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Structural insights into heparanase activity using a fluorogenic heparan sulfate disaccharide

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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.

Graphical abstract: Structural insights into heparanase activity using a fluorogenic heparan sulfate disaccharide

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Article information


Submitted
02 Sep 2020
Accepted
09 Oct 2020
First published
10 Oct 2020

Chem. Commun., 2020, Advance Article
Article type
Communication

Structural insights into heparanase activity using a fluorogenic heparan sulfate disaccharide

L. Wu, N. Wimmer, G. J. Davies and V. Ferro, Chem. Commun., 2020, Advance Article , DOI: 10.1039/D0CC05932C

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