Regulski Miłosz, Regulska Katarzyna, Prukała Wiesław, Piotrowska Hanna, Stanisz Beata, Murias Marek
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.
Drug Discov Today. 2016 Apr;21(4):598-615. doi: 10.1016/j.drudis.2015.12.003. Epub 2015 Dec 23.
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.
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。
