کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1361432 | 981463 | 2008 | 10 صفحه PDF | دانلود رایگان |
The inhibition of methyltransferases is currently of high interest, particularly in the areas of microbial infection and cell proliferation, as there have been serious attempts to develop novel anti-microbial agents. In the present investigation, a series of 11 S-adenosyl-l-homocysteine analogues have been synthesized and effect of these analogues on DNA methylation catalyzed by DNA methyltransferases was studied. It was found that, while 5′-S-(propionic acid)5′-deoxy-9-(1′-β-d-ribofuranosyl)1,3-dideazaadenine was an activator of EcoP15I and HhaI DNA methyltransferases, 5′-S-(propionic acid)5′-deoxy-9-(1′-β-dribofuranosyl)adenine inhibited the methyltransferases in a non-competitive manner. An understanding of the binding of analogues to DNA methyltransferases will greatly assist the design of novel anti-microbial compounds.
A series of 11 AdoHcy analogues were synthesized and evaluated for their modulating effects on DNA methylation catalyzed by DNA methyltransferases.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry - Volume 16, Issue 5, 1 March 2008, Pages 2276–2285