Design strategies for protein kinase inhibitors

Authors

Keykavous Parang, University of Rhode Island
Gongqin Sun, University of Rhode Island

Document Type

Article

Date of Original Version

9-1-2004

Abstract

Deregulation of protein kinases due to mutation or overexpression is a hallmark of several diseases, for example, cancer, diabetes, inflammation and cardiovascular disorders. Consequently, there has been a growing interest in the discovery of protein kinase inhibitors as novel drugs. Here, we focus on key milestones and advances in protein kinase inhibitor drug discovery over the last year, with an emphasis on novel strategies such as targeting of single and multiple binding sites, inactive conformations of kinases, allosteric sites, regulatory domains and heat shock proteins. We will highlight recent developments for specific inhibitors in clinical studies for growth factor receptors, non-receptor tyrosine kinases and serine/threonine kinases.

Publication Title, e.g., Journal

Current Opinion in Drug Discovery and Development

Volume

7

Issue

5

Citation/Publisher Attribution

Parang, Keykavous, and Gongqin Sun. "Design strategies for protein kinase inhibitors." Current Opinion in Drug Discovery and Development 7, 5 (2004). https://digitalcommons.uri.edu/cmb_facpubs/426