Methoxymethyl threofuranosyl thymidine (4 `-MOM-TNA-T) at the T7 position of the thrombin-binding aptamer boosts anticoagulation activity, thermal stability, and nuclease resistance

TitleMethoxymethyl threofuranosyl thymidine (4 `-MOM-TNA-T) at the T7 position of the thrombin-binding aptamer boosts anticoagulation activity, thermal stability, and nuclease resistance
Publication TypeJournal Article
Year of Publication2020
AuthorsVarada, M, Aher, M, Erande, N, Kumar, VA, Fernandes, M
JournalACS Omega
Volume5
Issue1
Pagination498-506
Date PublishedJAN
Type of ArticleArticle
ISSN2470-1343
Abstract

The synthesis of 4'-methoxymethyl threofuranosyl (4'-MOM-TNA) thymidine and derived oligomers of the G-rich thrombin-binding aptameric (TBA) sequence is reported. The G-quadruplex stability, anticoagulation activity, and the enzymatic stability of these oligomers bearing the 2'-3'-phosphodiester backbone as single substitutions in the loop regions are studied. Amongst all the oligomers, TBA-7T bearing the 4'-MOM-TNA unit at the T7 position formed a quadruplex with the highest thermal stability. It also resulted in enhanced anticlotting activity that allowed a one-third reduction in the dose, relative to TBA. Further, TBA-7T exhibited enhanced nuclease resistance properties to both endo- and exonucleases.

DOI10.1021/acsomega.9b03042
Type of Journal (Indian or Foreign)

Foreign

Impact Factor (IF)

2.870

Divison category: 
Organic Chemistry

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