Targeting epigenetic regulators to overcome drug resistance in cancers

N Wang, T Ma, B Yu - Signal transduction and targeted therapy, 2023 - nature.com
Drug resistance is mainly responsible for cancer recurrence and poor prognosis. Epigenetic
regulation is a heritable change in gene expressions independent of nucleotide sequence …

An update of epigenetic drugs for the treatment of cancers and brain diseases: a comprehensive review

Z Sahafnejad, S Ramazi, A Allahverdi - Genes, 2023 - mdpi.com
Epigenetics has long been recognized as a significant field in biology and is defined as the
investigation of any alteration in gene expression patterns that is not attributed to changes in …

SETD7 functions as a transcription repressor in prostate cancer via methylating FOXA1

Z Wang, J Petricca, M Liu, S Zhang… - Proceedings of the …, 2023 - National Acad Sciences
Dysregulation of histone lysine methyltransferases and demethylases is one of the major
mechanisms driving the epigenetic reprogramming of transcriptional networks in castration …

[HTML][HTML] A lncRNA from the FTO locus acts as a suppressor of the m6A writer complex and p53 tumor suppression signaling

J Zhang, J Wei, R Sun, H Sheng, K Yin, Y Pan… - Molecular cell, 2023 - cell.com
Summary N 6-methyladenosine (m 6 A) of mRNAs modulated by the METTL3-METTL14-
WTAP-RBM15 methyltransferase complex and m 6 A demethylases such as FTO play …

In vivo inhibition of nuclear ACE2 translocation protects against SARS-CoV-2 replication and lung damage through epigenetic imprinting

WJ Tu, M Melino, J Dunn, RD McCuaig… - Nature …, 2023 - nature.com
In vitro, ACE2 translocates to the nucleus to induce SARS-CoV-2 replication. Here, using
digital spatial profiling of lung tissues from SARS-CoV-2-infected golden Syrian hamsters …

LSD1 inhibitors for cancer treatment: Focus on multi-target agents and compounds in clinical trials

B Noce, E Di Bello, R Fioravanti, A Mai - Frontiers in pharmacology, 2023 - frontiersin.org
Histone lysine-specific demethylase 1 (LSD1/KDM1A) was first identified in 2004 as an
epigenetic enzyme able to demethylate specific lysine residues of histone H3, namely …

Triazole-fused pyrimidines in target-based anticancer drug discovery

XJ Dai, LP Xue, SK Ji, Y Zhou, Y Gao, YC Zheng… - European Journal of …, 2023 - Elsevier
In recent decades, the development of targeted drugs has featured prominently in the
treatment of cancer, which is among the major causes of mortality globally. Triazole-fused …

LSD1/PRMT6-targeting gene therapy to attenuate androgen receptor toxic gain-of-function ameliorates spinobulbar muscular atrophy phenotypes in flies and mice

R Prakasam, A Bonadiman, R Andreotti… - Nature …, 2023 - nature.com
Spinobulbar muscular atrophy (SBMA) is caused by CAG expansions in the androgen
receptor gene. Androgen binding to polyQ-expanded androgen receptor triggers SBMA …

Methylation across the central dogma in health and diseases: new therapeutic strategies

R Liu, E Zhao, H Yu, C Yuan, MN Abbas… - Signal Transduction and …, 2023 - nature.com
The proper transfer of genetic information from DNA to RNA to protein is essential for cell-
fate control, development, and health. Methylation of DNA, RNAs, histones, and non-histone …

Lysine-specific demethylase 1 promises to be a novel target in cancer drug resistance: therapeutic implications

FF Yang, XL Xu, T Hu, JQ Liu, JZ Zhou… - Journal of Medicinal …, 2023 - ACS Publications
Chemotherapy, targeted therapy, and immunotherapy are effective against most tumors, but
drug resistance remains a barrier to successful treatment. Lysine-specific demethylase 1 …