Direct binding of Bcl-2 family proteins by quercetin triggers its pro-apoptotic activity.
ACS Chem Biol
; 9(12): 2737-41, 2014 Dec 19.
Article
en En
| MEDLINE
| ID: mdl-25211642
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.
Texto completo:
1
Colección:
01-internacional
Asunto principal:
Quercetina
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Regulación Neoplásica de la Expresión Génica
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Proteínas Proto-Oncogénicas c-bcl-2
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Proteína bcl-X
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Antineoplásicos Fitogénicos
Límite:
Humans
Idioma:
En
Revista:
ACS Chem Biol
Año:
2014
Tipo del documento:
Article
País de afiliación:
Grecia