Evaluation of the Interactions of Cabozantinib with Topoisomerase Enzymes by in vitro Enzyme Activity Assays, and its Effects on Cancer Cell Proliferation

Feyza Oflaz, Naz Ünal, Burcin Gungor, Pakize Cantürk
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Abstract

The discovery of many drugs in recent years provides a definitive solution in the treatment of various diseases, but today, despite the discovery of many effective anticancer drugs, there are various types of cancer that have limitations in treatment and are still not completely curable. Since most of these limitations are due to cancer cells gaining resistance or compounds only being effective in certain types of cancer cells, the search for more effective anticancer drugs that are also effective in these types of cancer is inevitable. Cabozantinib is in medical use as a highly effective anticancer drug in various types of cancer, such as medullary thyroid cancer and kidney cancer. The anticancer properties of the Cabozantinib compound have attracted more attention in recent years, however, more studies are needed to define the anticancer activities of this compound. In our study, the interactions of Cabozantinib with topoisomerase enzymes, were demonstrated through in vitro enzyme activity tests, and the anti-proliferative effect of Cabozantinib was studied on MCF7, A549 and PC3 cell lines. By analyzing the interactions of the Cabozantinib with topoisomerases, the action mechanisms of the compound at the molecular level was evaluated.
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通过体外酶活性测定评估卡博替尼与拓扑异构酶的相互作用及其对癌细胞增殖的影响
近年来,许多药物的发现为各种疾病的治疗提供了明确的解决方案,但如今,尽管发现了许多有效的抗癌药物,但仍有各种类型的癌症在治疗上存在局限性,仍无法完全治愈。由于这些局限性大多是由于癌细胞产生抗药性或化合物只对某些类型的癌细胞有效,因此,寻找对这些类型的癌症同样有效的更有效的抗癌药物是不可避免的。卡博替尼(Cabozantinib)作为一种高效抗癌药物,已被用于治疗甲状腺髓样癌和肾癌等多种癌症。近年来,卡博替尼(Cabozantinib)化合物的抗癌特性引起了越来越多的关注,但要明确该化合物的抗癌活性还需要更多的研究。在我们的研究中,我们通过体外酶活性测试证明了Cabozantinib与拓扑异构酶的相互作用,并研究了Cabozantinib对MCF7、A549和PC3细胞系的抗增殖作用。通过分析 Cabozantinib 与拓扑异构酶的相互作用,评估了该化合物在分子水平上的作用机制。
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审稿时长
10 weeks
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