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

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.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Debnath J,Dasgupta S,Pathak T

doi

10.1016/j.bioorg.2013.11.005

subject

Has Abstract

pub_date

2014-02-01 00:00:00

pages

56-61

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(13)00075-8

journal_volume

52

pub_type

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