Pharmacological Targeting of EphA2: Advancing Precision Therapeutics in Cancer Treatment
DOI:
https://doi.org/10.62382/twc07y24Keywords:
EphA2 receptor, Antineoplastic agents, Immunotherapy, Targeted drug delivery systems, Drug resistanceAbstract
EphA2, an oncogenic receptor tyrosine kinase overexpressed in various malignancies, represents a compelling therapeutic target in oncology. The role of this factor in the growth of tumors, angiogenesis, and cancer metastasis has prompted the emergence of pharmacological interventions, including small-molecule inhibitors, therapeutic monoclonal antibodies, antibody-drug conjugates (ADCs), and novel modalities like proteolysis-targeting chimeras (PROTACs). While preclinical studies have demonstrated potent anticancer effects, clinical translation remains challenging due to tumor heterogeneity, suboptimal pharmacokinetics, and toxicity profiles. Current strategies focus on improving drug delivery using EphA2-targeted nanoparticles and bicycle toxin conjugates, which enhance specificity and reduce off-target effects. Immune-based approaches, such as EphA2-specific CAR-T cells and dendritic cell vaccines, are being explored for synergistic combination therapies to overcome immune resistance. Despite limited success in trials, ongoing innovations in delivery systems and biomarker development aims to address these barriers. This review emphasizes the pharmacological potential of EphA2-targeted therapies and their integration into precision oncology, highlighting critical challenges and emerging solutions for advancing these agents into clinical practice.
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