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2017 ; 18
(10
): ä Nephropedia Template TP
gab.com Text
Twit Text FOAVip
Twit Text #
English Wikipedia
Coumestrol Epigenetically Suppresses Cancer Cell Proliferation: Coumestrol Is a
Natural Haspin Kinase Inhibitor
#MMPMID29064398
Kim JE
; Lee SY
; Jang M
; Choi HK
; Kim JH
; Chen H
; Lim TG
; Dong Z
; Lee KW
Int J Mol Sci
2017[Oct]; 18
(10
): ä PMID29064398
show ga
Targeting epigenetic changes in gene expression in cancer cells may offer new
strategies for the development of selective cancer therapies. In the present
study, we investigated coumestrol, a natural compound exhibiting broad
anti-cancer effects against skin melanoma, lung cancer and colon cancer cell
growth. Haspin kinase was identified as a direct target protein of coumestrol
using kinase profiling analysis. Histone H3 is a direct substrate of haspin
kinase. We observed haspin kinase overexpression as well as greater
phosphorylation of histone H3 at threonine 3 (Thr-3) in the cancer cells compared
to normal cells. Computer modeling using the Schrödinger Suite program identified
the binding interface within the ATP binding site. These findings suggest that
the anti-cancer effect of coumestrol is due to the direct targeting of haspin
kinase. Coumestrol has considerable potential for further development as a novel
anti-cancer agent.
|A549 Cells
[MESH]
|Binding Sites
[MESH]
|Cell Line, Tumor
[MESH]
|Cell Proliferation/*drug effects
[MESH]
|Coumestrol/*pharmacology
[MESH]
|HCT116 Cells
[MESH]
|Histones/metabolism
[MESH]
|Humans
[MESH]
|Intracellular Signaling Peptides and Proteins/*antagonists &
inhibitors/chemistry/metabolism
[MESH]