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2017 ; 8
(1
): 329-344
Nephropedia Template TP
gab.com Text
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English Wikipedia
Arctigenin inhibits STAT3 and exhibits anticancer potential in human
triple-negative breast cancer therapy
#MMPMID27861147
Feng T
; Cao W
; Shen W
; Zhang L
; Gu X
; Guo Y
; Tsai HI
; Liu X
; Li J
; Zhang J
; Li S
; Wu F
; Liu Y
Oncotarget
2017[Jan]; 8
(1
): 329-344
PMID27861147
show ga
Triple-negative breast cancers (TNBCs) are the most aggressive and hard-to-treat
breast tumors with poor prognosis, and exploration for novel therapeutic drugs is
impending. Arctigenin (Atn), a bioactive lignan isolated from seeds of Arctium
lappa L, has been reported to inhibit many cancer types; however, the effect of
Atn on TNBC remains unclear. In this study, we demonstrated that Atn decreased
proliferation, and induced apoptosis in TNBC cells. Furthermore, we explored the
underlying mechanism of Atn inhibition on TNBC cells. Computational docking and
affinity assay showed that Atn bound to the SH2 domain of STAT3. Atn inhibited
STAT3 binding to genomic DNA by disrupting hydrogen bond linking between DNA and
STAT3. In addition, Atn augmented TaxotereŽ-induced TNBC cell cytotoxicity. TNBC
xenograft tests also confirmed the antitumor effect of Atn in vivo. These
characteristics render Atn as a promising candidate drug for further development
and for designing new effective STAT3 inhibitors.
|Animals
[MESH]
|Antineoplastic Agents/*pharmacology/therapeutic use
[MESH]