9th Glyco@Event with Herman Overkleeft
on the July 6, 2018
At 10:00 a.m.
Herman Overkleeft, from Leiden Institute of Chemistry, Leiden University, Netherlands, is the 9th invited speaker participating to the Glyco@Events. The event will take place on Friday, July 6th at Nanobio building.
The 9th Glyco@Event will take place at Nanobio building on Friday, July 6th from 10:00. The invited speaker is Herman Overkleeft, from Leiden Institute of Chemistry, Leiden University, Netherlands, who will give a talk on “Activity-based glycosidase profiling in biomedicine and biotechnology”. Two young glycoscientists from Glyco@Alps, Arnaud Masselin and Laura Gauthier will kick off the event with short talks.
Activity-based protein profiling (ABPP) is a rapidly emerging field in chemical biology research. Enzymes that employ a mechanism in processing their substrate that involves formation of a covalent enzyme-intermediate adduct can be blocked by mechanism-based suicide inhibitors: compounds that react within the enzyme active site to form a covalent and irreversible adduct. Introduction of a reporter moiety (‘TAG’ in the below picture) yields an activity-based probe (ABP) through which enzyme activities can be discovered (comparative ABPP) and the efficacy enzyme inhibitors in complex biological systems analyzed (competitive ABPP).
Our work on ABPP development focuses on retaining glycosidases: hydrolytic enzymes able to cleave interglycosidic linkages and that do so through the formation of covalent enzyme-substrate intermediates. Configurational and functional analogues of the natural product and mechanism-based retaining beta-glucosidase inhibitor, cyclophellitol, prove to be highly versatile tools to study retaining glycosidases of various nature and origin in relation to human health and disease, but also in the field of biotechnology. In this lecture the current state in the design, synthesis and application of synthetic cyclophellitol derivatives in studying retaining glycosidases will be presented. Discussed subjects will include 1) diagnosis of human lysosomal exoglycosidases in relation to lysosomal storage disorders; 2) glycosylation of cyclophellitol derivatives top arrive at retaining endoglycosidase ABPs and 3) application of glycosidase ABPs in the functional profiling of fungal secretomes for the discovery of glycosidases for biotechnology application.
10:00 Young glycoscientists talks
10:40 Coffee break and discussions
11:00 Invited speaker: Herman Overkleeft
10:40 Coffee break and discussions
11:00 Invited speaker: Herman Overkleeft
Invited speaker
Activity-based glycosidase profiling in biomedicine and biotechnology
Herman Overkleeft, University of Leiden, NetherlandsActivity-based protein profiling (ABPP) is a rapidly emerging field in chemical biology research. Enzymes that employ a mechanism in processing their substrate that involves formation of a covalent enzyme-intermediate adduct can be blocked by mechanism-based suicide inhibitors: compounds that react within the enzyme active site to form a covalent and irreversible adduct. Introduction of a reporter moiety (‘TAG’ in the below picture) yields an activity-based probe (ABP) through which enzyme activities can be discovered (comparative ABPP) and the efficacy enzyme inhibitors in complex biological systems analyzed (competitive ABPP).
Our work on ABPP development focuses on retaining glycosidases: hydrolytic enzymes able to cleave interglycosidic linkages and that do so through the formation of covalent enzyme-substrate intermediates. Configurational and functional analogues of the natural product and mechanism-based retaining beta-glucosidase inhibitor, cyclophellitol, prove to be highly versatile tools to study retaining glycosidases of various nature and origin in relation to human health and disease, but also in the field of biotechnology. In this lecture the current state in the design, synthesis and application of synthetic cyclophellitol derivatives in studying retaining glycosidases will be presented. Discussed subjects will include 1) diagnosis of human lysosomal exoglycosidases in relation to lysosomal storage disorders; 2) glycosylation of cyclophellitol derivatives top arrive at retaining endoglycosidase ABPs and 3) application of glycosidase ABPs in the functional profiling of fungal secretomes for the discovery of glycosidases for biotechnology application.
Young scientists talks
Innovative therapeutic strategies for Wilson disease
Laura Gauthier, SYMMESTriazinyl-glycosides as new activity-based probes for carbohydrate-active enzymes
Arnaud Masselin, Cermav
Published on August 29, 2018
Practical informations
Location
Bâtiment Nanobio - Salle de conférence
570 Rue de la Chimie
Domaine universitaire de Grenoble