Inhibition of Eph/ephrin interaction with the small molecule UniPR500 improves glucose tolerance in healthy and insulin-resistant mice.

Targeting Eph/ephrin system in cancer therapy.

The clinical success of conventional and targeted therapies is compromised by the low response rates and development of therapeutic resistance. Dysregulated Eph-ephrin signaling has emerged as a critical factor in mediating resistance to therapeutics and radiation in human malignancies. Eph receptors belong to superfamily of receptor protein tyrosine kinases that interact with their membrane-anchored ligands, ephrins, to regulate a variety of processes under physiological and pathological conditions including cancer. This book chapter sheds light on the functional role of Eph-ephrins in tumor development, and progression and how their aberrant expression contributes toward therapeutic and radiation resistance. The potential of targeting this gene family to combat tumor resistance and enhance therapeutic sensitivity with an overview of the available agents currently in preclinical or clinical phase is also discussed.

Eph/ephrin family proteins and therapeutic resistance

Circulating tumor cell analysis in a first-in-human phase I study of sEphB4-HSA, an inhibitor of EphrinB2-EphB4 signaling

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Circulating tumor cell analysis in a first-in-human phase I study of sEphB4-HSA, an inhibitor of EphrinB2-EphB4 signaling