Browsing by Subject "Focused amide library"

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    A facile hydroxyindole carboxylic acid based focused library approach for potent and selective inhibitors of Mycobacterium protein tyrosine phosphatase B
    (Wiley, 2013) Zeng, Li-Fan; Xu, Jie; He, Yantao; He, Rongjun; Wu, Li; Gunawan, Andrea M.; Zhang, Zhong-Yin; Biochemistry and Molecular Biology, School of Medicine
    Focused on Mtb: A facile hydroxyindole carboxylic acid based focused amide library was designed to target both the PTP active site and a unique nearby pocket for enhanced affinity and selectivity. HTS of the library led to the identification of a highly potent and selective inhibitor, 11 a, of mPTPB, an essential virulence factor for Mycobacterium tuberculosis. Compound 11 a shows high cellular activity and is capable of reversing the altered immune responses induced by mPTPB in macrophages.