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

Published on December 31, 2015   21 min
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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.
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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.
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Epigenetics as a paradigm for cancer treatment: chemically targeting the histone lysine methyltransferase EZH2

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