Methoxymethyl Threofuranosyl Thymidine (4'-MOM-TNA-T) at the T7 Position of the Thrombin-Binding Aptamer Boosts Anticoagulation Activity, Thermal Stability, and Nuclease Resistance.,ACS Omega

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Methoxymethyl Threofuranosyl Thymidine (4'-MOM-TNA-T) at the T7 Position of the Thrombin-Binding Aptamer Boosts Anticoagulation Activity, Thermal Stability, and Nuclease Resistance.
ACS Omega ( IF 3.7 ) Pub Date : 2019-12-26 , DOI: 10.1021/acsomega.9b03042
Manojkumar Varada ₁ , Manisha Aher _{1,

2} , Namrata Erande _{1,

2} , Vaijayanti A Kumar _{1,

2} , Moneesha Fernandes _{1,

2}

Affiliation

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.

中文翻译：

凝血酶结合适体的T7位置上的甲氧甲基苏糖呋喃基胸苷（4'-MOM-TNA-T）可增强抗凝活性，热稳定性和核酸酶抗性。

据报道，合成了4'-甲氧基甲基苏呋喃糖基（4'-MOM-TNA）胸苷和富含G的凝血酶结合适体（TBA）序列的衍生寡聚物。研究了这些带有2'-3'-磷酸二酯主链的低聚物的G-四链体稳定性，抗凝活性和酶稳定性，这些低聚物在环区域中是单个取代基。在所有低聚物中，在T7位置带有4'-MOM-TNA单元的TBA-7T形成了具有最高热稳定性的四链体。与TBA相比，它还提高了抗凝活性，使剂量减少了三分之一。此外，TBA-7T对核酸内切酶和核酸外切酶均显示出增强的核酸酶抗性。

更新日期：2020-01-14

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