Inhibition of Mycobacterium tuberculosis pantothenate synthetase by analogues of the reaction intermediate.

Alessio Ciulli (Lead / Corresponding author), D.E. Scott, M. Ando, Fernando Reyes, S. Adrian Saldanha, K.L. Tuck, D.Y. Chirgadze, T.L. Blundell, C. Abell (Lead / Corresponding author)

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    Abstract

    Get stuck in: Pantothenate synthetase is an attractive target for the development of novel small-molecule drugs against Mycobacterium tuberculosis. Three related sulfamoyl adenylate inhibitors were designed to closely mimic the structure of the reaction intermediate, pantoyl adenylate. The most potent inhibitor exhibited dissociation and inhibition constants of about 100 nM. The structural elucidation of the compounds bound to the enzyme will aid development of subsequent inhibitors.
    Original languageEnglish
    Pages (from-to)2606-2611
    Number of pages6
    JournalChemBioChem
    Volume9
    Issue number16
    DOIs
    Publication statusPublished - 3 Nov 2008

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  • Cite this

    Ciulli, A., Scott, D. E., Ando, M., Reyes, F., Saldanha, S. A., Tuck, K. L., Chirgadze, D. Y., Blundell, T. L., & Abell, C. (2008). Inhibition of Mycobacterium tuberculosis pantothenate synthetase by analogues of the reaction intermediate. ChemBioChem, 9(16), 2606-2611. https://doi.org/10.1002/cbic.200800437