Amino and carboxy functionalized modified nucleosides: a potential class of inhibitors for angiogenin

Debnath, Joy ; Dasgupta, Swagata ; Pathak, Tanmaya (2014) Amino and carboxy functionalized modified nucleosides: a potential class of inhibitors for angiogenin Bioorganic Chemistry, 52 . pp. 56-61. ISSN 0045-2068

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Official URL: http://www.sciencedirect.com/science/article/pii/S...

Related URL: http://dx.doi.org/10.1016/j.bioorg.2013.11.005

Abstract

The 3′-amino and carboxy functionalize thymidines execute their ribonucleolytic inhibition activity for angiogenin. These modified nucleosidic molecules inhibit the ribonucleolytic activity of angiogenin in a competitive manner like the other conventional nucleotidic inhibitors, which have been confirmed from kinetic experiments. The improved inhibition constant (Ki) values 427 ± 7, 775 ± 6 μM clearly indicate modified nucleosides are an obvious option for the designing of inhibitors of angiogenesis process. The chorioallantoic membrane (CAM) assay qualitatively suggests that amino functionalized nucleosides have an effective potency to inhibited angiogenin-induced angiogenesis. Docking studies further demonstrate the interaction of their polar amino group with the P1 site residues of angiogenin, i.e., His-13 and His-114 residues.

Item Type:Article
Source:Copyright of this article belongs to Elsevier Science.
Keywords:Thymidine; Angiogenesis; Chorioallantoic Membrane (CAM) Assay; Docking
ID Code:103826
Deposited On:22 Mar 2017 05:07
Last Modified:22 Mar 2017 05:07

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