Carboxylated acyclonucleosides: synthesis and RNase A inhibition

Chakraborty, Kaustav ; Dasgupta, Swagata ; Pathak, Tanmaya (2015) Carboxylated acyclonucleosides: synthesis and RNase A inhibition Molecules, 20 (4). pp. 5924-5941. ISSN 1420-3049


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Strategically designed carboxylated acyclonucleosides have been probed as a new class of RNase A inhibitors. Several experimental and theoretical studies have been performed to compile relevant qualitative and quantitative information regarding the nature and extent of inhibition. The inhibition constant (Ki) values were determined using a UV-based kinetics experiment. The changes in the secondary structure of the enzyme upon binding with the inhibitors were obtained from circular dichroism studies. The binding constants for enzyme-inhibitor interactions were determined with the help of fluorescence spectroscopy. Docking studies were performed to reveal the possible binding sites of the inhibitors within the enzyme. The cytosine analogues were found to possess better inhibitory properties in comparison to the corresponding uracil derivatives. An increment in the number of carboxylic acid groups (-COOH) in the inhibitor backbone was found to result in better inhibition.

Item Type:Article
Source:Copyright of this article belongs to Molecular Diversity Preservation International.
Keywords:Acyclonucleosides; RNase A; Inhibition; Kinetics; Docking
ID Code:103742
Deposited On:22 Mar 2017 05:56
Last Modified:22 Mar 2017 05:56

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