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Celecoxib and Bcl-2: emerging possibilities for anticancer drug design.

ABSTRACT: Celecoxib is a multifaceted drug with promising anticancer properties. A number of studies have been conducted that implicate the compound in modulating the expression of Bcl-2 family members and mitochondria-mediated apoptosis. The growing data surrounding the role of celecoxib in the regulation of the mitochondrial death pathway provides a platform for ongoing debate. Studies that describe celecoxib's properties as a BH3 mimic or as a direct inhibitor of Bcl-2 are not available. The motivations for this review are: to provide the basis for the development of novel compounds that modulate Bcl-2 expression using celecoxib as a structural starting point and to encourage additional biological studies (such as binding and enzymatic assays) that would provide information regarding celecoxib's role as a Bcl-2 antagonist. The current review summarizes work that identifies the role of celecoxib in blocking the activity of Bcl-2.

SUBMITTER: Winfield LL

PROVIDER: S-EPMC3398981 | biostudies-literature | 2012 Mar

REPOSITORIES: biostudies-literature

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Celecoxib and Bcl-2: emerging possibilities for anticancer drug design.

Winfield Leyte L LL Payton-Stewart Florastina F

Future medicinal chemistry 20120301 3

Celecoxib is a multifaceted drug with promising anticancer properties. A number of studies have been conducted that implicate the compound in modulating the expression of Bcl-2 family members and mitochondria-mediated apoptosis. The growing data surrounding the role of celecoxib in the regulation of the mitochondrial death pathway provides a platform for ongoing debate. Studies that describe celecoxib's properties as a BH3 mimic or as a direct inhibitor of Bcl-2 are not available. The motivation ...[more]

PMID: 22393942

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