Fragment-based substrate activity screening method for the identification of potent inhibitors of the Mycobacterium tuberculosis phosphatase PtpB

Abstract

A new substrate-based fragment approach for the identification of novel PTP inhibitors is presented. This method was applied to Mycobacterium tuberculosis PtpB, a promising new target for the treatment of tuberculosis. This resulted in the development of the most potent PtpB inhibitor reported to date (0.22 μM) with low molecular weight and good selectivity against a panel of other protein tyrosine phosphatases. Copyright © 2007 American Chemical Society.