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