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Mechanism‐Based Inhibitor of DNA Cytosine‐5 Methyltransferase by a SNAr Reaction with an Oligodeoxyribonucleotide Containing a 2‐Amino‐4‐Halopyridine‐C‐Nucleoside
ChemBioChem ( IF 3.2 ) Pub Date : 2018-03-14 , DOI: 10.1002/cbic.201700688
Kousuke Sato 1 , Yuma Kunitomo 2 , Yukiko Kasai 2 , Shohei Utsumi 2 , Isao Suetake 3 , Shoji Tajima 3 , Satoshi Ichikawa 2, 4 , Akira Matsuda 2, 4
Affiliation  

SNAr reaction on DNMTs: Oligodeoxyribonucleotides containing 2‐amino‐4‐halopyridine‐C‐nucleosides (dXP) at the CpG site form a covalent complex with DNA cytosine‐5 methyltransferases (DNMTs) through a nucleophilic aromatic substitution (SNAr) reaction. DNA containing dXP in a CpG sequence could be a useful chemical probe for studies of epigenetics and a potential nucleic acid drug lead in cancer chemotherapy.
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中文翻译:

基于机制的DNA胞嘧啶5甲基转移酶抑制剂通过SNAr反应与包含2-氨基-4-卤代吡啶-C-核苷的寡脱氧核糖核苷酸的反应

小号Ñ上转移酶的Ar反应:含有寡脱氧核糖核苷酸的2-氨基-4- halopyridine- Ç核苷(d X P)在CpG位点形成复合物与DNA胞嘧啶-5-甲基转移酶(转移酶)通过亲核芳族取代的共价(S Ñ Ar)反应。CpG序列中含有d X P的DNA可能是用于研究表观遗传学的有用化学探针,并可能成为癌症化学疗法中潜在的核酸药物。
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更新日期:2018-03-14
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