Stability Is Not Everything: The Case of the Cyclisation of a Thrombin‐Binding Aptamer
Résumé
With the aim of developing a new approach to obtain improved aptamers, a cyclic thrombin-binding aptamer (TBA) analogue (cycTBA) has been prepared by exploiting a copper(I)-assisted azide-alkyne cycloaddition. The markedly increased serum resistance and exceptional thermal stability of the G-quadruplex versus TBA were associated with halved thrombin inhibition, which suggested that some flexibility in the TBA structure was necessary for protein recognition.
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19ChemBioChem1789_cycTBA-manuscript_13-12-2018FM-2.pdf (825.34 Ko)
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