Document Type

Journal Article

Department/Unit

Department of Chemistry

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.

Publication Year

2016

Journal Title

Journal of Medicinal Chemistry

Volume number

59

Issue number

8

Publisher

American Chemical Society

First Page (page number)

4026

Last Page (page number)

4031

Referreed

1

DOI

10.1021/acs.jmedchem.6b00112

ISSN (print)

00222623

Link to Publisher’s Edition

http://dx.doi.org/10.1021/acs.jmedchem.6b00112

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