2. Academic Validation
  3. Crispene E, a cis-clerodane diterpene inhibits STAT3 dimerization in breast cancer cells

Crispene E, a cis-clerodane diterpene inhibits STAT3 dimerization in breast cancer cells

  • Org Biomol Chem. 2015 Apr 7;13(13):3882-6. doi: 10.1039/c5ob00052a.
Julia Mantaj 1,  S M Abdur Rahman,  Bishwajit Bokshi,  Choudhury M Hasan,  Paul J M Jackson,  Richard B Parsons,  Khondaker M Rahman
Affiliations

Affiliation

  • 1 Institute of Pharmaceutical Science, King's College London, London SE1 9NH, UK. [email protected].
PMID: 25721973 DOI: 10.1039/c5ob00052a
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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