Developing nanobodies as allosteric molecular chaperones of glucocerebrosidase function

Abstract The enzyme glucocerebrosidase (GCase) catalyses the hydrolysis of glucosylceramide to glucose and ceramide within lysosomes. Homozygous or compound heterozygous mutations in the GCase-encoding GBA1 gene cause the lysosomal storage disorder Gaucher disease, while heterozygous and homozygous...

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Main Authors: Thomas Dal Maso, Chiara Sinisgalli, Gianluca Zilio, Elisa Franzin, Isabella Tessari, Els Pardon, Jan Steyaert, Steven Ballet, Elisa Greggio, Wim Versées, Nicoletta Plotegher
Format: Article
Language:English
Published: Nature Portfolio 2025-05-01
Series:Nature Communications
Online Access:https://doi.org/10.1038/s41467-025-60134-4
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author Thomas Dal Maso
Chiara Sinisgalli
Gianluca Zilio
Elisa Franzin
Isabella Tessari
Els Pardon
Jan Steyaert
Steven Ballet
Elisa Greggio
Wim Versées
Nicoletta Plotegher
author_facet Thomas Dal Maso
Chiara Sinisgalli
Gianluca Zilio
Elisa Franzin
Isabella Tessari
Els Pardon
Jan Steyaert
Steven Ballet
Elisa Greggio
Wim Versées
Nicoletta Plotegher
author_sort Thomas Dal Maso
collection DOAJ
description Abstract The enzyme glucocerebrosidase (GCase) catalyses the hydrolysis of glucosylceramide to glucose and ceramide within lysosomes. Homozygous or compound heterozygous mutations in the GCase-encoding GBA1 gene cause the lysosomal storage disorder Gaucher disease, while heterozygous and homozygous mutations are the most frequent genetic risk factor for Parkinson’s disease. These mutations commonly affect GCase stability, trafficking or activity. Here, we report the development and characterization of nanobodies (Nbs) targeting and acting as molecular chaperones for GCase. We identify several Nb families that bind with nanomolar affinity to GCase. Based on biochemical characterization, we group the Nbs in two classes: Nbs that improve the activity of the enzyme and Nbs that increase GCase stability in vitro. A selection of the most promising Nbs is shown to improve GCase function in cell models and positively impact the activity of the N370S mutant GCase. These results lay the foundation for the development of new therapeutic routes.
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spelling doaj-art-bfb317ed106347bebcca7900f74c935c2025-08-20T02:03:31ZengNature PortfolioNature Communications2041-17232025-05-0116111910.1038/s41467-025-60134-4Developing nanobodies as allosteric molecular chaperones of glucocerebrosidase functionThomas Dal Maso0Chiara Sinisgalli1Gianluca Zilio2Elisa Franzin3Isabella Tessari4Els Pardon5Jan Steyaert6Steven Ballet7Elisa Greggio8Wim Versées9Nicoletta Plotegher10VIB-VUB Center for Structural Biology, VIBDepartment of Biology, University of PadovaDepartment of Biology, University of PadovaDepartment of Biology, University of PadovaDepartment of Biology, University of PadovaVIB-VUB Center for Structural Biology, VIBVIB-VUB Center for Structural Biology, VIBResearch Group of Organic Chemistry, Vrije Universiteit BrusselDepartment of Biology, University of PadovaVIB-VUB Center for Structural Biology, VIBDepartment of Biology, University of PadovaAbstract The enzyme glucocerebrosidase (GCase) catalyses the hydrolysis of glucosylceramide to glucose and ceramide within lysosomes. Homozygous or compound heterozygous mutations in the GCase-encoding GBA1 gene cause the lysosomal storage disorder Gaucher disease, while heterozygous and homozygous mutations are the most frequent genetic risk factor for Parkinson’s disease. These mutations commonly affect GCase stability, trafficking or activity. Here, we report the development and characterization of nanobodies (Nbs) targeting and acting as molecular chaperones for GCase. We identify several Nb families that bind with nanomolar affinity to GCase. Based on biochemical characterization, we group the Nbs in two classes: Nbs that improve the activity of the enzyme and Nbs that increase GCase stability in vitro. A selection of the most promising Nbs is shown to improve GCase function in cell models and positively impact the activity of the N370S mutant GCase. These results lay the foundation for the development of new therapeutic routes.https://doi.org/10.1038/s41467-025-60134-4
spellingShingle Thomas Dal Maso
Chiara Sinisgalli
Gianluca Zilio
Elisa Franzin
Isabella Tessari
Els Pardon
Jan Steyaert
Steven Ballet
Elisa Greggio
Wim Versées
Nicoletta Plotegher
Developing nanobodies as allosteric molecular chaperones of glucocerebrosidase function
Nature Communications
title Developing nanobodies as allosteric molecular chaperones of glucocerebrosidase function
title_full Developing nanobodies as allosteric molecular chaperones of glucocerebrosidase function
title_fullStr Developing nanobodies as allosteric molecular chaperones of glucocerebrosidase function
title_full_unstemmed Developing nanobodies as allosteric molecular chaperones of glucocerebrosidase function
title_short Developing nanobodies as allosteric molecular chaperones of glucocerebrosidase function
title_sort developing nanobodies as allosteric molecular chaperones of glucocerebrosidase function
url https://doi.org/10.1038/s41467-025-60134-4
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