Gasse, C;
Zaarour, M;
Noppen, S;
Abramov, M;
Marliere, P;
Liekens, S;
De Strooper, B;
(2018)
Modulation of BACE1 Activity by Chemically Modified Aptamers.
ChemBioChem
, 19
(7)
pp. 754-763.
10.1002/cbic.201700461.
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Abstract
A modified DNA aptamer that binds BACE1, a therapeutic target involved in Alzheimer's disease has been developed. This ssXNA not only tightly binds to BACE1 but also inhibits its protease activity in vitro in the same range as a previously described unmodified aptamer. We report the in vitro selection of functional oligonucleotides incorporating two nucleobase modifications: 5‐chlorouracil and 7‐deazaadenine. The nucleoside analogue 5‐chloro‐2′‐deoxyuridine has already been explored as a replacement for thymidine in a chemically modified genome of a bacterium. Thus, 5‐chlorouracil modification is a good candidate to support genetic transfer in vivo as well as functional activity.
| Type: | Article |
|---|---|
| Title: | Modulation of BACE1 Activity by Chemically Modified Aptamers |
| Open access status: | An open access version is available from UCL Discovery |
| DOI: | 10.1002/cbic.201700461 |
| Publisher version: | https://doi.org/10.1002/cbic.201700461 |
| Language: | English |
| Additional information: | This version is the author accepted manuscript. For information on re-use, please refer to the publisher’s terms and conditions. |
| Keywords: | aptamers, BACE1, inhibitors, secretases, XNA |
| UCL classification: | UCL UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Brain Sciences UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Brain Sciences > UK Dementia Research Institute HQ |
| URI: | https://discovery-pp.ucl.ac.uk/id/eprint/10057826 |
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