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Researchers unveil vital key to cancer
Date:8/6/2008

rk will allow chemists to design an anti-cancer drug with fewer side effects, allowing scientists to assess the relative importance of Mps1 inhibition in different disease indications, including those that are currently hard to treat such as lung and pancreatic cancers.

Dr Eyers, whose findings are published in the Journal of Biological Chemistry (August 2008), said: "The crystallalographic structures of only a few key "mitotic" kinases are currently known so we are very early in the game. The scientific community has high hopes for developing novel "anti-mitotic" cancer therapies using this method of structure-based drug design.

"Mps1 is a rational target because of its critical role in preventing aneuploidy. We wanted to see what this protein looked like at the molecular level and, by revealing the active site "lock", help design a new inhibitory "key" to physically block the ATP-binding site.

His colleague Dr Lydia Tabernero added: "This work presents the first crystallographic structure of human Mps1, an important regulator of chromosomal stability and a potential target in cancer therapy. Our research has revealed several important structural features and additional binding sites that could be exploited for the development of specific Mps1 inhibitors."


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Contact: Mikaela Sitford
Mikaela.Sitford@manchester.ac.uk
01-612-752-111
University of Manchester
Source:Eurekalert

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