Article
Light-Triggered Control of Glucocerebrosidase Inhibitors: Towards Photoswitchable Pharmacological Chaperones.
Chemistry (Weinheim an der Bergstrasse, Germany) - 3 Apr 2023
Clemente Francesca, Davighi Maria Giulia, Matassini Camilla, Cardona Francesca, Goti Andrea, Morrone Amelia, Paoli Paolo, Tejero Tomás, Merino Pedro, Cacciarini Martina
Abstract excerpt
Piperidine-based photoswitchable derivatives have been developed as putative pharmacological chaperones for glucocerebrosidase (GCase), the defective enzyme in Gaucher disease (GD). The structure-activity study revealed that both the iminosugar and the light-sensitive azobenzene are essential features to exert inhibitory activity towards human GCase and a system with the correct inhibition trend (IC50 of the...
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