Target intelligence / Profile preview

Ephrin type-A receptor 10 (EPHA10)

Target
EPHA10
Molecular classification
Receptor tyrosine kinase (pseudokinase subclass; lacks catalytic kinase activity), Receptor, Type I membrane protein
01

Overview

Ephrin type-A receptor 10 (EPHA10) is a member of the largest family of receptor tyrosine kinases (RTKs), known as the Eph receptors[1]. Unlike most Eph family members, EPHA10 is a classified pseudokinase: although it possesses typical receptor architecture (extracellular domain, juxtamembrane region, pseudokinase domain, SAM domain, and PDZ-binding motif), it lacks key residues required for kinase activity and is considered "kinase-dead"[1][4]. EPHA10 contributes to cell–cell communication in developmental patterning and epithelial homeostasis through non-catalytic signaling mechanisms, largely by interacting with other Eph receptors and adaptors[1][2]. Overexpression and differential isoform localization of EPHA10 are associated with increased cell proliferation, disrupted cell–cell adhesion, epithelial–mesenchymal transition, and metastasis, notably in breast and other epithelial cancers[2][3]. Though lacking intrinsic kinase activity, EPHA10 can bind ATP and small-molecule kinase inhibitors, suggesting a potential for therapeutic targeting to modulate oncogenic pathways[1]. Its role as both a biomarker of cancer aggressiveness and a putative target makes it a candidate for further clinical investigation[2][3].

Other names
EPHA10Ephrin type-A receptor 10FLJ16103FLJ33655DFNA88EphA10s proteinephrin type-A receptor 10
02

Mechanism of action

ATP-competitive inhibition at the pseudokinase domain (non-catalytic binding). Potential pharmacological targeting to disrupt non-canonical oncogenic signaling.

03

Biological functions

Cell–cell communicationSignal transduction (through non-catalytic mechanisms)Regulation of epithelial–mesenchymal transitionCell adhesionCell proliferation
04

Disease associations

Cancer (especially breast, prostate, colon, and oral squamous cell carcinoma)Tumor metastasis (particularly lymph node metastasis in breast cancer)
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Safety considerations

Pseudokinase targeting may have off-target effects due to non-catalytic signaling complexityFunctional redundancy with other Eph receptors can complicate targeted therapy; compensatory mechanisms may reduce efficacy
06

Interacting drugs

Dasatinib

1 more in the full profile.

07

Biomarkers

EPHA10 overexpression is a clinical biomarker for disease progression, lymph node metastasis, and tumor stage in cancers such as breast cancerIsoform expression patterns (membrane-bound EphA10s vs. cytoplasmic full-length EphA10) are relevant for predicting invasive/metastatic cancer phenotype

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