Email Address:rui.zhao@cuanschutz.edu

Developing a First-in-class Allosteric Eya2 Tyrosine Phosphatase Inhibitor for Brain Cancer Therapy

This proposal targets the unmet needs in treating medulloblastoma (MB) and glioblastoma (GBM), two challenging brain cancers. MB, the most common malignant brain tumor in children, lacks effective targeted therapies, while GBM, the most aggressive adult primary brain cancer, has a poor prognosis with current treatments. The team discovered that the Tyr phosphatase activity of EYA2 is crucial for tumor progression in both cancers. They developed a first-in-class allosteric inhibitor specific to EYA2’s activity and designed analogs that cross the blood-brain barrier, significantly inhibiting tumor growth in mouse models. Support from SPARK will help finalize the evaluation of these analogs and identify a preclinical candidate for IND-filing studies. Collaborators: Rui Zhao, PhD,  Heide Ford, PhD, and Xiang Wang, PhD