Document Type

Journal Article

Department/Unit

Department of Chemistry

Title

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

Language

English

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 Date

8-31-2015

Source Publication Title

Journal of Medicinal Chemistry

Volume

58

Issue

16

Start Page

6697

End Page

6703

Publisher

American Chemical Society

Peer Reviewed

1

DOI

10.1021/acs.jmedchem.5b00375

Link to Publisher's Edition

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

ISSN (print)

00222623

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