Toward anticancer gold-based compounds targeting PARP-1: a new case study
Toward anticancer gold-based compounds targeting PARP-1: a new case study
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DOI：
10.1039/c6ra11606j
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发表时间：
2016-01-01
期刊：
影响因子：
3.9
通讯作者：
Casini, A.
中科院分区：
文献类型：
--
作者：
Citta, A.;Scalcon, V.;Casini, A.
合成了一种新的含2-（（2,2'-联吡啶）-5-基）- 1h -苯并咪唑-4-羧酰胺配体的金（III）配合物，并对其体外生物学性质进行了表征。除了显示出对人类癌细胞的有希望的抗增殖作用外，该化合物还能有效和选择性地抑制锌指蛋白PARP-1，相对于硒酶硫氧还蛋白还原酶。这一结果为设计新的金基抗癌药物提供了希望，这些药物可以破坏PARP-1的功能并用于联合治疗。
A new gold(III) complex bearing a 2-((2,2'-bipyridin)-5-yl)-1H-benzimidazol-4-carboxamide ligand has been synthesized and characterized for its biological properties in vitro. In addition to showing promising antiproliferative effects against human cancer cells, the compound potently and selectively inhibits the zinc finger protein PARP-1, with respect to the seleno-enzyme thioredoxin reductase. The results hold promise for the design of novel gold-based anticancer agents disrupting PARP-1 function and to be used in combination therapies.