Photoswitchable inhibitors of human β-glucocerebrosidase

Maria Giulia Davighi; Francesca Clemente; Camilla Matassini; Francesca Cardona; Mogens Brøndsted Nielsen; Andrea Goti; Amelia Morrone; Paolo Paoli; Martina Cacciarini

doi:10.1039/D1OB02159A

Photoswitchable inhibitors of human β-glucocerebrosidase†

Maria Giulia Davighi,‡^a Francesca Clemente,‡^a Camilla Matassini,

*^a Francesca Cardona,

^ab Mogens Brøndsted Nielsen,

^c Andrea Goti,

^ab Amelia Morrone,^d Paolo Paoli

^e and Martina Cacciarini

*^a

Author affiliations

* Corresponding authors

^a Department of Chemistry “U. Schiff”, University of Florence, via della Lastruccia 3-13, 50019 Sesto F.no (FI), Italy
E-mail: martina.cacciarini@unifi.it, camilla.matassini@unifi.it

^b Associated with LENS, via N. Carrara 1, 50019 Sesto F.no (FI), Italy

^c Department of Chemistry, University of Copenhagen, Universitetsparken 5, DK-2100 Copenhagen Ø, Denmark

^d Paediatric Neurology Unit and Laboratories, Neuroscience Department, Meyer Children's Hospital, and Department of Neurosciences, Pharmacology and Child Health. University of Florence, Viale Pieraccini 24, 50139 Firenze, Italy

^e Department of Experimental and Clinical Biomedical Sciences, University of Florence, Viale Morgagni 50, 50134 Firenze, Italy

Abstract

Light-switchable inhibitors of the enzyme β-glucocerebrosidase (GCase) have been developed by anchoring a specific azasugar to a dihydroazulene or an azobenzene responsive moiety. Their inhibitory effect towards human GCase, before and after irradiation are reported, and the effect on thermal denaturation of recombinant GCase and cytotoxicity were studied on selected candidates.

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DOI: https://doi.org/10.1039/D1OB02159A
Article type: Communication
Submitted: 03 Nov 2021
Accepted: 27 Jan 2022
First published: 27 Jan 2022
This article is Open Access

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Org. Biomol. Chem., 2022,20, 1637-1641

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Photoswitchable inhibitors of human β-glucocerebrosidase

M. G. Davighi, F. Clemente, C. Matassini, F. Cardona, M. B. Nielsen, A. Goti, A. Morrone, P. Paoli and M. Cacciarini, Org. Biomol. Chem., 2022, 20, 1637 DOI: 10.1039/D1OB02159A

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Organic & Biomolecular Chemistry

Photoswitchable inhibitors of human β-glucocerebrosidase†

Abstract

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Photoswitchable inhibitors of human β-glucocerebrosidase

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