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KEK and Astellas Begin Collaborative Research to Discover New Drugs for Neglected Tropical Diseases

Published: Monday, October 08, 2012
Last Updated: Monday, October 08, 2012
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The design of the novel pharmaceuticals will be based on the three-dimensional structure of proteins using synchrotron X-ray crystallography.

The High Energy Accelerator Research Organization  (KEK) and Astellas Pharma Inc. will begin collaborative research to discover new drugs  for the  treatment of neglected tropical  diseases through the use of synchrotron X-ray crystallography. 

The target of this research is infectious diseases caused by parasitic protozoans, namely leishmaniasis, Chagas disease and Sleeping sickness and will be divided into two major phases. The first phase involves elucidating the three-dimensional structure of parasitic protozoan proteins that are potential drug targets, allowing the identification of inhibiting compounds that block the action of pathogenic proteins. The second phase consists of the Access to Healthstructural analysis of target proteins in complex with the inhibitory compound. Crystallization robots and dedicated beamlines developed by KEK will be employed with structural analysis performed efficiently and over a short time period.    Structural data obtained through the successful application of this collaborative research will contribute to the discovery of new drugs for the treatment of parasitic protozoan diseases.  

Neglected Tropical Diseases (NTDs), prevalent mainly in poor remote rural areas, are infectious diseases spread by parasites or bacteria. Approximately one billion people are affected worldwide and some 500,000 die each year as a result. NTDs are a serious healthcare issue that is being addressed on a global scale. A valuable approach to new drug development that has evolved rapidly in recent years is the design of pharmaceuticals based on the three-dimensional structure of proteins. This method involves designing drugs for the target protein by analyzing and comparing the structure of various compounds and complex conjugates in order to develop an overall understanding of the mechanism by which protein activity is inhibited (or activated). Since 2006, KEK and Astellas have been progressing drug discovery research using synchrotron X-ray beams. The synchrotron  radiation  beam produced in the Photon Factory in KEK  has high-brilliant and high-energy  properties conferring advantages such as the ability to  conduct  experiments on small  crystals that would have been difficult to analyze using conventional X-rays and to acquire data in an  extremely short period that would otherwise take vast amounts of time.

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