Identification of an Iridium(III)-Based Inhibitor of Tumor Necrosis Factor-α

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• 作者：Tian-Shu Kang ; Zhifeng Mao ; Chan-Tat Ng ; Modi Wang ; Wanhe Wang ; Chunming Wang ; Simon Ming-Yuen Lee ; Yitao Wang ; Chung-Hang Leung ; Dik-Lung Ma
• 刊名：Journal of Medicinal Chemistry
• 出版年：2016
• 出版时间：April 28, 2016
• 年：2016
• 卷：59
• 期：8
• 页码：4026-4031
• 全文大小：341K
• 年卷期：0
• ISSN：1520-4804

文摘

The novel iridium(III) complex 1 was verified as a potent inhibitor of the TNF-α–TNFR protein–protein interaction in vitro and in cellulo. The iridium(III) center plays a critical role in organizing the structure of the bioactive metal complex, as the isolated ligands were found to be completely inactive. Both iridium enantiomers inhibited TNF-α-induced NF-κB activity and TNF-α–TNFR binding. 1 represents a promising scaffold for the further development of more potent organometallic TNF-α inhibitors.