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  • Saccharin: A lead compound for structure-based drug design of carbonic anhydrase IX inhibitors

    Author(s)
    Mahon, Brian P
    Hendon, Alex M
    Driscoll, Jenna M
    Rankin, Gregory M
    Poulsen, Sally-Ann
    Supuran, Claudiu T
    McKenna, Robert
    Griffith University Author(s)
    Poulsen, Sally-Ann
    Year published
    2015
    Metadata
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    Abstract
    Carbonic anhydrase IX (CA IX) is a key modulator of aggressive tumor behavior and a prognostic marker and target for several cancers. Saccharin (SAC) based compounds may provide an avenue to overcome CA isoform specificity, as they display both nanomolar affinity and preferential binding, for CA IX compared to CA II (>50-fold for SAC and >1000-fold when SAC is conjugated to a carbohydrate moiety). The X-ray crystal structures of SAC and a SAC-carbohydrate conjugate bound to a CA IX-mimic are presented and compared to CA II. The structures provide substantial new insight into the mechanism of SAC selective CA isoform inhibition.Carbonic anhydrase IX (CA IX) is a key modulator of aggressive tumor behavior and a prognostic marker and target for several cancers. Saccharin (SAC) based compounds may provide an avenue to overcome CA isoform specificity, as they display both nanomolar affinity and preferential binding, for CA IX compared to CA II (>50-fold for SAC and >1000-fold when SAC is conjugated to a carbohydrate moiety). The X-ray crystal structures of SAC and a SAC-carbohydrate conjugate bound to a CA IX-mimic are presented and compared to CA II. The structures provide substantial new insight into the mechanism of SAC selective CA isoform inhibition.
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    Journal Title
    Bioorganic and Medicinal Chemistry Letters
    Volume
    23
    Issue
    4
    DOI
    https://doi.org/10.1016/j.bmc.2014.12.030
    Subject
    Medicinal and biomolecular chemistry
    Medicinal and biomolecular chemistry not elsewhere classified
    Organic chemistry
    Pharmacology and pharmaceutical sciences
    Publication URI
    http://hdl.handle.net/10072/101272
    Collection
    • Journal articles

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