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Heparinase I (Hep I) EC 188.8.131.52
Degrades heparin and the S-domains of heparan sulfate.
Catalyses the eliminative scission of the glycosidic linkage between N-sulfated glucosamine (GlcNSO3) and 2-O-sulfated iduronic acid (IdoA,2SO3). The IdoA,2SO3 residue is essential for the activity of Heparinase I while 6-O-sulfation of GlcNSO3 enhances enzyme activity.
The disaccharide cleaved by Heparinase I is common in heparin but it is quite rare in HS where it is confined to the sulfated domains. Thus Heparinase I will attack HS only in the S-domains bringing about limited scission of the polymer chain. This is a very valuable and under exploited property of Heparinase I. For example Heparinase I can be used to determine the spacing between S-domains in HS. This spacing is reflected in the size of the HS fragments that resist the action of the enzyme. Heparinase I can also be used to identify biological properties of HS that depend upon the integrity of the S-domains. For example HS-activation of fibroblast growth factor 2 (FGF2) is inhibited by treatment with Heparinase I (but not by Heparinase III).