Thursday, March 28, 2013
Publication and contact
Automated, high throughput,
microfluidic SAR platform
An automated, microfluidic
SAR platform could be used to rapidly optimize kinase inhibitors. Gleevec imatinib, a small
molecule inhibitor of BCR-ABL tyrosine kinase,
was subjected to repeated cycles of computer-assisted derivatization,
synthesis, purification and screening using a microfluidic system. The best
of the resulting compounds had about 100-fold more potent IC50
values for BCR-ABL than imatinib. The molecules also were more effective
against imatinib-resistant mutant versions of the enzyme and were cell
permeable. Next steps include adapting the platform for cell culture and
screening against nonsoluble targets.
Gleevec is marketed by Novartis AG to treat
Published online March 28, 2013
available for partnering
Desai, B. et al. J. Med.
Chem.; published online Feb. 26, 2013;
Contact: Christopher N. Selway, Cyclofluidic Ltd.,
Welwyn Garden City, U.K.
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