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Literature summary extracted from

  • Bame, K.J.
    Heparanases: endoglycosidases that degrade heparan sulfate proteoglycans (2001), Glycobiology, 11, 91R-98R.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.2.1.166 basic fibroblast growth factor
-
 Cricetulus griseus
3.2.1.166 additional information no inhibition by basic fibroblast growth factor Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.2.1.166 heparan sulfate proteoglycan + H2O Homo sapiens heparanase cleaves the heparan sulfate glycosaminoglycans from proteoglycan core proteins and degrades them to small oligosaccharides. Inside cells, the enzyme is important for the normal catabolism of heparan sulfate proteoglycans, generating glycosaminoglycan fragments that are then transported to lysosomes and completely degraded. When secreted, heparanase degrades basement membrane heparan sulfate glycosaminoglycans at sites of injury or inflammation, allowing extravasion of immune cells into nonvascular spaces and releasing factors that regulate cell proliferation and angiogenesis. At physiological pH the enzyme binds to the extracellular matrix of cell surface heparan sulfate proteolycan but is inactive. When the pH is lowered, which could occur at sites of inflammation or matrix damage, the bound enzyme becomes active and cleaves the heparan sulfate proteoglycan it is bound to heparan sulfate fragment + truncated heparan sulfate proteoglycan
-
 ?
3.2.1.166 heparan sulfate proteolycan + H2O Cricetulus griseus
-
 heparan sulfate fragment + truncated heparan sulfate proteoglycan
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
3.2.1.166 Cricetulus griseus
-
-
-
3.2.1.166 Homo sapiens Q9Y251
-
-

Posttranslational Modification

EC Number Posttranslational Modification Comment Organism
3.2.1.166 glycoprotein synthesized as an inactive 65000 Da glycoprotein that is cleaved at the N-terminus to generate the active enzyme Cricetulus griseus
3.2.1.166 glycoprotein synthesized as an inactive 65000 Da glycoprotein that is cleaved at the N-terminus to generate the active enzyme Homo sapiens
3.2.1.166 proteolytic modification synthesized as an inactive 65000 Da glycoprotein that is cleaved at the N-terminus to generate the active enzyme Cricetulus griseus
3.2.1.166 proteolytic modification synthesized as an inactive 65000 Da glycoprotein that is cleaved at the N-terminus to generate the active enzyme Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.2.1.166 blood platelet
-
 Homo sapiens
-
3.2.1.166 CHO cell
-
 Cricetulus griseus
-
3.2.1.166 additional information highly expressed in tumors and metastatic cell lines derived from a variety of tissues Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.2.1.166 heparan sulfate proteoglycan + H2O heparanase cleaves the heparan sulfate glycosaminoglycans from proteoglycan core proteins and degrades them to small oligosaccharides. Inside cells, the enzyme is important for the normal catabolism of heparan sulfate proteoglycans, generating glycosaminoglycan fragments that are then transported to lysosomes and completely degraded. When secreted, heparanase degrades basement membrane heparan sulfate glycosaminoglycans at sites of injury or inflammation, allowing extravasion of immune cells into nonvascular spaces and releasing factors that regulate cell proliferation and angiogenesis. At physiological pH the enzyme binds to the extracellular matrix of cell surface heparan sulfate proteolycan but is inactive. When the pH is lowered, which could occur at sites of inflammation or matrix damage, the bound enzyme becomes active and cleaves the heparan sulfate proteoglycan it is bound to Homo sapiens heparan sulfate fragment + truncated heparan sulfate proteoglycan
-
 ?
3.2.1.166 heparan sulfate proteoglycan + H2O cleavage of the beta-1,4-glycosidic bond between a D-glucuronate and a D-glucosamine in heparan sulfate. Cleavage to short chains of 6000-8000 Da. 2-O-sulfate groups are not required for C1A heparanase to recognize and degrade the substrate Cricetulus griseus heparan sulfate fragment + truncated heparan sulfate proteoglycan
-
 ?
3.2.1.166 heparan sulfate proteoglycan + H2O cleavage to 5000 Da oligosaccharides Homo sapiens heparan sulfate fragment + truncated heparan sulfate proteoglycan
-
 ?
3.2.1.166 heparan sulfate proteolycan + H2O
-
 Cricetulus griseus heparan sulfate fragment + truncated heparan sulfate proteoglycan
-
 ?
3.2.1.166 heparin sulfate + H2O cleavage to 5000 Da oligosaccharides Homo sapiens ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.2.1.166 C1A heparanase
-
 Cricetulus griseus
3.2.1.166 Hpa1 heparanase
-
 Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.2.1.166 5.5 5.8
-
 Cricetulus griseus
3.2.1.166 5.5 5.8
-
 Homo sapiens