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Literature summary for 3.2.1.166 extracted from

  • Loka, R.S.; Yu, F.; Sletten, E.T.; Nguyen, H.M.
    Design, synthesis, and evaluation of heparan sulfate mimicking glycopolymers for inhibiting heparanase activity (2017), Chem. Commun. (Camb.), 53, 9163-9166 .
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
drug development the natural heparan sulfate-heparanase interactions are used as a template for the design of heparan sulfate-mimicking glycopolymers Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
heparin IC50 is 0.001 mg/ml Homo sapiens
additional information the natural heparan sulfate-heparanase interactions are used as a template for the design of heparan sulfate-mimicking glycopolymers, e.g. saccharide-functionalized neo-glycopolymers, which retain the key biological properties of the natural polysaccharides, synthesis and mass spectrometric identification, detailed overview. A glycopolymer with 12 repeating units is determined to be the most potent inhibitor and to have tight-binding characteristics. This glycopolymer also lacks anticoagulant activity. Inhibition of heparanase by HS mimicking monomers and neo-glycopolymers using TR-FRET assay Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
extracellular matrix
-
Homo sapiens 31012
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
heparan sulfate + H2O Homo sapiens
-
?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9Y251
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
heparan sulfate + H2O
-
Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
endo-beta-D-glucuronidase
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
additional information
-
IC50 values of heparan sulfate-mimicking glycopolymers, overview Homo sapiens additional information

General Information

General Information Comment Organism
physiological function heparanase is an enzyme which cleaves heparan sulfate (HS) polysaccharides of the extracellular matrix. It is a regulator of tumor behavior, plays a key role in kidney related diseases and autoimmune diabetes Homo sapiens