(415) Development of an EZH2 PROTAC-Nanoparticle targeting Breast Cancer Brain Metastases

Enhancer of zeste homolog 2 (EZH2), a histone methyltransferase, promotes metastases and is overexpressed in triple negative breast cancer brain metastases [1]. PROTACs (proteolysis targeting chimeras) are a novel drug class that induces selective protein degradation and have been shown to be more efficacious compared to current EZH2 inhibitors [2]. However, poor pharmacokinetics limit the translational potential for PROTACs, underscoring the need for improved delivery strategies to cross the blood brain barrier.