Document Type

Journal Article

Department/Unit

Department of Chemistry

Title

An iridium(III) complex inhibits JMJD2 activities and acts as a potential epigenetic modulator

Abstract

A novel iridium(III) complex was synthesized and evaluated for its ability to target JMJD2 enzymatic activity. The iridium(III) complex 1 can inhibit JMJD2 activity and was selective for JMJD2 activity over JARID, JMJD3, and HDAC activities. Moreover, 1 suppressed the trimethylation of the p21 promoter on H3K9me3 and interrupted the JMJD2D–H3K9me3 interactions in human cells, suggesting that it could act as an epigenetic modulator. To our knowledge, 1 represents the first metal-based JMJD2 inhibitor reported in the literature.

Publication Year

2015

Journal Title

Journal of Medicinal Chemistry

Volume number

58

Issue number

16

Publisher

American Chemical Society

First Page (page number)

6697

Last Page (page number)

6703

Referreed

1

DOI

10.1021/acs.jmedchem.5b00375

ISSN (print)

00222623

Link to Publisher’s Edition

http://dx.doi.org/10.1021/acs.jmedchem.5b00375

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