title: Identification of an Iridium(III)-Based Inhibitor of Tumor Necrosis Factor-α.
abstract: 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.
authors.affiliation: State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau , Taipa, Macao, P. R. China.
authors.forename: Tian-Shu
authors.initials: TS
authors.lastname: Kang
authors.affiliation: Department of Chemistry, Hong Kong Baptist University , Kowloon Tong, Hong Kong, P. R. China.
authors.forename: Zhifeng
authors.initials: Z
authors.lastname: Mao
authors.affiliation: State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau , Taipa, Macao, P. R. China.
authors.forename: Chan-Tat
authors.initials: CT
authors.lastname: Ng
authors.affiliation: Department of Chemistry, Hong Kong Baptist University , Kowloon Tong, Hong Kong, P. R. China.
authors.forename: Modi
authors.initials: M
authors.lastname: Wang
authors.affiliation: Department of Chemistry, Hong Kong Baptist University , Kowloon Tong, Hong Kong, P. R. China.
authors.forename: Wanhe
authors.initials: W
authors.lastname: Wang
authors.affiliation: State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau , Taipa, Macao, P. R. China.
authors.forename: Chunming
authors.initials: C
authors.lastname: Wang
authors.affiliation: State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau , Taipa, Macao, P. R. China.
authors.forename: Simon Ming-Yuen
authors.initials: SM
authors.lastname: Lee
authors.affiliation: State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau , Taipa, Macao, P. R. China.
authors.forename: Yitao
authors.initials: Y
authors.lastname: Wang
authors.affiliation: State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau , Taipa, Macao, P. R. China.
authors.forename: Chung-Hang
authors.initials: CH
authors.lastname: Leung
authors.affiliation: Department of Chemistry, Hong Kong Baptist University , Kowloon Tong, Hong Kong, P. R. China.
authors.forename: Dik-Lung
authors.initials: DL
authors.lastname: Ma
mesh_terms: D056945:Hep G2 Cells; D006801:Humans; D007495:Iridium / Q000494:pharmacology*; D016328:NF-kappa B / Q000378:metabolism; D011485:Protein Binding; D018124:Receptors, Tumor Necrosis Factor / Q000378:metabolism; D015398:Signal Transduction; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors*
chemical_list: D016328:NF-kappa B; D018124:Receptors, Tumor Necrosis Factor; D014409:Tumor Necrosis Factor-alpha; D007495:Iridium