Targeting Cancer: The Challenges and Successes of Structure-Based Drug Design Against the Human Purinome

Author(s): Mark Knapp , Cornelia Bellamacina , Jeremy M. Murray , Dirksen E. Bussiere .

Journal Name: Current Topics in Medicinal Chemistry

Volume 6 , Issue 11 , 2006

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Abstract:

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.

Keywords: Structure-based drug design, purine-binding proteins, structural biology, Eg5, KSP, kinases, purine nucleoside phosphorylase, PNP

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Article Details

VOLUME: 6
ISSUE: 11
Year: 2006
Page: [1129 - 1159]
Pages: 31
DOI: 10.2174/156802606777812040
Price: $58

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