Cloned (Comment) | Organism |
---|---|
the catalytic domain of ADAMTS-5 comprising amino acids S263 to I480 preceded by a Met-Ala sequence and incorporating the single point mutation L282K is expressed in Escherichia coli | Homo sapiens |
Crystallization (Comment) | Organism |
---|---|
ADAMTS-5 catalytic domain in complex with inhibitor, vapor diffusion method, using 30% (w/v) PEG 3350 and 0.1 M Tris pH 8.5, at 22°C | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(2R)-2-[4-(1,3-benzodioxol-5-yl)benzyl]-N4-hydroxy-N1-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide | nanomolar inhibitor of both ADAMTS-5 | Homo sapiens | |
N-hydroxy-4-(4-(4-(trifluoromethyl)-phenoxy)phenylsulfonyl)-tetrahydro-2H-pyran-4-carboxamide | nanomolar inhibitor of both ADAMTS-5 | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | Q9UNA0 | - |
- |
Purification (Comment) | Organism |
---|---|
gel filtration | Homo sapiens |
Renatured (Comment) | Organism |
---|---|
- |
Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
aggrecan + H2O | at Glu373/Ala374 | Homo sapiens | ? | - |
? | |
K-[6FAM]-DVQEFRGVTAVIRC-[Qsy9]-KGK + H2O | - |
Homo sapiens | K-[6FAM]-DVQE + FRGVTAVIRC-[Qsy9]-KGK | - |
? |
Synonyms | Comment | Organism |
---|---|---|
a disintegrin and metalloproteinase with thrombospondin motifs-5 | - |
Homo sapiens |
ADAMTS-5 | - |
Homo sapiens |
aggrecanase-2 | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000129 | - |
pH and temperature not specified in the publication | Homo sapiens | (2R)-2-[4-(1,3-benzodioxol-5-yl)benzyl]-N4-hydroxy-N1-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide | |
0.129 | - |
pH and temperature not specified in the publication | Homo sapiens | N-hydroxy-4-(4-(4-(trifluoromethyl)-phenoxy)phenylsulfonyl)-tetrahydro-2H-pyran-4-carboxamide |