Article
Recent developments in the third generation inhibitors of Bcr-Abl for overriding T315I mutation.
Current medicinal chemistry - 1 Jan 2011
Lu X Y, Cai Q, Ding K
Abstract excerpt
In the treatment of chronic myeloid leukemia (CML) with Bcr-Abl kinase inhibitors, the T315I gatekeeper mutant has emerged as resistant to all currently approved agents, such as imatinib, nilotinib and dasatinib, by discrupting important contact interactions between the inhibitors and the enzyme. To overcome this particular resistance, several different strategies have been explored and many molecules have been...
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