Identification of novel inhibitors of DNA methylation by screening of a chemical library

A Ceccaldi, A Rajavelu, S Ragozin… - ACS chemical …, 2013 - ACS Publications
In order to discover new inhibitors of the DNA methyltransferase 3A/3L complex, we used a
medium-throughput nonradioactive screen on a random collection of 1120 small organic …

[HTML][HTML] Substituted anthraquinones represent a potential scaffold for DNA methyltransferase 1-specific inhibitors

RL Switzer, J Medrano, DA Reedel, J Weiss - PLoS One, 2019 - journals.plos.org
In humans, the most common epigenetic DNA modification is methylation of the 5-carbon of
cytosines, predominantly in CpG dinucleotides. DNA methylation is an important epigenetic …

Identification and optimization of hydrazone-gallate derivatives as specific inhibitors of DNA methyltransferase 3A

A Erdmann, Y Menon, C Gros, V Masson… - Future Medicinal …, 2016 - Taylor & Francis
DNA methylation is the most studied epigenetic event. Since the methylation profile of the
genome is widely modified in cancer cells, DNA methyltransferases are the target of new …

Discovery and optimization of inhibitors of DNA methyltransferase as novel drugs for cancer therapy

J Yoo, JL Medina-Franco - … —A Case Study Based Insight into …, 2011 - books.google.com
The genome contains genetic and epigenetic information. While the genome provides the
blueprint for the manufacture of all the proteins required to create a living thing, the …

Novel and selective DNA methyltransferase inhibitors: Docking-based virtual screening and experimental evaluation

D Kuck, N Singh, F Lyko, JL Medina-Franco - Bioorganic & medicinal …, 2010 - Elsevier
The DNA methyltransferase (DNMT) enzyme family consists of four members with diverse
functions and represents one of the most promising targets for the development of novel …

Epigenetic relevant chemical space: a chemoinformatic characterization of inhibitors of DNA methyltransferases

E Fernández-de Gortari, JL Medina-Franco - Rsc Advances, 2015 - pubs.rsc.org
DNA methylation is an epigenetic mechanism mediated by a family of proteins called DNA
methyltransferases (DNMTs). The misregulation of the covalent modification of DNA through …

Design and synthesis of new non nucleoside inhibitors of DNMT3A

A Erdmann, Y Menon, C Gros, N Molinier… - Bioorganic & Medicinal …, 2015 - Elsevier
DNA methylation, an epigenetic modification regulating gene expression, is a promising
target in cancer. In an effort to identify new non nucleosidic inhibitors of DNA …

Synthesis and characterization of transition-state analogue inhibitors against human DNA methyltransferase 1

F Lamiable-Oulaidi, RK Harijan… - Journal of medicinal …, 2022 - ACS Publications
Hypermethylation of CpG regions by human DNA methyltransferase 1 (DNMT1) silences
tumor-suppression genes, and inhibition of DNMT1 can reactivate silenced genes. The 5 …

Developing new chemical tools for DNA methyltransferase 1 (DNMT 1): a small-molecule activity-based probe and novel tetrazole-containing inhibitors

B Zhu, J Ge, SQ Yao - Bioorganic & Medicinal Chemistry, 2015 - Elsevier
DNA methylation is an important epigenetic modification catalyzed by DNA
methyltransferases (DNMTs). Abnormal expression of endogenous DNMTs in human …

Identifying novel selective non-nucleoside DNA methyltransferase 1 inhibitors through docking-based virtual screening

S Chen, Y Wang, W Zhou, S Li, J Peng… - Journal of Medicinal …, 2014 - ACS Publications
The DNA methyltransferases (DNMTs) found in mammals include DNMT1, DNMT3A, and
DNMT3B and are attractive targets in cancer chemotherapy. DNMT1 was the first among the …