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Cellzome enters second strategic drug discovery pact with GSK in inflammatory disease
Cambridge, England | Thursday, March 11, 2010, 08:00 Hrs  [IST]

Cellzome announced that it has formed a second strategic alliance with GlaxoSmithKline (GSK). This new collaboration gives GSK exclusive access to Cellzome's proprietary Episphere technology in the emerging field of epigenetics as applied to immunoinflammatory disease. Epigenetic mechanisms play a key role in controlling immune cell differentiation and inflammatory gene expression during an excessive inflammatory response.

Under the terms of the agreement, the companies will work together using Cellzome's Episphere technology platform, to identify selective small-molecule drug candidates against targets from four different epigenetic target classes. The companies will share operational responsibility for the programs until identification of drug candidates, at which stage GSK will assume responsibility for any further preclinical and clinical development and commercialisation.

Under the financial terms, Cellzome will receive an upfront payment of EUR33 million, comprising technology access fees and the purchase of equity. In addition, Cellzome is eligible for milestone payments and tiered royalties for each programme. Milestone payments under this collaboration could reach over EUR475 million if all programmes under the alliance are successfully developed and commercialised.

Episphere 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.

Tim Edwards, chief executive officer of Cellzome, said: "We are delighted to form another major alliance with GSK, using our leading technology and people to find transformative medicines in this exciting field of biology. Combining forces with GSK will accelerate the development of new anti-inflammatory drugs for the benefit of patients."

Cellzome is a privately-owned drug discovery and development company, and a leader in the use of chemical proteomics technologies to identify a new generation of drug candidates for the treatment of inflammatory diseases.

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