Target intelligence / Profile preview

Tyrosine-protein kinase EphB4 (EphB4)

Target
EphB4
Molecular classification
Receptor tyrosine kinase, Enzyme, Receptor
01

Overview

Tyrosine-protein kinase EphB4 is a member of the largest subgroup of receptor tyrosine kinases, distinguished by mediating contact-dependent signaling with ephrin-B family ligands, especially ephrin-B2. Activation of EphB4 triggers forward and reverse signaling events that guide cell adhesion, migration, vascular development, angiogenesis, and heart morphogenesis. EphB4 is highly expressed in various cancers and is linked to tumor cell survival, migration, invasiveness, and the regulation of pathological angiogenesis. Targeted therapies include peptides, antibodies, and small-molecule inhibitors designed to block the EphB4-ephrin-B2 interaction or kinase activity, though care must be taken to avoid detrimental impacts on normal tissue functions

Other names
EPH receptor B4Ephrin type-B receptor 4HTKMYK1TYRO11HFASDCMAVM2LMPHM7
02

Mechanism of action

Inhibition of EphB4-ephrin-B2 interaction (peptides, antibodies, small molecules); Kinase inhibition (ATP-competitive inhibitors); Induction of receptor degradation (specific antibody, e.g., MAb131)

03

Biological functions

Signal transductionCell adhesionCell migrationVascular developmentAngiogenesisHeart morphogenesisCell proliferation
04

Disease associations

Cancer (numerous types: breast, colon, bladder, prostate, ovarian, melanoma)Cardiovascular disease (e.g., arteriovenous malformations)Other (e.g., lymphatic malformations)
05

Safety considerations

Targeting EphB4 may affect normal vascular and heart development or functionPotential off-target kinase inhibition with low selectivity small moleculesPossible interference with normal cell adhesion, migration, and angiogenesis
06

Interacting drugs

TNYL-RAW peptide (antagonist)

4 more in the full profile.

07

Biomarkers

EphB4 expression level for patient selection in oncology (e.g., breast, colon, mesothelioma)EphB4-ephrin-B2 signaling activity (used in some experimental settings)

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