Invited Speaker; Spatiotemporal delivery of epigenetic and chemotherapeutic nucleoside analogs to pancreatic cancer

Category
Mini Symposia – Cancer Epigenetics, Epigenetic Drugs and Delivery
Year
2014
Authors
Dr. Rajgopal Govindarajan
Institutions
Associate Professor, Pharmaceutical and Biomedical Sciences, University of Georgia, Athens, GA
Summary

Recently, it has been shown that a potent chemical inhibitor of S-adenosylhomocysteine hydrolase, 3-deazaneplanocin A (DZNep), modulates chromatin through indirect (i.e., reducing methyl group availability) inhibition of histone methyltransferases including Enhancer of Zeste Homolog 2 (EZH2). DZNep, a carbocyclic analog of adenosine, depletes cellular levels of the Polycomb Repressive Complex 2 (PRC2) components while inhibiting the associated histone H3 at lysine 27 trimethylation (H3K27me3).