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环氧化酶-2抑制剂:乳腺癌治疗的新策略。

COX-2 inhibitors: a novel strategy in the management of breast cancer.

作者信息

Regulski Miłosz, Regulska Katarzyna, Prukała Wiesław, Piotrowska Hanna, Stanisz Beata, Murias Marek

机构信息

Poznan University of Medical Sciences, Chair and Department of Toxicology, 30th Dojazd Street, 60-631 Poznań, Poland.

Greater Poland Oncology Center, 15th Garbary Street, 61-866 Poznań, Poland.

出版信息

Drug Discov Today. 2016 Apr;21(4):598-615. doi: 10.1016/j.drudis.2015.12.003. Epub 2015 Dec 23.

Abstract

Cyclooxygenase-2 (COX-2) inhibitors are common anti-inflammatory drugs with pleiotropic, endogenous actions that could be useful in the management of breast cancer. Here, we provide a complete understanding of the biochemistry of COX-2 and discuss the various molecular mechanisms behind its increased expression in breast cancer. We also analyze the possible mechanisms responsible for the anticancer effect of COX-2 inhibitors and provide an overview of the available preclinical and clinical data on the use of COX-2 inhibitors in breast cancer. Finally, we describe a mathematical model of the relation between the structure and biological potency of promising new COX-2 inhibitors (trans-stilbenes) using a 2D quantitative structure-activity relationship (QSAR) technique.

摘要

环氧化酶-2(COX-2)抑制剂是一类常见的具有多种内源性作用的抗炎药物,可能对乳腺癌的治疗有益。在此,我们全面阐述了COX-2的生物化学特性,并探讨了其在乳腺癌中表达增加背后的各种分子机制。我们还分析了COX-2抑制剂抗癌作用的可能机制,并概述了关于在乳腺癌中使用COX-2抑制剂的现有临床前和临床数据。最后,我们使用二维定量构效关系(QSAR)技术描述了有前景的新型COX-2抑制剂(反式芪类)的结构与生物活性之间关系的数学模型。

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