• Characterization of a triazole scaffold compound as an inhibitor of Mycobacterium tuberculosis Imidazoleglycerol‐phosphate dehydratase

    3 days ago - By Wiley

    Abstract
    Mycobacterium tuberculosis , the causative agent of human tuberculosis , employs ten enzymes including imidazoleglycerol-phosphate dehydratase for de novo biosynthesis of histidine. The absence of histidine-biosynthesis in humans combined with its essentiality for Mtb makes the enzymes of this pathway major anti-TB drug targets. We explored the inhibitory potential of a small molecule β--DL-alanine against Mtb IGPD. DLA exhibits an in vitro inhibitory efficacy in the lower micromolar range. Higher-resolution crystal structures of native and substrate-bound Mtb IGPD provided...
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