Ontology highlight
ABSTRACT:
SUBMITTER: Rawls KA
PROVIDER: S-EPMC2801607 | biostudies-literature | 2009 Dec
REPOSITORIES: biostudies-literature
Rawls Katherine A KA Lang P Therese PT Takeuchi Jun J Imamura Shinichi S Baguley Tyler D TD Grundner Christoph C Alber Tom T Ellman Jonathan A JA
Bioorganic & medicinal chemistry letters 20091025 24
The development of low muM inhibitors of the Mycobacterium tuberculosis phosphatase PtpA is reported. The most potent of these inhibitors (K(i)=1.4+/-0.3 microM) was found to be selective when tested against a panel of human tyrosine and dual-specificity phosphatases (11-fold vs the highly homologous HCPtpA, and >70-fold vs all others tested). Modeling the inhibitor-PtpA complexes explained the structure-activity relationships observed in vitro and revealed further possibilities for compound dev ...[more]