title: Crispene E, a cis-clerodane diterpene inhibits STAT3 dimerization in breast cancer cells.
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.
authors.affiliation: Institute of Pharmaceutical Science, King's College London, London SE1 9NH, UK. k.miraz.rahman@kcl.ac.uk.
authors.forename: Julia
authors.initials: J
authors.lastname: Mantaj
authors.forename: S M Abdur
authors.initials: SM
authors.lastname: Rahman
authors.forename: Bishwajit
authors.initials: B
authors.lastname: Bokshi
authors.forename: Choudhury M
authors.initials: CM
authors.lastname: Hasan
authors.forename: Paul J M
authors.initials: PJ
authors.lastname: Jackson
authors.forename: Richard B
authors.initials: RB
authors.lastname: Parsons
authors.forename: Khondaker M
authors.initials: KM
authors.lastname: Rahman
mesh_terms: D001943:Breast Neoplasms / Q000473:pathology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D045785:Diterpenes, Clerodane / Q000494:pharmacology*; D015972:Gene Expression Regulation, Neoplastic / Q000187:drug effects; D006801:Humans; D008958:Models, Molecular; D055503:Protein Multimerization / Q000187:drug effects*; D020836:Protein Structure, Quaternary; D050796:STAT3 Transcription Factor / Q000737:chemistry* / Q000235:genetics
chemical_list: D045785:Diterpenes, Clerodane; D050796:STAT3 Transcription Factor; C000603321:crispene E