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Bioorg Med Chem Lett ; 28(10): 1765-1768, 2018 06 01.
Article in English | MEDLINE | ID: mdl-29678465

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.


Subject(s)
Aptamers, Nucleotide/pharmacology , Thrombin/antagonists & inhibitors , Aptamers, Nucleotide/chemistry , Binding Sites , Blood Coagulation/drug effects , Dose-Response Relationship, Drug , Fibrin/antagonists & inhibitors , Fibrin/metabolism , G-Quadruplexes , Molecular Structure , Polymerization/drug effects , Structure-Activity Relationship
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