[HTML][HTML] N6-methyladenosine links RNA metabolism to cancer progression

D Dai, H Wang, L Zhu, H Jin, X Wang - Cell death & disease, 2018 - nature.com
Abstract N6-methyladenosine (m6A) is the most abundant mRNA modification. With the
development of antibody-based sequencing technologies and the findings of m6A-related …

Targeting metalloenzymes for therapeutic intervention

AY Chen, RN Adamek, BL Dick, CV Credille… - Chemical …, 2018 - ACS Publications
Metalloenzymes are central to a wide range of essential biological activities, including
nucleic acid modification, protein degradation, and many others. The role of metalloenzymes …

Chromatin histone modifications and rigidity affect nuclear morphology independent of lamins

AD Stephens, PZ Liu, EJ Banigan… - Molecular biology of …, 2018 - Am Soc Cell Biol
Nuclear shape and architecture influence gene localization, mechanotransduction,
transcription, and cell function. Abnormal nuclear morphology and protrusions termed …

Meclofenamic acid selectively inhibits FTO demethylation of m6A over ALKBH5

Y Huang, J Yan, Q Li, J Li, S Gong, H Zhou… - Nucleic acids …, 2015 - academic.oup.com
Two human demethylases, the fat mass and obesity-associated (FTO) enzyme and ALKBH5,
oxidatively demethylate abundant N 6-methyladenosine (m6A) residues in mRNA …

Epigenetic protein families: a new frontier for drug discovery

CH Arrowsmith, C Bountra, PV Fish, K Lee… - Nature reviews Drug …, 2012 - nature.com
Epigenetic regulation of gene expression is a dynamic and reversible process that
establishes normal cellular phenotypes but also contributes to human diseases. At the …

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 …

Histone modifications in epigenetic regulation of cancer: Perspectives and achieved progress

ME Neganova, SG Klochkov, YR Aleksandrova… - Seminars in Cancer …, 2022 - Elsevier
Epigenetic changes associated with histone modifications play an important role in the
emergence and maintenance of the phenotype of various cancer types. In contrast to direct …

Development of Cell-Active N6-Methyladenosine RNA Demethylase FTO Inhibitor

B Chen, F Ye, L Yu, G Jia, X Huang… - Journal of the …, 2012 - ACS Publications
The direct nucleic acid repair dioxygenase FTO is an enzyme that demethylates N 6-
methyladenosine (m6A) residues in mRNA in vitro and inside cells. FTO is the first RNA …

Advances in histone demethylase KDM4 as cancer therapeutic targets

DH Lee, GW Kim, YH Jeon, J Yoo, SW Lee… - The FASEB …, 2020 - Wiley Online Library
Abstract The KDM4 subfamily H3K9 histone demethylases are epigenetic regulators that
control chromatin structure and gene expression by demethylating histone H3K9, H3K36 …

Recent progress in histone demethylase inhibitors

TE McAllister, KS England, RJ Hopkinson… - Journal of medicinal …, 2016 - ACS Publications
There is increasing interest in targeting histone N-methyl-lysine demethylases (KDMs) with
small molecules both for the generation of probes for target exploration and for therapeutic …