jm6b00112_si_002.csv (3.27 kB)
Identification of an Iridium(III)-Based Inhibitor of Tumor Necrosis Factor‑α
dataset
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 MaThe
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.