Methoxymethyl threofuranosyl thymidine (4 `-MOM-TNA-T) at the T7 position of the thrombin-binding aptamer boosts anticoagulation activity, thermal stability, and nuclease resistance
| Title | Methoxymethyl threofuranosyl thymidine (4 `-MOM-TNA-T) at the T7 position of the thrombin-binding aptamer boosts anticoagulation activity, thermal stability, and nuclease resistance |
| Publication Type | Journal Article |
| Year of Publication | 2020 |
| Authors | Varada, M, Aher, M, Erande, N, Kumar, VA, Fernandes, M |
| Journal | ACS Omega |
| Volume | 5 |
| Issue | 1 |
| Pagination | 498-506 |
| Date Published | JAN |
| Type of Article | Article |
| ISSN | 2470-1343 |
| 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. |
| DOI | 10.1021/acsomega.9b03042 |
| Type of Journal (Indian or Foreign) | Foreign |
| Impact Factor (IF) | 2.870 |
Divison category:
Organic Chemistry