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Cellzome Announces Second Major Strategic Drug Discovery Alliance with GlaxoSmithKline in Inflammatory Disease
Date:3/10/2010

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About Episphere(TM) and epigenetics

Episphere(TM) is a chemical proteomics technology for the discovery of novel drugs directed against targets involved in epigenetic regulation. The technology allows the screening and profiling of inhibitors of epigenetic targets in their native environment, directly in the lysate of cells and tissues and can also differentiate between the complexes these targets operate in. The term epigenetics refers to heritable changes in gene expression and phenotype caused by mechanisms other than changes in DNA sequence. One major mechanism is the specific enzymatic modification of histone tails, which affects the packaging of DNA into chromatin and through that controls the transcription of specific genes. Enzymes, such as histone deacetylases (HDAC) or methyltransferases (HMT) can change the modification of the histone tails and therefore change the 'histone code'. Dysregulation of these modifications is thought to play a central role in cancer and in chronic degenerative diseases like neurological and autoimmune disease. The enzymes which carry out these histone modifications are part of large multifunctional protein complexes, which represent attractive novel targets for drug discovery.


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