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.
All contents Copyright © 1993-2015 BioCentury Publications, Inc. ALL RIGHTS RESERVED. All use of this Web Site and its contents is governed by the BioCentury User Agreement
. The contents of this Web Site are protected under U.S. and foreign copyright and intellectual property laws, and no part of this Web Site or its contents may be photocopied, reproduced or retransmitted in any form without the written consent of BioCentury, which may be requested from Reprints/Permissions
. BioCentury®; The Bernstein Report on BioBusiness™; The BioCentury 100™; The Clear Route to ROI™; Because Real Intelligence is Hard to Find™; BCIQ™; and BioPharma's Knowledge Center™; are trademarks of BioCentury Publications, Inc., P.O. Box 1246, San Carlos, CA 94070. SciBX® and SciBX: Science-Business eXchange® are trademarks of Nature America, Inc. that are jointly used by BioCentury Publications, Inc. and Nature America, Inc.
Thanks for purchasing this article.
Please bookmark this url for future reference.
We have also sent you a confirming e-mail with a receipt and this same url for your
close [ X ]