Crispene E, a Cis-clerodane Diterpene Inhibits STAT3 Dimerization in Breast Cancer Cells

Overview

Journal Org Biomol Chem

Publisher Royal Society of Chemistry

Specialties Biochemistry
Chemistry

Date 2015 Feb 28

PMID 25721973

Citations 10

Authors

Julia Mantaj

S M Abdur Rahman

Bishwajit Bokshi

Choudhury M Hasan

Paul J M Jackson

Richard B Parsons

Khondaker M Rahman

Affiliations

Soon will be listed here.

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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