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Crispene E, a cis-clerodane diterpene inhibits STAT3 dimerization in breast cancer cells
Julia Mantaj1, S M Abdur Rahman, Bishwajit Bokshi
1Institute of Pharmaceutical Science, King's College London, London SE1 9NH, UK. k.miraz.rahman@kcl.ac.uk.
Abstract:
Crispene E, a new clerodane-type diterpene, inhibited STAT3 dimerization in a cell-free fluorescent polarisation assay and was found to have significant toxicity against STAT3-dependent MDA-MB 231 breast cancer cell line and selectively inhibited the expression of STAT3 and STAT3 target genes cyclin D1, Fascin and bcl-2. Molecular docking studies suggest the molecule inhibits STAT3 by interacting with its SH2 domain. The compound has been isolated from Tinospora crispa and characterized using standard spectroscopic techniques.
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