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Celecoxib and Bcl-2: Emerging possibilities for anticancer drug design

机译:Celecoxib和Bcl-2:抗癌药物设计的新兴可能性

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摘要

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.
机译:塞来昔布是具有前景的抗癌特性的多方面药物。已经进行了许多研究,暗示该化合物调节Bcl-2家族成员的表达和线粒体介导的细胞凋亡。围绕塞来昔布在线粒体死亡途径调控中作用的越来越多的数据为正在进行的辩论提供了平台。尚无描述塞来昔布作为BH3模拟物或作为Bcl-2直接抑制剂的特性的研究。这篇综述的目的是:为开发新化合物提供基础,这些新化合物以塞来昔布为结构起点来调节Bcl-2表达,并鼓励进行其他生物学研究(例如结合和酶法测定),以提供有关塞来昔布的信息。作为Bcl-2拮抗剂。本综述总结了确定塞来昔布在阻断Bcl-2活性中的作用的工作。

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