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Stability Is Not Everything: The Case of the Cyclisation of a Thrombin-Binding Aptamer |
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| Authors: | Dr Claudia Riccardi Dr Albert Meyer Dr Jean-Jacques Vasseur Dr Irene Russo?Krauss Prof Luigi Paduano Dr Rosario Oliva Prof Luigi Petraccone Dr François Morvan Prof Daniela Montesarchio |
| Affiliation: | 1. Department of Chemical Sciences, University of Naples Federico II, Via Cintia 21, 80126 Napoli, Italy;2. Institut des Biomolécules Max Mousseron, UMR 5247, CNRS, ENSCM, University of Montpellier, Place E. Bataillon, 34095 Montpellier Cedex 5, France |
| Abstract: | 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. |
| Keywords: | aptamers click chemistry cyclization G-quadruplexes molecular recognition |