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BRENDA support

Literature summary for 3.2.1.166 extracted from

  • Dredge, K.; Hammond, E.; Davis, K.; Li, C.P.; Liu, L.; Johnstone, K.; Handley, P.; Wimmer, N.; Gonda, T.J.; Gautam, A.; Ferro, V.; Bytheway, I.
    The PG500 series: novel heparan sulfate mimetics as potent angiogenesis and heparanase inhibitors for cancer therapy (2010), Invest. New Drugs, 28, 276-283.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
additional information the PG500 series of heparan sulfate mimetics potently block the enzymatic activity of heparanase (fully sulfated, single entity oligosaccharides attached to a lipophilic moiety, which have been optimized for drug development) Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9Y251
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Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
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additional information PG517: 162 nM, PG518: 59 nM, PG536: 6 nM, PG537: 6 nM, PG545: 6 nM, PG546: 4 nM, PG547: 16 nM, PG554: 9 nM, PG561: 11 nM, PG562: 9 nM, PI-88: 8 nM Homo sapiens