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Literature summary for 3.4.24.B12 extracted from
- Calcium pentosan polysulfate is a multifaceted exosite inhibitor of aggrecanases (2008), FASEB J., 22, 3515-3524.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expression of a recombinant interglobular domain of human aggrecan, residues 330YTGED to HLPGG458 tagged with glutathione S-transferase and FLAG, in Escherichia coli | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| calcium pentosan polysulfate | chemically sulfated xylopyranose from beechwood. Multifaceted exosite inhibitor, protects cartilage against aggrecan degradation. Inhibitor interacts with the noncatalytic spacer domain of isoform ADAMTS-4 and the cysteine-rich domain of ADAMTS-5, blocking activity against their natural substrate aggrecan with inhibitory concentration 50 values of 10-40 nM but only weakly inhibiting hydrolysis of a nonglycosylated recombinant protein substrate. calcium pentosan polysulfate increases cartilage levels of tissue inhibitor of metalloproteinases TIMP-3, an endogenous inhibitor of ADAMTS-4 and -5 | Homo sapiens |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | Q9UNA0 | - |
- |
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Release 2023.1 (January 2023)
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