Related Experiment Video
Updated: May 4, 2026

Co-immunoprecipitation Assay for Studying Functional Interactions Between Receptors and Enzymes
Published on: September 28, 2018
Therapeutic targeting of EPH receptors and their ligands
Andrew W Boyd1, Perry F Bartlett2, Martin Lackmann3
1Leukaemia Foundation Research Laboratory, Queensland Institute of Medical Research, 300 Herston Road, Brisbane, Queensland 4029, Australia.
Abstract:
Critical roles for EPH receptor (EPH)-ephrin signalling in a range of chronic and regenerative diseases are increasingly being recognized. In particular, the complex roles of EPHs and ephrins in tumour growth and progression, and in nerve injury and regeneration have been studied extensively. This has led to considerable progress in developing strategies for their therapeutic targeting, with some anticancer agents already in clinical trials. Promising leads for non-malignant diseases are also emerging, with compelling preclinical data encouraging clinical development. We discuss this rapidly developing area of drug discovery, highlighting the associated challenges and limitations.
Insights
EPH receptor-ephrin signaling plays critical roles in chronic diseases and nerve regeneration. Therapeutic targeting shows promise for cancer and non-malignant conditions, with ongoing clinical development.
Area of Science:
- Molecular biology
- Cell signaling
- Drug discovery
Background:
- EPH receptor (EPH)-ephrin signaling is crucial in various chronic and regenerative diseases.
- The roles of EPHs and ephrins in tumor progression and nerve injury are extensively studied.
- This signaling pathway is a key focus in understanding disease mechanisms.
Purpose of the Study:
- To review the critical roles of EPH-ephrin signaling in disease.
- To discuss therapeutic targeting strategies for EPH-ephrin pathways.
- To highlight progress and challenges in drug discovery for these targets.
Main Methods:
- Literature review of EPH-ephrin signaling in disease.
- Analysis of preclinical and clinical data for therapeutic agents.
- Discussion of drug development challenges and limitations.
Main Results:
- EPH-ephrin signaling is implicated in tumor growth and nerve regeneration.
- Several anticancer agents targeting EPHs are in clinical trials.
- Preclinical data supports the development of therapies for non-malignant diseases.
Conclusions:
- EPH-ephrin signaling represents a promising area for therapeutic intervention.
- Significant progress has been made in developing targeted therapies.
- Further research and development are needed to overcome challenges in clinical application.
Related Concept Videos
Role of Ephrin-Eph Signalling in Intestinal Stem Cell Renewal
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:
Mitogens and the Cell Cycle
Targeted Cancer Therapies
There are several types of targeted therapies against...
Targeted Cancer Therapies
Targets for Drug Action: Overview
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...

