The role of Eph receptors in cancer and how to target them : novel approaches in cancer treatment

INTRODUCTION: Erythropoietin-producing human hepatocellular (Eph) receptors are among the largest family of tyrosine kinases that are divided into two classes: EphA and EphB receptors. Over the past two decades, their role in cancer has become more evident.

AREAS COVERED: There is a need for new anticancer treatments and more insight in the emerging role of Eph receptors in cancer. Molecular mechanisms underlying the pro-tumorigenic effects of Eph receptors could be exploited for future therapeutic strategies. This review describes the variability in expression levels and different effects on oncogenic and tumor suppressive downstream signaling of Eph receptors in various cancer types, and the small molecules, antibodies and peptides that target these receptors.

EXPERT OPINION: The complexity of Eph signaling is a challenge for the definition of clear targets for cancer treatment. Nevertheless, numerous drugs that target EphA2 and EphB4 are currently in clinical trials. However, some Eph targeted drugs also inhibit other tyrosine kinases, so it is unclear to what extent the targeting of Eph receptors contributes to their efficacy. Future research is warranted for an improved understanding of the full network in which Eph receptors function. This will be critical for the improvement of the anticancer effects of drugs that target the Eph receptors.

Medienart:

E-Artikel

Erscheinungsjahr:

2020

Erschienen:

2020

Enthalten in:

Zur Gesamtaufnahme - volume:29

Enthalten in:

Expert opinion on investigational drugs - 29(2020), 6 vom: 03. Juni, Seite 567-582

Sprache:

Englisch

Beteiligte Personen:

Buckens, Oscar J [VerfasserIn]
El Hassouni, Btissame [VerfasserIn]
Giovannetti, Elisa [VerfasserIn]
Peters, Godefridus J [VerfasserIn]

Links:

Volltext

Themen:

Anti-cancer drugs
Antineoplastic Agents
Cancer
EC 2.7.10.1
Eph receptors
Expression levels
Journal Article
Mechanisms
Protein Kinase Inhibitors
Receptor tyrosine kinases
Receptors, Eph Family
Review

Anmerkungen:

Date Completed 27.01.2021

Date Revised 16.04.2022

published: Print-Electronic

Citation Status MEDLINE

doi:

10.1080/13543784.2020.1762566

funding:

Förderinstitution / Projekttitel:

PPN (Katalog-ID):

NLM309320224