Ghosh, Kalyan S. ; Debnath, Joy ; Dutta, Palash ; Sahoo, Bijaya K. ; Dasgupta, Swagata (2008) Exploring the potential of 3′-O-carboxy esters of thymidine as inhibitors of ribonuclease A and angiogenin Bioorganic & Medicinal Chemistry, 16 (6). pp. 2819-2828. ISSN 0968-0896
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Official URL: https://www.sciencedirect.com/science/article/pii/...
Related URL: http://dx.doi.org/10.1016/j.bmc.2008.01.003
Abstract
In this study, compounds with a carboxy ester in lieu of the phosphate ester at the 3′-position have been employed to inhibit the ribonucleolytic activity of ribonuclease A (RNase A). Phosphates at the 3′-position of pyrimidine bases are well-known inhibitors of the protein. We have investigated the inhibition of RNase A by 3′-O-carboxy esters of thymidine. The compounds behave as competitive inhibitors with inhibition constants ranging from 42 to 95 μM. The mode of inhibition has also been confirmed by 1H NMR studies of the active site histidines of RNase A. Docking studies have further substantiated the experimental results. The compounds are also found to inhibit the ribonucleolytic activity of angiogenin, a homologous protein and potent inducer of blood vessel formation.
Item Type: | Article |
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Source: | Copyright of this article belongs to Elsevier Science. |
Keywords: | Ribonuclease A; Angiogenin; Thymidine-3′-O-Carboxy Ester; Competitive Inhibition; FT-IR; Circular Dichroism; Docking |
ID Code: | 113774 |
Deposited On: | 10 May 2018 12:07 |
Last Modified: | 10 May 2018 12:07 |
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