
  • Recombinant Fusion Proteins
  • Receptor, EphA2