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

Tian Shu Kang, Zhifeng Mao, Chan Tat Ng, Modi Wang, Wanhe Wang, Chunming Wang, Simon Ming Yuen Lee, Yitao Wang, Chung Hang Leung*, Edmond Dik Lung MA

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

38 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)4026-4031
Number of pages6
JournalJournal of Medicinal Chemistry
Volume59
Issue number8
DOIs
Publication statusPublished - 28 Apr 2016

Scopus Subject Areas

  • Molecular Medicine
  • Drug Discovery

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