Picking pockets to fuel antimicrobial drug discovery

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    5 Citations (Scopus)

    Abstract

    The inhibition of essential enzymes in microbial pathogens offers a route to treatment of infectious diseases. However, although the biology of the organism dictates a need for a particular enzyme activity, this does not necessarily mean that the enzyme is a good drug target. The chemistry of the active site (size, shape and properties) determines the likelihood of finding a molecule with the right properties to influence drug discovery. Discriminating between good and less-good targets is important. Studies on enzymes involved in the regulation of oxidative stress and pterin/folate metabolism of trypanosomatid parasites and isoprenoid precursor biosynthesis in bacteria and apicomplexan parasites illustrates a range of active sites representing those that are challenging with respect to the discovery of potent inhibitors, to others that provide more promising opportunities in drug discovery.

    Original languageEnglish
    Pages (from-to)980-984
    Number of pages5
    JournalBiochemical Society Transactions
    Volume35
    DOIs
    Publication statusPublished - Nov 2007

    Keywords

    • antimicrobial drug
    • enzyme inhibition
    • isoprenoid
    • non-mevalonate pathway
    • pteridine reductase
    • trypanothione reductase
    • ISOPRENOID PRECURSOR BIOSYNTHESIS
    • MAJOR PTERIDINE REDUCTASE
    • NON-MEVALONATE PATHWAY
    • TRYPANOTHIONE REDUCTASE
    • CRYSTAL-STRUCTURE
    • LEISHMANIA-MAJOR
    • 2,4-CYCLODIPHOSPHATE SYNTHASE
    • CRITHIDIA-FASCICULATA
    • MAXIMAL AFFINITY
    • ESSENTIAL ENZYME

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