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  • Approaches to Protozoan Drug Discovery: Phenotypic Screening. Miniperspectives Series on Phenotypic Screening for Antiinfective Targets

    Author(s)
    Sykes, Melissa L
    Avery, Vicky M
    Griffith University Author(s)
    Sykes, Melissa L.
    Avery, Vicky M.
    Year published
    2013
    Metadata
    Show full item record
    Abstract
    Determining the activity of a compound and the potential impact on a diseased state is frequently undertaken using phenotypic or target-based approaches. Phenotypic screens have the advantage of the whole organism being exposed to the compound and thus all the targets and biological pathways associated with it. Cell penetration and access to targets in their "natural" environment are taken into account. Unless utilizing a genetically modified organism with an additional target associated indicator, elucidation of specific target(s) of active compounds is necessary. Target discovery is desirable to allow development of chemical ...
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    Determining the activity of a compound and the potential impact on a diseased state is frequently undertaken using phenotypic or target-based approaches. Phenotypic screens have the advantage of the whole organism being exposed to the compound and thus all the targets and biological pathways associated with it. Cell penetration and access to targets in their "natural" environment are taken into account. Unless utilizing a genetically modified organism with an additional target associated indicator, elucidation of specific target(s) of active compounds is necessary. Target discovery is desirable to allow development of chemical entities based upon knowledge of the target structure. Phenotypic drug discovery has successfully identified new molecular entities for neglected protozoan disease research. In this perspective, the phenotypic approaches used to identify chemical entities for drug discovery and for use as tools against the parasites Plasmodium falciparum , Trypanosoma brucei brucei , and Trypanosoma cruzi will be outlined.
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    Journal Title
    Journal of Medicinal Chemistry
    Volume
    56
    Issue
    20
    DOI
    https://doi.org/10.1021/jm4004279
    Subject
    Medicinal and biomolecular chemistry
    Medicinal and biomolecular chemistry not elsewhere classified
    Organic chemistry
    Pharmacology and pharmaceutical sciences
    Publication URI
    http://hdl.handle.net/10072/56542
    Collection
    • Journal articles

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