Abstract
Small molecule protein kinase inhibitors show great promise as anti-cancer agents, however, de novo and acquired resistance present problems. These are reviewed and illustrated using the receptor tyrosine kinase, KIT, as an example. Emerging solutions are presented, such as targeting active kinase conformations.
Keywords: Anti-cancer agents, protein kinase inhibitors, drug design, active kinase conformation, nactive kinase conformation, selectivity, inactive kinase conformation
Mini-Reviews in Medicinal Chemistry
Title: Small Molecule Inhibitors of Protein Kinases in Cancer- How to Overcome Resistance
Volume: 6 Issue: 10
Author(s): R. Griffith, M. N. Brown, A. McCluskey and L. K. Ashman
Affiliation:
Keywords: Anti-cancer agents, protein kinase inhibitors, drug design, active kinase conformation, nactive kinase conformation, selectivity, inactive kinase conformation
Abstract: Small molecule protein kinase inhibitors show great promise as anti-cancer agents, however, de novo and acquired resistance present problems. These are reviewed and illustrated using the receptor tyrosine kinase, KIT, as an example. Emerging solutions are presented, such as targeting active kinase conformations.
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Cite this article as:
Griffith R., N. Brown M., McCluskey A. and K. Ashman L., Small Molecule Inhibitors of Protein Kinases in Cancer- How to Overcome Resistance, Mini-Reviews in Medicinal Chemistry 2006; 6 (10) . https://dx.doi.org/10.2174/138955706778560184
DOI https://dx.doi.org/10.2174/138955706778560184 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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