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Epigenetics as a paradigm for cancer treatment: chemically targeting the histone lysine methyltransferase EZH2

Published on December 31, 2015   21 min

A selection of talks on Pharmaceutical Sciences

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0:00
The title of today's talk is 'Epigenetics as a Paradigm for Cancer Treatment: Chemically Targeting the Histone Lysine Methyltransferase EZH2. My name is Sharad Verma and I work for GlaxoSmithKline, and I support the Oncology Therapeutic area in the area of early development.
0:24
The objectives of today's presentation are as follows. I would like to provide the viewer with an improved understanding of first, cancer as an unmet medical need, and then discuss epigenetics as a paradigm for treating cancer. In this regard, I will discuss epigenetics from a structural mechanistic standpoint, and then focus on one particular class of enzymes called histone methyltransferases. I will then discuss EZH2 as an example within this target class. Specifically, what is EZH2 and what it does and the rationale for targeting EZH2 in oncology. Further discussion will then focus on the development of EZH2 inhibitors. First, some general drug discovery themes, and then discussion around some of the lead molecules that have arisen from those discovery efforts, and then finally a summary and future outlook.
1:33
Cancer is a major unmet medical need of global significance. It is the leading cause of death worldwide and the second leading cause of death in the United States, following coronary heart disease. It is estimated by the American Cancer Society that in 2015, there will be 1.66 million new cases of cancer diagnosed. The number of cancer cases is continually rising especially in the United States and European Union countries. This is in large part driven by an aging population, as cancer cases are more prominent in an elderly population. 2/3rds of all cases are in patients 65 and older.

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Epigenetics as a paradigm for cancer treatment: chemically targeting the histone lysine methyltransferase EZH2

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