Projects per year
Abstract
A synthetic heparan sulfate disaccharide has been assessed as a fluorogenic heparanase substrate, enabling enzyme turnover and inhibition kinetics measurements despite slow turnover. Crystal structures with human heparanase also provide the first ever observation of a substrate in an activated 1S3 conformation, highlighting previously unknown interactions involved in enzymatic processing. Our data provide insights into the heparanase catalytic mechanism, and will inform the design of improved heparanase substrates and inhibitors.
Original language | English |
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Pages (from-to) | 13780-13783 |
Number of pages | 4 |
Journal | Chemical Communications |
Volume | 56 |
Issue number | 89 |
Early online date | 10 Oct 2020 |
DOIs | |
Publication status | Published - 18 Nov 2020 |
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Application of activity-based glycosidase probes for mechanism, enzyme discovery and clinical diagnosis
1/01/18 → 31/12/21
Project: Research project (funded) › Research
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Glycosylation: Programmes for Observation, Inhibition & Structure-based Exploitation of key carbohydrate-active enzymes
1/05/13 → 30/04/19
Project: Research project (funded) › Research