Inhibitors of protein methyltransferases and demethylases

HU Kaniskan, ML Martini, J Jin - Chemical reviews, 2018 - ACS Publications
Post-translational modifications of histones by protein methyltransferases (PMTs) and
histone demethylases (KDMs) play an important role in the regulation of gene expression …

KDM4B as a target for prostate cancer: structural analysis and selective inhibition by a novel inhibitor

CH Chu, LY Wang, KC Hsu, CC Chen… - Journal of medicinal …, 2014 - ACS Publications
The KDM4/JMJD2 Jumonji C-containing histone lysine demethylases (KDM4A–KDM4D),
which selectively remove the methyl group (s) from tri/dimethylated lysine 9/36 of H3 …

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

LJ Liu, L Lu, HJ Zhong, B He, DWJ Kwong… - Journal of medicinal …, 2015 - ACS Publications
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 …

Activity of epigenetic inhibitors against Plasmodium falciparum asexual and sexual blood stages

LN Vanheer, H Zhang, G Lin… - Antimicrobial agents and …, 2020 - Am Soc Microbiol
Earlier genetic and inhibitor studies showed that epigenetic regulation of gene expression is
critical for malaria parasite survival in multiple life stages and a promising target for new …

Docking and linking of fragments to discover jumonji histone demethylase inhibitors

M Korczynska, DD Le, N Younger… - Journal of medicinal …, 2016 - ACS Publications
Development of tool molecules that inhibit Jumonji demethylases allows for the investigation
of cancer-associated transcription. While scaffolds such as 2, 4-pyridinedicarboxylic acid (2 …

JIB-04 has broad-spectrum antiviral activity and inhibits SARS-CoV-2 replication and coronavirus pathogenesis

J Son, S Huang, Q Zeng, TL Bricker, JB Case, J Zhou… - MBio, 2022 - Am Soc Microbiol
Pathogenic coronaviruses are a major threat to global public health. Here, using a
recombinant reporter virus-based compound screening approach, we identified small …

JIB-04, an inhibitor of Jumonji histone demethylase as a potent antitubercular agent against Mycobacterium tuberculosis

P Li, Q Huang, Y Xie, Z Zhu, S Zhan, J Meng… - Archives of …, 2024 - Springer
The increasing drug resistance of Mycobacterium tuberculosis (Mtb), coupled with the
limited availability of effective anti-tuberculosis medications, poses significant challenges for …

Identification of small molecule modulators of gene transcription with anticancer activity

TA Tran, J Wichterman-Kouznetsova… - ACS chemical …, 2014 - ACS Publications
Epigenetic regulation of gene expression is essential in many biological processes, and its
deregulation contributes to pathology including tumor formation. We used an image-based …