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 Chemjournal_title
Bioorganic chemistryauthors
Debnath J,Dasgupta S,Pathak Tdoi
10.1016/j.bioorg.2013.11.005subject
Has Abstractpub_date
2014-02-01 00:00:00pages
56-61eissn
0045-2068issn
1090-2120pii
S0045-2068(13)00075-8journal_volume
52pub_type
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