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Sulfocoumarins as dual inhibitors of human carbonic anhydrase isoforms IX/XII and of human thioredoxin reductase.
Journal of Enzyme inhibition and Medicinal Chemistry ( IF 5.6 ) Pub Date : 2020-01-13 , DOI: 10.1080/14756366.2020.1712596
Mikhail Krasavin 1 , Raivis Žalubovskis 2, 3 , Aiga Grandāne 2 , Ilona Domračeva 2 , Petr Zhmurov 1 , Claudiu T Supuran 4
Affiliation  

The hypothesis that sulfocoumarin acting as inhibitors of human carbonic anhydrase (CA, EC 4.2.1.1) cancer-associated isoforms hCA IX and - hCA XII is being able to also inhibit thioredoxin reductase was verified and confirmed. The dual targeting of two cancer cell defence mechanisms, i.e. hypoxia and oxidative stress, may both contribute to the observed antiproliferative profile of these compounds against many cancer cell lines. This unprecedented dual anticancer mechanism may lead to a new approach for designing innovative therapeutic agents.

中文翻译:

磺香豆素是人碳酸酐酶同工型IX / XII和人硫氧还蛋白还原酶的双重抑制剂。

证实并证实了硫代香豆素可作为人类碳酸酐酶抑制剂(CA,EC 4.2.1.1)与癌症相关的亚型hCA IX和-hCA XII的抑制剂也能抑制硫氧还蛋白还原酶的假说。两种癌细胞防御机制(即缺氧和氧化应激)的双重靶向可能都有助于观察到的这些化合物对多种癌细胞的抗增殖作用。这种前所未有的双重抗癌机制可能会导致设计创新治疗剂的新方法。
更新日期:2020-04-20
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