Article
Crenolanib is a selective type I pan-FLT3 inhibitor.
Proceedings of the National Academy of Sciences of the United States of America - 8 Apr 2014
Smith Catherine Choy, Lasater Elisabeth A, Lin Kimberly C, Wang Qi, McCreery Melissa Quino, Stewart Whitney K, Damon Lauren E, Perl Alexander E, Jeschke Grace R, Sugita Mayumi, Carroll Martin, Kogan Scott C, Kuriyan John, Shah Neil P
Abstract excerpt
Tyrosine kinase inhibitors (TKIs) represent transformative therapies for several malignancies. Two critical features necessary for maximizing TKI tolerability and response duration are kinase selectivity and invulnerability to resistance-conferring kinase domain (KD) mutations in the intended target. No prior TKI has demonstrated both of these properties. Aiming to maximize selectivity, medicinal chemists have...
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