Functional characterization of selective exosite-binding inhibitors of matrix metalloproteinase-13 (MMP-13) - Experimental validation in human breast and colon cancer
|dc.identifier.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.|
© 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.
|dc.title||Functional characterization of selective exosite-binding inhibitors of matrix metalloproteinase-13 (MMP-13) - Experimental validation in human breast and colon cancer|
|dcterms.source.title||Bioscience, Biotechnology and Biochemistry|
|curtin.department||School of Biomedical Sciences|
|curtin.accessStatus||Fulltext not available|
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