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Title 

Direct binding of Bcl-2 family proteins by quercetin triggers its pro-apoptotic activity

Authors 

A PrimikyriM V ChatziathanasiadouE KaraliE KostarasM D MantzarisE HatzimichaelShin Jae-SunSeung-Wook ChiE BriasoulisE KolettasI P GerothanassisA G Tzakos

Publisher 

American Chemical Society

Issue Date 

2014

Citation 

ACS Chemical Biology, vol. 9, no. 0, pp. 2737-2741

Abstract 

Bcl-2 family proteins are important regulators of apoptosis and its antiapoptotic members, which are overexpressed in many types of cancer, are of high prognostic significance, establishing them as attractive therapeutic targets. Quercetin, a natural flavonoid, has drawn much attention because it exerts anticancer effects, while sparing normal cells. A multidisciplinary approach has been employed herein, in an effort to reveal its mode of action including dose-response antiproliferative activity and induced apoptosis effect, biochemical and physicochemical assays, and computational calculations. It may be concluded that, quercetin binds directly to the BH3 domain of Bcl-2 and Bcl-xL proteins, thereby inhibiting their activity and promoting cancer cell apoptosis.

ISSN 

1554-8929

Link 

http://dx.doi.org/10.1021/cb500259e

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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