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

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posted on 2016-04-07, 00:00 authored by 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
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.

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