2015
DOI: 10.1021/acs.jmedchem.5b00375
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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 i… Show more

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Cited by 60 publications
(32 citation statements)
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“…Many non-platinum metal complexes, such as copper, ruthenium and osmium complexes, show promising anti-proliferative activities12. As demonstrated by Sadler, Meggers and Ma et al ., organometallic Ir(III) complexes can also exert potent anticancer activities through catalyzing cellular redox reactions, inhibiting protein activities or protein-protein interactions34567.…”
mentioning
confidence: 99%
“…Many non-platinum metal complexes, such as copper, ruthenium and osmium complexes, show promising anti-proliferative activities12. As demonstrated by Sadler, Meggers and Ma et al ., organometallic Ir(III) complexes can also exert potent anticancer activities through catalyzing cellular redox reactions, inhibiting protein activities or protein-protein interactions34567.…”
mentioning
confidence: 99%
“…Most forms of disseminated tumors are currently untreatable, although developments in chemotherapy over the past years have led to the treatment of various cancers (Thota et al, 2018). Cis-platin exerts good and broad-spectrum anticancer effects (Deubel and Lau, 2006;Romero-Canelón and Sadler, 2013;Muhammad and Guo, 2014), but, when used extensively, platinum-based drugs may promote drug resistance and instability; become insoluble in biological media; and become toxic to blood and gastrointestinal tract (Ma et al, 2014;Liu et al, 2015). Thus, various organometallic anticancer drugs, such as tin, iridium, ruthenium, and osmium anticancer complexes, have been developed (Sun and Che, 2009;Lu et al, 2015;Zeng et al, 2017;Ge et al, 2019;Li et al, 2019).…”
Section: Introductionmentioning
confidence: 99%
“…An essential step in this process is the identification of interactions between drugs and pharmacological targets. Although the existence of interactions can be reliably confirmed by in vitro binding assays, see e.g., [2][3][4][5], such methods are expensive and time consuming [6]. In order to address this bottleneck, computational approaches have been designed and implemented for the estimation of the probability of interactions.…”
Section: Introductionmentioning
confidence: 99%