EPHA2 (EPH receptor A2)

This study examined the role of EphA2 in cell cycle progression in Adriamycin (ADR)-treated cells...EphA2 upregulation following DNA damage may be pro-tumorigenic by maintaining G2 arrest to keep DNA damage at tolerable levels. These findings provide a rationale for combining EphA2 inhibition with DNA-damaging agents in certain cancer types.

We utilized HeLa S3-derived HeLa S3/v-Src cells, which allow inducible v-Src expression upon doxycycline (Dox) treatment...However, as Src signaling intensifies, it overrides the counteracting effect of EphA2, resulting in cell rounding and detachment. The balance between Src and EphA2 may act as a key regulator of cellular adhesion dynamics.

Moreover, in HGSOC patient-derived xenograft (PDX) models, brigatinib and PARPi combination therapy induced tumor regression and improved overall survival compared with PARPi alone, particularly in models with high FAK and EPHA2. These findings support dual targeting of FAK and EPHA2 as a strategy to achieve effective and durable PARPi responses and identify a promising biomarker-based combinatorial approach using brigatinib and PARPi for HGSOC, particularly the subset characterized by high FAK and EPHA2.

Analysis of the complexes showed success in selective disruption: the mutant gp42-HLA class II complex showed stability with a root mean square deviation (RMSD) of 2.29 ± 0.18 Å and mean root mean square fluctuation (RMSF) of 1.31 Å when compared to the mutant gH/gL-EphA2 interaction, which showed significant instability with an RMSD of 4.77 ± 0.22 Å and mean RMSF of 2.11 Å, with 46% of residues exceeding the 2.0 Å flexibility. In summation, this paper intends to lay an initial computational framework for a B cell-selective oncolytic EBV variant that eliminates epithelial off-target effects while maintaining therapeutic efficacy against leukemic B cells.

These findings indicate that EphA2 overexpression and its S897 phosphorylation play a critical role in NPC radioresistance. The A11 peptide emerges as a promising therapeutic agent by degrading EphA2 and blocking its phosphorylation, offering a potential strategy to enhance radiotherapy efficacy and improve outcomes in NPC patients.

miR-302a-3p significantly mitigated inflammatory responses and suppressed cell apoptosis by directly targeting and downregulating EPHA2 expression, thereby delaying the progression of IDD.

P1/2, N=288, Active, not recruiting, BicycleTx Limited | Recruiting --> Active, not recruiting | Trial completion date: Oct 2025 --> Jul 2027 | Trial primary completion date: Oct 2025 --> Jul 2026

The dualistic nature of Eph/ephrin signaling underscores its translational promise as both a biomarker framework and a precision-guided therapeutic target. Combinatorial receptor-ligand modulation strategies may advance the treatment of central nervous system malignancies by exploiting the context-dependent roles of Eph/ephrin interactions.

Superior imaging performance was observed in both orthotopic colorectal cancer and liver metastasis models. Owing to its high tumor-to-background ratio (TBR>2.0) and prolonged imaging window, EPH-3-DBS holds significant potential for application in fluorescence-guided surgery.

Indeed, an EPHA2 kinase-inactive mutant, but not EPHA2 wild-type, induced proliferative masses consistent with well differentiated cholangiocarcinoma in a validated mouse model of cholangiocarcinogenesis. Thus, EPHA2 has the attributes of a driver gene with tumor suppressor activity in biliary tract cancers.

This study identifies CEMJ4 as a promising peptide ligand for tumor-targeted radionuclide delivery and emphasizes the clinical potential of radionuclide therapy combined with immunotherapy in theranostics to enhance therapeutic precision and efficacy.

Our findings demonstrate that anti-EphA2-Mb is an excellent targeting molecule, and [64Cu]Cu-NOTA-anti-EphA2-Mb is a promising immunoPET agent with potential for use for other theranostic applications.