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Activation and inhibition of DNA methyltransferases by S-adenosyl-$L$-homocysteine analogues

Kumar, Ritesh and Srivastava, Richa and Singh, Ramendra Kumar and Surolia, Avadhesha and Rao, Desirazu N (2008) Activation and inhibition of DNA methyltransferases by S-adenosyl-$L$-homocysteine analogues. In: Bioorganic & Medicinal Chemistry, 16 (5). pp. 2276-2285.

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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 $5^{\prime}$-S-(propionic acid)$5^{\prime}$-deoxy-9-($1^{\prime}$-\beta-$D$-ribofuranosyl)1,3-dideazaadenine was an activator of EcoP15I and HhaI DNA methyltransferases, $5^{\prime}$-S-(propionic acid)$5^{\prime}$-deoxy-9-($1^{\prime}$-\beta-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.

Item Type: Journal Article
Publication: Bioorganic & Medicinal Chemistry
Publisher: Elsevier
Additional Information: Copyright of this article belongs to Elsevier.
Department/Centre: Division of Biological Sciences > Molecular Biophysics Unit
Division of Biological Sciences > Biochemistry
Date Deposited: 12 May 2008
Last Modified: 19 Sep 2010 04:44
URI: http://eprints.iisc.ac.in/id/eprint/13945

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