Cover image for Vol. 19 Issue 4

Editor: Ruben Ragg; Editorial Board Chairs: Thomas Carell, Donald Hilvert, Barbara Imperiali

Online ISSN: 1439-7633

Associated Title(s): ChemCatChem, ChemMedChem, ChemPhysChem, ChemSusChem

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February 15, 2018

Very Important Paper: Mechanism-based Inhibitor of DNA Cytosine-5 Methyltransferase (DNMT) via a SNAr Reaction with an Oligodeoxyribonucleotide Containing 2-Amino-4-Halopyridine-C-Nucleoside (dXP)

Very Important Paper: Mechanism-based Inhibitor of DNA Cytosine-5 Methyltransferase (DNMT) via a SNAr Reaction with an Oligodeoxyribonucleotide Containing 2-Amino-4-Halopyridine-C-Nucleoside (dXP) Kousuke Sato,* Yuma Kunitomo, Yukiko Kasai, Shohei Utsumi, Isao Suetake, Shoji Tajima, Satoshi Ichikawa, Akira Matsuda

Inhibition of human DNA cytosine-5 methyltransferase (DNMT), which is responsible for generating 5-methylcytosine in CpG sequences, is an effective strategy to treat various cancers. Sato (Health Sciences University of Hokkaido, Japan) and co-workers describe the design, synthesis, and evaluation of the properties of 2-amino-4-halopyridine-C-nucleosides (dXP) and oligodeoxyribonucleotides (ODNs) containing dXP as a novel mechanism-based inhibitor of DNMTs. The ODN forms a complex with DNMTs via covalent bonding through a nucleophilic aromatic substitution (SNAr) reaction. This study suggests that dXP in a CpG sequence of DNA could serve as a potential nucleic acid drug lead in cancer chemotherapy and a useful chemical probe for epigenetic studies.

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