Monash team determines cancer protein form

By Graeme O'Neill
Tuesday, 25 October, 2005

Monash University researchers have determined the structure of a key oncoprotein, JAK2, being targeted by Melbourne oncology drug developer Cytopia (ASX:CYT). Cytopia MD Dr Kevin Healey said the new structural data on the JAK2 kinase, originally identified by researchers at the Ludwig Cancer Research Institute in Melbourne, should greatly assist in designing drugs to inhibit its activity in cancerous cells. Healey said the enzyme is a driver for many cancers and cardiovascular disorders. "Drugs that can prevent the activity of JAK2 kinase could generate sales of billions of dollars," he said,

Researchers recently identified a JAK2 mutation as the primary cause of a range of myeloproliferative disorders involving over-production of various blood cell types, including polythemia vera, a rare red-blood cell disorder that causes thrombosis. Dr Jamie Rossjohn's research group at Monash University identified the protein's active site, a potential target for antagonist drugs. A number of kinase inhibitors are already on the market, but are non-selective in their action, according to Dr Rossjohn -- the way is now open to develop specific inhibitors of JAK2 kinase, which is highly expressed in many cancers.

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