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Favorable 2'-substitution in the loop region of a thrombin-binding DNA aptamer
Ragini Awachat1, Atish A Wagh1, Manisha Aher1
1Organic Chemistry Division, CSIR-National Chemical Laboratory, Homi Bhabha Road, Pashan, Pune 411008, India; Academy of Scientific and Innovative Research (AcSIR), CSIR-NCL Campus, Pune 411008, India.
Bioorganic & Medicinal Chemistry Letters
|April 22, 2018
Abstract:
Simple 2'-OMe-chemical modification in the loop region of the 15mer G-rich DNA sequence GGTTGGTGTGGTTGG is reported. The G-quadruplex structure of this thrombin-binding aptamer (TBA), is stabilized by single modifications (T → 2'-OMe-U), depending on the position of the modification. The structural stability also renders significantly increased inhibition of thrombin-induced fibrin polymerization, a process closely associated with blood-clotting.