Structure of Glivec target revealed
receptor-associated tyrosine kinase which has been associated with
a number of malignant cancers.
Syrrx has determined the atomic structure of c-Kit kinase, a receptor-associated tyrosine kinase which has been associated with a number of malignant cancers. The work opens the door to the development of a new generation of highly specific anticancer drugs.
This particular enzyme has emerged as a particularly promising drug target in cancer on the back of the success of Novartis' Glivec/Gleevec (imatinib), which has achieved unprecedented efficacy in chronic myelogenous leukaemia and is also showing promise in other cancers. Glivec targets c-Kit kinase, along with another related enzyme known as c-Abl kinase.
The c-Kit structure was determined using Syrrx's high-throughput structural biology platform that uses automation and the company's proprietary Nanovolume Crystallization technology to crystallize disease-causing proteins.
The details of the structure will appear in the September issue of the Journal of Biological Chemistry.