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Targeting cancer: the challenges and successes of structure-based drug design against the human purinome

by: Mark Knapp, Cornelia Bellamacina, Jeremy M Murray, Dirksen E Bussiere
Current Topics In Medicinal Chemistry, Vol. 6, No. 11. (2006), pp. 1129-1159.


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Purine-binding proteins are of critical importance to all living organisms. Approximately 13% of the human genome is devoted to coding for purine-binding proteins. Given their importance, purine-binding proteins are attractive targets for chemotherapeutic intervention against a variety of disease states, particularly cancer. Modern computational and biophysical techniques, combined together in a structure-based drug design approach, aid immensely in the discovery of inhibitors of these targets. This review covers the process of modern structure-based drug design and gives examples of its use in discovery and development of drugs that target purine-binding proteins. The targets reviewed are human purine nucleoside phosphorylase, human epidermal growth factor receptor kinase, and human kinesin spindle protein. [Journal Article; In English; Netherlands; In-Process]


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