Article
A novel pyridopyrimidine inhibitor of abl kinase is a picomolar inhibitor of Bcr-abl-driven K562 cells and is effective against STI571-resistant Bcr-abl mutants.
Clinical cancer research : an official journal of the American Association for Cancer Research - 1 Apr 2003
Huron David R, Gorre Mercedes E, Kraker Alan J, Sawyers Charles L, Rosen Neal, Moasser Mark M
Abstract excerpt
Inhibition of the constitutively active Bcr-abl tyrosine kinase(TK) by STI571 has proven to be a highly effective treatment for chronic myelogenous leukemia (CML). However, STI571 is only transiently effective in blast crisis, and drug resistance emerges by amplification of or development of mutational changes in Bcr-abl. We have screened a family of TK inhibitors of the pyrido [2,3-d]pyrimidine class, unrelated...
Read the complete abstract on PubMedTopics
Share this publication in a Topic to start or enrich a Post.
