Affinage

EFNA1

Ephrin-A1 · UniProt P20827

Length
205 aa
Mass
23.8 kDa
Annotated
2026-06-09
27 papers in source corpus 12 papers cited in narrative 12 extracted findings
Cross-family judge vs UniProt: Affinage preferred faithfulness: 5/5 claims corpus-supported (100%)

Mechanistic narrative

Synthesis pass · prose summary of the discoveries below

EFNA1 (ephrinA1) is a GPI-anchored ligand for Eph receptor tyrosine kinases, primarily EphA2, and functions as a context-dependent regulator of cell proliferation, invasion, angiogenesis, and inflammatory signaling (PMID:11741747, PMID:8660976). In trans, engagement of EphA2 by soluble or surface EFNA1 drives receptor tyrosine hyperphosphorylation followed by EphA2 downregulation, and concurrently phosphorylates E-cadherin and beta-catenin, an autocrine circuit that overcomes contact inhibition in carcinoma cells (PMID:11741747, PMID:15649254). In cis on the same cell surface, EFNA1 instead lowers EphA2 tyrosine phosphorylation and activates Src/AKT/STAT3 forward signaling to promote tumorigenesis (PMID:39964764), and across multiple tumor types EFNA1 sustains pro-survival and proliferative signaling through AKT/ERK1/2 and through an EphA2–cMYC–cell cycle axis whose disruption activates autophagy (PMID:40578286, PMID:37160815). EFNA1 expression is multiply controlled: transcriptionally by FOSL2-bound super-enhancers (PMID:39964764), by EPAS1/HIF-2α promoter binding (PMID:41941163), and by STAT5/NCOA2 in an angiogenic positive-feedback loop in endothelial cells (PMID:41867368); and post-transcriptionally by miR-200c acting on a 3'UTR SNP site (PMID:23065816) and by the lncRNA GMAN, which sequesters the inhibitory antisense GMAN-AS to license EFNA1 translation and drive invasion and metastasis (PMID:30445010). Beyond ligand–receptor engagement, EFNA1 is shed from epithelial cells by ADAM9 upon TLR5/flagellin stimulation, disrupting EPHA2–EFNA1 trans-binding and triggering ligand-independent inflammatory EPHA2 signaling, defining a pathogen-sensing role (PMID:39991543).

Mechanistic history

Synthesis pass · year-by-year structured walk · 11 steps
  1. 1996 Medium

    Established the molecular identity of EFNA1 as a GPI-anchored Eph receptor ligand, defining the structural class that enables bidirectional Eph signaling.

    Evidence Chromosomal mapping by Southern/FISH and structural classification in human and mouse

    PMID:8660976

    Open questions at the time
    • No functional signaling consequence tested
    • Receptor binding partners not yet defined in this study
  2. 2002 Medium

    Showed that autocrine EFNA1-EphA2 signaling drives EphA2/E-cadherin/beta-catenin phosphorylation and supports 3D growth, linking the ligand to overcoming contact inhibition.

    Evidence Antisense knockdown, EFNA1-Fc stimulation, phospho-western, and 3D spheroid vs monolayer assays in HT29 colon carcinoma cells

    PMID:11741747

    Open questions at the time
    • Mechanism connecting EphA2 to beta-catenin phosphorylation not resolved
    • Single cell line
  3. 2005 Medium

    Demonstrated that trans EFNA1 engagement triggers EphA2 phosphorylation followed by receptor downregulation and growth suppression, establishing a ligand-induced negative-feedback outcome.

    Evidence Soluble ephrinA1-Fc stimulation with protein/phosphorylation/growth readouts in gastric cancer lines

    PMID:15649254

    Open questions at the time
    • Growth-suppressive trans effect contrasts with proliferative roles elsewhere; context determinants unresolved
    • No in vivo confirmation
  4. 2006 Low

    Mapped Efna1 expression alongside Epha1 and Efna3 in early mouse mesoderm, suggesting a developmental migratory/adhesive role.

    Evidence Whole-mount in situ hybridization in early mouse embryos

    PMID:16466970

    Open questions at the time
    • Localization only; no functional consequence demonstrated for EFNA1
    • No loss-of-function phenotype
  5. 2012 Medium

    Identified EFNA1 as a direct miR-200c target whose suppression is modulated by a 3'UTR SNP, adding allele-dependent post-transcriptional control.

    Evidence Allele-specific luciferase reporter assays, genotyping, and tumor qRT-PCR

    PMID:23065816

    Open questions at the time
    • Functional downstream consequence of altered EFNA1 not tested
    • Effect on EphA2 signaling not measured
  6. 2018 High

    Defined a lncRNA-based translational control mechanism where GMAN sequesters GMAN-AS to permit EFNA1 translation, with EFNA1 mediating invasion and metastasis.

    Evidence RNA pulldown/mapping, polysome profiling, CRISPR/RNAi, genetic rescue, and xenograft metastasis in gastric cancer

    PMID:30445010

    Open questions at the time
    • Receptor signaling pathway downstream of EFNA1 in this context not dissected
    • How GMAN-AS blocks translation mechanistically not fully resolved
  7. 2025 Medium

    Revealed a cis EFNA1-EphA2 interaction that lowers EphA2 phosphorylation and activates Src/AKT/STAT3, plus super-enhancer/FOSL2 transcriptional control, distinguishing cis from trans signaling outcomes.

    Evidence Epigenomic profiling, FOSL2 knockdown with ChIP/luciferase, EFNA1 knockdown, pathway inhibitors, in vivo cervical cancer models

    PMID:39964764

    Open questions at the time
    • Molecular basis of cis vs trans switch unresolved
    • Single lab
  8. 2025 High

    Established ADAM9-mediated EFNA1 shedding downstream of TLR5/flagellin as a pathogen-sensing trigger of ligand-independent inflammatory EPHA2 signaling.

    Evidence EFNA1 cleavage assay, ADAM9 and EPHA2 perturbation, forced shedding, and in vivo flagellin/P. aeruginosa challenge

    PMID:39991543

    Open questions at the time
    • How loss of trans-binding mechanistically activates EPHA2 not fully defined
    • Cleavage site not mapped
  9. 2025 Medium

    Showed EFNA1 promotes pro-survival AKT/ERK1/2 signaling and proliferation in HNSCC reversible by EFNA1 antibody, and placed EFNA1 upstream of an EPHA2-cMYC-cell cycle/autophagy axis in ESCC.

    Evidence EFNA1/EPHA2 knockdown and overexpression, proliferation/colony/cell-cycle assays, autophagy imaging, and western blot

    PMID:37160815 PMID:40578286

    Open questions at the time
    • Direct link from EFNA1 to cMYC regulation not mechanistically traced
    • Single lab per tumor type
  10. 2025 Medium

    Identified an IL-15/STAT5/NCOA2-driven EFNA1 positive-feedback loop promoting endothelial angiogenesis in diabetic retinopathy.

    Evidence STAT5 inhibition, NCOA2/EFNA1 knockdown, promoter binding assay, high-glucose co-culture, and angiogenesis assays

    PMID:41867368

    Open questions at the time
    • Mechanism of EFNA1 feedback onto NCOA2 not defined
    • Eph receptor involvement in angiogenic effect not tested
  11. 2026 Medium

    Defined EFNA1 as the critical EPAS1/HIF-2α-driven mediator of diclofenac's COX-independent anti-tumor activity in breast cancer.

    Evidence RNA-seq, EFNA1 promoter luciferase assay, overexpression rescue, and xenograft validation

    PMID:41941163

    Open questions at the time
    • Downstream signaling through which EFNA1 mediates the effect not specified
    • Single lab

Open questions

Synthesis pass · forward-looking unresolved questions
  • The determinants that switch EFNA1 between growth-suppressive trans signaling and proliferative cis/forward signaling, and the signaling output of EFNA1 in non-tumor developmental and vascular contexts, remain unresolved.
  • No unified model of cis vs trans signaling control
  • No structural model of cis EFNA1-EphA2 engagement
  • Developmental loss-of-function phenotype uncharacterized

Mechanism profile

Synthesis pass · controlled-vocabulary classification · explore literature graph →
Molecular activity
GO:0048018 receptor ligand activity 3 GO:0098772 molecular function regulator activity 3
Localization
GO:0005886 plasma membrane 3
Pathway
R-HSA-162582 Signal Transduction 3 R-HSA-1643685 Disease 3 R-HSA-168256 Immune System 1
Partners

Evidence

Reading pass · 12 per-paper findings extracted from the source corpus
Year Finding Method Journal Conf PMIDs
2002 EFNA1 (ephrinA1) is a GPI-anchored ligand that preferentially binds to the receptor tyrosine kinase EphA2; activation of EphA2 by EFNA1 in HT29 colon carcinoma cells leads to tyrosine hyperphosphorylation of EphA2, E-cadherin, and beta-catenin, and reduced EFNA1 expression slows three-dimensional spheroid growth but not monolayer growth, implicating autocrine EFNA1-EphA2 signaling in overcoming contact inhibition. Antisense transfection to reduce EFNA1 expression, EFNA1-Fc stimulation, western blot for phosphorylation of EphA2/E-cadherin/beta-catenin, 3D spheroid vs monolayer growth assay Cancer letters Medium 11741747
2005 Stimulation of EPHA2-expressing gastric cancer cell lines with soluble ephrinA1-Fc (EFNA1) leads to decreased EphA2 protein expression, increased EphA2 phosphorylation, and inhibition of cell growth upon repetitive stimulation, demonstrating that EFNA1 engagement of EphA2 triggers receptor downregulation and growth suppression. Stimulation with soluble ephrinA1-Fc, western blotting, northern blotting, RT-PCR, cell growth assay Cancer science Medium 15649254
2006 Efna1 (ephrinA1) is expressed in overlapping and complementary domains with its receptor Epha1 and paralog Efna3 in the primitive streak and posterior paraxial mesoderm during early mouse development, consistent with bidirectional Eph-ephrin signaling regulating cell migratory and adhesive behavior in this context. Whole-mount in situ hybridization in early mouse embryos Gene expression patterns : GEP Low 16466970
2018 The lncRNA GMAN promotes translation of EFNA1 mRNA into protein by competitively binding GMAN-AS (an antisense RNA complementary to EFNA1 mRNA), thereby preventing GMAN-AS from suppressing EFNA1 translation; elevated EFNA1 protein in turn promotes gastric cancer cell invasion and metastasis, as demonstrated by rescue of GMAN-knockdown invasive phenotype by ectopic EFNA1 expression. RNA pulldown and mapping assays, polysome profiling, siRNA/shRNA knockdown, CRISPR/Cas9 knockout, overexpression, Transwell invasion assay, mouse xenograft metastasis model, immunoblot Gastroenterology High 30445010
2012 A SNP (rs12904, G>A) in the 3'UTR of EFNA1 alters the binding site for hsa-miR-200c; luciferase assays confirmed EFNA1 as a direct target of miR-200c and showed that the G allele reduces miR-200c-mediated suppression of EFNA1 expression, while the A allele permits stronger miR-200c-mediated repression. Luciferase reporter assay, case-control genotyping, qRT-PCR on patient tumor tissues Molecular carcinogenesis Medium 23065816
2025 EFNA1 cis-interacts with its receptor EphA2 on the same cell surface in cervical cancer cells, leading to decreased EphA2 tyrosine phosphorylation and subsequent activation of the Src/AKT/STAT3 forward signaling pathway; inhibition of this pathway with specific inhibitors attenuated tumorigenic capacity, and EFNA1 expression is driven by a tumor-specific super-enhancer containing FOSL2 binding sites whose knockdown suppresses both H3K27ac enrichment and luciferase activity at the SE region. Integrated epigenomic/transcriptomic profiling, FOSL2 knockdown with luciferase and ChIP assays, EFNA1 knockdown, specific pathway inhibitors, in vitro and in vivo tumor models The Journal of clinical investigation Medium 39964764
2025 Flagellin-induced TLR5 signaling causes ADAM9 metalloproteinase-dependent cleavage/shedding of EFNA1 from airway epithelial cells, disrupting EPHA2-EFNA1 trans-binding and activating ligand-independent EPHA2 signaling; EPHA2 ablation reduced inflammatory responses to flagellin and Pseudomonas aeruginosa, and forced EFNA1 shedding alone (without PAMPs) was sufficient to stimulate inflammatory responses, establishing EFNA1 shedding as a pathogen-sensing mechanism. EFNA1 cleavage assay, ADAM9 inhibition/knockdown, EPHA2 knockout, in vitro and in vivo (mouse) flagellin/P. aeruginosa challenge, inflammatory cytokine readout iScience High 39991543
2025 In HNSCC cells, EFNA1 knockdown reduces activity of the AKT/ERK1/2 signaling pathway, and EFNA1 overexpression increases cell proliferation that is reversible by EFNA1 antibody treatment, establishing that EFNA1 promotes survival signaling through AKT/ERK1/2. EFNA1 knockdown and overexpression, western blotting for EphA2pS898/EphA2/EFNA1/AKT/ERK1/2, cell proliferation and apoptosis assays Biochemical and biophysical research communications Medium 40578286
2025 In diabetic retinopathy, IL-15 secreted by monocytes/macrophages activates STAT5 in endothelial cells, which binds the EFNA1 promoter in an NCOA2-dependent manner to induce EFNA1 expression and promote angiogenesis; EFNA1 and NCOA2 form a positive feedback loop where knockdown of either gene reduces expression of the other. STAT5 inhibition, NCOA2 knockdown, EFNA1 knockdown, ChIP-implied STAT5 promoter binding assay, co-culture with THP-1 under high-glucose conditions, angiogenesis assays Molecular vision Medium 41867368
2026 Diclofenac reduces EFNA1 expression in breast cancer cells by impairing EPAS1 (HIF-2α) binding to the EFNA1 promoter region (-1353 to -782); EFNA1 overexpression rescues the anti-tumor effects of diclofenac, establishing EFNA1 as the critical mediator of diclofenac's COX-independent anti-cancer activity. RNA-seq, luciferase reporter assay for EFNA1 promoter, EFNA1 overexpression rescue, qRT-PCR, western blot, xenograft model Current medicinal chemistry Medium 41941163
2025 In esophageal squamous cell carcinoma, EFNA1 knockdown suppresses cMYC expression and its downstream cell cycle genes and activates autophagy; similar effects are seen with knockdown of its receptor EPHA2, placing EFNA1 upstream of the EPHA2-cMYC-cell cycle/autophagy axis. EFNA1 and EPHA2 knockdown, CCK-8 and colony formation assays, wound healing, flow cytometry (cell cycle), transmission electron microscopy (autophagolysosome), western blot Discover oncology Medium 37160815
1996 EFNA1 (LERK-1/EPLG1) encodes a GPI-anchored membrane protein belonging to the LERK family of Eph receptor ligands and is located on human chromosome 1q21-q22; its GPI anchor distinguishes it from transmembrane LERKs and is consistent with bidirectional signaling via Eph receptors. Southern hybridization of somatic cell hybrid DNAs, fluorescence in situ hybridization, interspecific backcross mapping Genomics Medium 8660976

Source papers

Stage 0 corpus · 27 papers · ranked by NIH iCite citations
Year Title Journal Citations PMID
2018 Long Noncoding RNA GMAN, Up-regulated in Gastric Cancer Tissues, Is Associated With Metastasis in Patients and Promotes Translation of Ephrin A1 by Competitively Binding GMAN-AS. Gastroenterology 217 30445010
2005 EPHA2/EFNA1 expression in human gastric cancer. Cancer science 126 15649254
2010 EFNA1 ligand and its receptor EphA2: potential biomarkers for hepatocellular carcinoma. International journal of cancer 73 19642143
2002 Reduced expression of EphrinA1 (EFNA1) inhibits three-dimensional growth of HT29 colon carcinoma cells. Cancer letters 45 11741747
2019 Long noncoding RNA GMAN promotes hepatocellular carcinoma progression by interacting with eIF4B. Cancer letters 39 31875526
2020 Role of EFNA1 in tumorigenesis and prospects for cancer therapy. Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie 35 32745910
2012 G-A variant in miR-200c binding site of EFNA1 alters susceptibility to gastric cancer. Molecular carcinogenesis 24 23065816
2025 Super-enhancer-driven EFNA1 fuels tumor progression in cervical cancer via the FOSL2-Src/AKT/STAT3 axis. The Journal of clinical investigation 16 39964764
2006 Expression analysis of the Epha1 receptor tyrosine kinase and its high-affinity ligands Efna1 and Efna3 during early mouse development. Gene expression patterns : GEP 16 16466970
2022 Nintedanib Alleviates Experimental Colitis by Inhibiting CEBPB/PCK1 and CEBPB/EFNA1 Pathways. Frontiers in pharmacology 15 35910380
1996 The genes encoding the eph-related receptor tyrosine kinase ligands LERK-1 (EPLG1, Epl1), LERK-3 (EPLG3, Epl3), and LERK-4 (EPLG4, Epl4) are clustered on human chromosome 1 and mouse chromosome 3. Genomics 13 8660976
2013 rs12904 polymorphism in the 3'UTR of EFNA1 is associated with colorectal cancer susceptibility in a Chinese population. Asian Pacific journal of cancer prevention : APJCP 12 24175772
2022 EFNA1 in gastrointestinal cancer: Expression, regulation and clinical significance. World journal of gastrointestinal oncology 11 35646281
2023 Targeting EFNA1 suppresses tumor progression via the cMYC-modulated cell cycle and autophagy in esophageal squamous cell carcinoma. Discover oncology 10 37160815
2024 Combined detection of serum EFNA1 and MMP13 as diagnostic biomarker for gastric cancer. Scientific reports 6 38987376
2025 Integrative single-cell and exosomal multi-omics uncovers SCNN1A and EFNA1 as non-invasive biomarkers and drivers of ovarian cancer metastasis. Frontiers in immunology 5 40787466
2025 EFNA1 promotes the tumorigenesis and metastasis of cervical cancer by phosphorylation pathway and epithelial-mesenchymal transition. Acta histochemica 3 39999525
2026 Integrative Multiscale Analysis Reveals EFNA1-Driven Immune Remodeling Promotes Colorectal Cancer Lymph Node Metastasis. Human mutation 2 41542227
2025 Perturbation of EPHA2 and EFNA1 trans binding amplifies inflammatory response in airway epithelial cells. iScience 2 39991543
2026 ScRNA-Seq Deciphers an Autocrine EFNA1-EPHA1 Loop That Reprograms the Microenvironment in Hepatocellular Carcinoma. Journal of hepatocellular carcinoma 0 41847220
2026 Repurposing Diclofenac as an Anticancer Agent: Suppression of Breast Cancer and Progression through EPAS1-EFNA1 Regulation. Current medicinal chemistry 0 41941163
2026 Cross-species single-cell and spatial transcriptomic mapping reveals EFNA1-EPHA4-mediated stem-like epithelial-macrophage crosstalk driving colorectal cancer progression. Cancer letters 0 41966512
2025 Relative Quantitation of EFNA1 Expression in Mouse Heart Tissue Histologic Sections Using MALDI-MSI. International journal of molecular sciences 0 40003866
2025 Genetic Variants in RASSF1 (rs2073498), SERPINE1 (rs1799889), and EFNA1 (rs12904) Are Associated with Susceptibility in Mexican Patients with Colorectal Cancer: Clinical Associations and Their Analysis In Silico. Genes 0 40004552
2025 Molecular mechanism of secretory protein EFNA1 in HNSCC and its value in early screening. Biochemical and biophysical research communications 0 40578286
2025 Cancer genome profiling of prostate cancer identifies a patient with a novel EFNA1-NTRK1 fusion gene. International cancer conference journal 0 40625757
2025 Monocyte/macrophage-derived IL-15 activates STAT5 to trigger the EFNA1/NCOA2-positive feedback loop, facilitating retinal angiogenesis in high-glucose environments. Molecular vision 0 41867368

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