Photoswitchable inhibitors of human β-glucocerebrosidase

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 denatu...

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Veröffentlicht in:	Organic & biomolecular chemistry 2022-02, Vol.2 (8), p.1637-1641
Hauptverfasser:	Davighi, Maria Giulia, Clemente, Francesca, Matassini, Camilla, Cardona, Francesca, Nielsen, Mogens Brøndsted, Goti, Andrea, Morrone, Amelia, Paoli, Paolo, Cacciarini, Martina
Format:	Artikel
Sprache:	eng
Schlagworte:	Azo compounds Azo Compounds - chemical synthesis Azo Compounds - chemistry Azo Compounds - pharmacology Azulenes - chemical synthesis Azulenes - chemistry Azulenes - pharmacology Cell Line Cell Survival - drug effects Cytotoxicity Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Glucosylceramidase Glucosylceramidase - antagonists & inhibitors Glucosylceramidase - metabolism Humans Inhibitors Irradiation Light Molecular Structure Photochemical Processes Radiation Thermal denaturation Toxicity
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Beschreibung
Zusammenfassung:	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. Towards human GCase activity enhancement by means of light responsive inhibitors.
ISSN:	1477-0520 1477-0539
DOI:	10.1039/d1ob02159a