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Literature summary for 3.4.24.B12 extracted from

  • Shieh, H.S.; Tomasselli, A.G.; Mathis, K.J.; Schnute, M.E.; Woodard, S.S.; Caspers, N.; Williams, J.M.; Kiefer, J.R.; Munie, G.; Wittwer, A.; Malfait, A.M.; Tortorella, M.D.
    Structure analysis reveals the flexibility of the ADAMTS-5 active site (2011), Protein Sci., 20, 735-744.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.24.B12

Cloned(Commentary)

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 (Commentary)

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

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

Organism UniProt Comment Textmining
Homo sapiens Q9UNA0
-
-

Purification (Commentary)

Purification (Comment) Organism
gel filtration Homo sapiens

Renatured (Commentary)

Renatured (Comment) Organism
-
 Homo sapiens

Substrates and Products (Substrate)

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

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 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