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Pharmacological screening of a new class of NSD1 inhibitor

Jia-Ray Yu, PhD

Virginia Polytechnic Institute

Diffuse Intrinsic Pontine Glioma (DIPG) is one of the most aggressive types of pediatric brain cancer. It mainly affects children from the age of 5-12 with little chance of survival. DIPG originates from the pons in the brainstem and, therefore, cannot be removed by surgery. Currently, there is no effective therapy to treat DIPG, and the prognosis for these children is very poor. Therefore, there is a crucial need for new therapeutic interventions for DIPG.  Dr. Jia-Ray Yu, an Assistant Professor at Virginia Polytechnic Institute and State University, recently showed that experimental removal of the NSD1 gene (a methyltransferase) significantly reduced the growth of DIPG tumors in animal models suggesting that this might be a new and novel target for drug development.  Interestingly, the NSD1 gene is also elevated in pediatric AML, so novel inhibitors might find multiple uses. Using state-of-the-art technology and a grant from CURE Childhood Cancer, Dr. Yu’s laboratory will conduct a high-volume screen of potential inhibitors focusing on a novel feature of NSD1 that has not been previously targeted.