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    Functional characterization of selective exosite-binding inhibitors of matrix metalloproteinase-13 (MMP-13) - Experimental validation in human breast and colon cancer

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    Authors
    Kothapalli, R.
    Siveen, K.
    Tan, T.
    Thiery, J.
    Kumar, A.
    Sethi, Gautam
    Swaminathan, K.
    Date
    2016
    Type
    Journal Article
    
    Metadata
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    Citation
    Kothapalli, R. and Siveen, K. and Tan, T. and Thiery, J. and Kumar, A. and Sethi, G. and Swaminathan, K. 2016. Functional characterization of selective exosite-binding inhibitors of matrix metalloproteinase-13 (MMP-13) - Experimental validation in human breast and colon cancer. Bioscience, Biotechnology and Biochemistry. 80 (11): pp. 2122-2131.
    Source Title
    Bioscience, Biotechnology and Biochemistry
    DOI
    10.1080/09168451.2016.1200456
    ISSN
    0916-8451
    School
    School of Biomedical Sciences
    URI
    http://hdl.handle.net/20.500.11937/58851
    Collection
    • Curtin Research Publications
    Abstract

    © 2016 Japan Society for Bioscience, Biotechnology, and Agrochemistry.Considering the pathological significance of MMP-13 in breast and colon cancers, exosite-based inhibition of the C-terminal hemopexin (Hpx) domain could serve as an alternative strategy to develop selective inhibitors for MMP-13. Two of six lead compounds, compound 5 (2,3-dihydro-1,4-benzodioxine- 5-carboxylic acid) and compound 6 (1-acetyl-4-hydroxypyrrolidine-2-carboxylic acid) exhibited considerable inhibitory activity against MMP-13. Complementing to this study, we have also shown the gene expression levels of MMP-13 within the subtypes of colon and breast cancers classified from patients' tissue samples to provide a better understanding on which subtype of breast cancer patients would get benefited by MMP-13 inhibitors. Our current results show that compounds 5 and 6 could effectively inhibit MMP-13 and provide specific therapeutic possibilities in the treatment of inflammatory disorders and cancers. The characterization of these lead compounds would provide a better mechanistic understanding of exosite-based inhibition of MMP-13, which could overcome the challenges in the identification of other MMP catalytic domain-specific inhibitors.

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