Target intelligence / Profile preview

Ephrin-A1 (EFNA1)

Target
EFNA1
Molecular classification
Ephrin ligand, Ligand (protein), Glycosylphosphatidylinositol (GPI)-anchored protein, Receptor ligand, Other (developmental signaling protein)
01

Overview

Ephrin-A1 (EFNA1) is a glycosylphosphatidylinositol (GPI)-anchored cell surface ligand for Eph receptor tyrosine kinases, especially members of the EphA subclass such as EPHA2, EPHA4, EPHA5, EPHA6, and EPHA7[1][2]. It is a member of the ephrin family, which, with Eph receptors, constitutes the largest subfamily of receptor tyrosine kinases. Ephrin-A1 plays a major role in contact-mediated bidirectional signaling that governs cell migration, adhesion, repulsion, and tissue boundary formation during embryonic development, neuronal patterning, angiogenesis, and erythropoiesis. Ephrin-A1 critically regulates tumor cell behavior, suppresses oncogenic signaling by driving EPHA2 internalization and degradation, inhibits glioma tumorigenesis, and promotes neovascularization in tumors, making it relevant in cancer biology. Ephrin-A1 is encoded by the EFNA1 gene, with multiple known isoforms and numerous aliases, and is implicated in various pathologies, notably gastric cancer and hepatocellular carcinoma[1][2].

Other names
Tumor necrosis factor alpha-induced protein 4TNFAIP4EPLG1LERK1LERK-1ECKLGGMANB61EFL1Ephrin A1Ephrin-A1EPH-related receptor tyrosine kinase ligand 1Immediate early response protein B61ligand of eph-related kinase 1
02

Mechanism of action

Inhibitors or agonists modulate cell migration, adhesion, and angiogenesis by targeting EFNA1 interaction with Eph receptors (especially EPHA2), resulting in altered receptor phosphorylation, internalization, and downstream signaling events (PI3K/Rac1, FAK, etc.)[1][2].

03

Biological functions

Signal transductionCell migrationCell adhesionCell repulsionAngiogenesisNeuronal developmentRegulation of cell morphologyErythropoiesisTumor neovascularization
04

Disease associations

CancerInflammationNeurodevelopmental disorderCardiovascular disease
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Safety considerations

Disruption of EFNA1-Eph signaling may affect vascular development and tissue homeostasis; potential risk of unintended effects on neuronal and vascular systems if therapeutically targeted[1][2]
06

Biomarkers

Overexpression in certain cancers (e.g., gastric cancer, hepatocellular carcinoma) is associated with disease state and prognosis; may serve as a biomarker for tumor angiogenesis and metastatic potential[1]

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