BioCentury

Entinostat-derived LSD1 and HDAC dual inhibitor for pediatric glioma

November 21, 2019 9:05 PM UTC

INDICATION: Brain cancer

An HDAC and LSD1 inhibitor could treat diffuse intrinsic pontine glioma, a subtype of pediatric brain cancer. A dual HDAC and LSD1 inhibitor tool compound, derived from the HDAC inhibitor entinostat and a tranylcypromine analog that inhibits LSD1, reduced the viability of five human diffuse intrinsic pontine glioma cell lines compared with entinostat or the tranylcypromine analog alone. In xenograft mouse models of the disease, the inhibitor reduced tumor volume by 28-80%...