Identification of an iridium(III)-based inhibitor of tumor necrosis factor-α
Department of Chemistry
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.
Source Publication Title
Journal of Medicinal Chemistry
American Chemical Society
Link to Publisher's Edition
Kang, T., Mao, Z., Ng, C., Wang, M., Wang, W., Wang, C., Lee, S., Wang, Y., Leung, C., & Ma, D. (2016). Identification of an iridium(III)-based inhibitor of tumor necrosis factor-α. Journal of Medicinal Chemistry, 59 (8). https://doi.org/10.1021/acs.jmedchem.6b00112