Article
Re-programing Chromatin with a Bifunctional LSD1/HDAC Inhibitor Induces Therapeutic Differentiation in DIPG.
Cancer cell - 11 Nov 2019
Anastas Jamie N, Zee Barry M, Kalin Jay H, Kim Mirhee, Guo Robyn, Alexandrescu Sanda, Blanco Mario Andres, Giera Stefanie, Gillespie Shawn M, Das Jayanta, Wu Muzhou, Nocco Sarah, Bonal Dennis M, Nguyen Quang-De, Suva Mario L, Bernstein Bradley E, Alani Rhoda, Golub Todd R, Cole Philip A, Filbin Mariella G, Shi Yang
Abstract excerpt
H3K27M mutations resulting in epigenetic dysfunction are frequently observed in diffuse intrinsic pontine glioma (DIPGs), an incurable pediatric cancer. We conduct a CRISPR screen revealing that knockout of KDM1A encoding lysine-specific demethylase 1 (LSD1) sensitizes DIPG cells to histone deacetylase (HDAC) inhibitors. Consistently, Corin, a bifunctional inhibitor of HDACs and LSD1, potently inhibits DIPG...
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