Journal
ACS CHEMICAL BIOLOGY
Volume 9, Issue 12, Pages 2737-2741Publisher
AMER CHEMICAL SOC
DOI: 10.1021/cb500259e
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Funding
- European Union (European Social Fund-ESF)
- Greek national funds through the Operational Program Education and Lifelong Learning of the National Strategic Reference Framework (NSRF)-Research Funding Program: HERAKLEITOS II
- European Union (European Regional Development Fund-ERDF)
- Greek national funds through the Operational Program THESSALY-MAINLAND GREECE AND EPIRUS of the National Strategic Reference Framework (NSRF)
- Greek national funds through the Operational Program Education and Lifelong Learning of the National Strategic Reference Framework (NSRF)\-Research Funding Program: ARISTEIA II. Investing in knowledge society through the European Social Fund
- National R&D Program for Cancer Control, Ministry of Health & Welfare, Republic of Korea [1220150]
- Korea Health Promotion Institute [1220150] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
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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 doseresponse 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.
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