Inhibitors of infamous Ras oncogene reported by Genentech researchers

4 December 2011

A drug discovery team at Genentech, a subsidiary of Swiss drug major Roche (ROG: SIX) has uncovered a chink in the molecular armor of Ras, the most commonly occurring oncogene, which is a gene that when mutated has the potential of causing cancer in humans, reports the science news service EurekAlert.

The chink, binding pocket of "functional significance" on the Ras oncoprotein could provide the long-sought attack point for a therapeutic agent, making the "undruggable" Ras oncogene "druggable," the researchers reported at the American Society for Cell Biology's 51st Annual Meeting in Denver, Colorado.

The first human oncogene to be identified, Ras is mutated in about 25% of all human tumors. For cancer patients, the presence of an activated Ras oncogene is a poor prognosis marker. Ras has a molecular on-off switch, activated by the energy transfer molecule GTP. In the "on" position, the oncogene activates critical cell signaling pathways involving cell proliferation, cell migration and cell differentiation, all of which are in hyper-drive in tumors.

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