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Modulation of BACE1 Activity by Chemically Modified Aptamers

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.
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https://hal-cea.archives-ouvertes.fr/cea-02291360
Contributor : Marianne Leriche <>
Submitted on : Wednesday, September 18, 2019 - 4:21:30 PM
Last modification on : Wednesday, June 17, 2020 - 3:42:03 PM

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Cecile Gasse, Marwa Zaarour, Sam Noppen, Mikhail Abramov, Philippe Marliere, et al.. Modulation of BACE1 Activity by Chemically Modified Aptamers. ChemBioChem, Wiley-VCH Verlag, 2018, 19 (7), pp.754-763. ⟨10.1002/cbic.201700461⟩. ⟨cea-02291360⟩

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