6ZDM

Crystal structure of human heparanase in complex with a N',6O'-bis-sulfated 4-methylumbelliferyl heparan sulfate disaccharide

This is a non-PDB format compatible entry.

Summary for 6ZDM

• Entry DOI: 10.2210/pdb6zdm/pdb
• Descriptor: Heparanase, 2-acetamido-2-deoxy-beta-D-glucopyranose, 1,2-ETHANEDIOL, ... (7 entities in total)
• Functional Keywords: heparanase, substrate, fluorogenic, heparan sulfate, poised, 4-methylumbelliferyl, hydrolase
• Biological source: Homo sapiens (Human); More
• Total number of polymer chains: 2
• Total formula weight: 53713.26

Authors

Wu, L.,Davies, G.J. (deposition date: 2020-06-14, release date: 2020-10-21, Last modification date: 2024-01-24)

Primary citation

Wu, L.,Wimmer, N.,Davies, G.J.,Ferro, V.
Structural insights into heparanase activity using a fluorogenic heparan sulfate disaccharide.
Chem.Commun.(Camb.), 56:13780-13783, 2020

PubMed 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.

PubMed: 33073275
DOI: 10.1039/d0cc05932c

Experimental method

X-RAY DIFFRACTION (1.714 Å)