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
Current Topics in Medicinal Chemistry
Title: Targeting Cancer: The Challenges and Successes of Structure-Based Drug Design Against the Human Purinome
Volume: 6 Issue: 11
Author(s): Mark Knapp, Cornelia Bellamacina, Jeremy M. Murray and Dirksen E. Bussiere
Affiliation:
Keywords: Structure-based drug design, purine-binding proteins, structural biology, Eg5, KSP, kinases, purine nucleoside phosphorylase, PNP
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.
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Cite this article as:
Knapp Mark, Bellamacina Cornelia, Murray M. Jeremy and Bussiere E. Dirksen, Targeting Cancer: The Challenges and Successes of Structure-Based Drug Design Against the Human Purinome, Current Topics in Medicinal Chemistry 2006; 6 (11) . https://dx.doi.org/10.2174/156802606777812040
DOI https://dx.doi.org/10.2174/156802606777812040 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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