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Mini-Reviews in Medicinal Chemistry


ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Small Molecule Inhibitors of Protein Kinases in Cancer- How to Overcome Resistance

Author(s): R. Griffith, M. N. Brown, A. McCluskey and L. K. Ashman

Volume 6, Issue 10, 2006

Page: [1101 - 1110] Pages: 10

DOI: 10.2174/138955706778560184

Price: $65


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

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