Literature summary for 3.4.24.B12 extracted from

Shieh, H.S.; Mathis, K.J.; Williams, J.M.; Hills, R.L.; Wiese, J.F.; Benson, T.E.; Kiefer, J.R.; Marino, M.H.; Carroll, J.N.; Leone, J.W.; Malfait, A.M.; Arner, E.C.; Tortorella, M.D.; Tomasselli, A.
High resolution crystal structure of the catalytic domain of ADAMTS-5 (aggrecanase-2) (2008), J. Biol. Chem., 283, 1501-1507.

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Cloned(Commentary)

Cloned (Comment)	Organism
expressed in Escherichia coli MON208 cells	Homo sapiens

Crystallization (Commentary)

Crystallization (Comment)	Organism
vapour diffusion method with 25% (v/v) polyethylene glycol 3350, 200 mM ammonium acetate, 100 mM Tris, pH 8.5	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
N-hydroxy-4-([4-[4-(trifluoromethyl)phenoxy]phenyl]sulfonyl)tetrahydro-2H-pyran-4-carboxamide	-	Homo sapiens
TIMP-3	-	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Purification (Commentary)

Purification (Comment)	Organism
Sephacryl S-200 HR gel filtration	Homo sapiens

Renatured (Commentary)

Renatured (Comment)	Organism
in 50 mM HEPES, pH 8.0, 2 mM oxidized glutathione, 50 mM arginine, 10 mM CaCl2, 0.2 mM ZnCl2, and 1% protease inhibitors, at room temperature	Homo sapiens

Source Tissue

Source Tissue	Comment	Organism	Textmining
placenta	-	Homo sapiens	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
aggrecan + H2O	-	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
0.0000038	-	in 100 mM Tris-HCl, 100 mM NaCl, 0.01 mM CaCl2, 0.05% Brij, pH 7.5	Homo sapiens	TIMP-3
0.00029	-	in 100 mM Tris-HCl, 100 mM NaCl, 0.01 mM CaCl2, 0.05% Brij, pH 7.5	Homo sapiens	N-hydroxy-4-([4-[4-(trifluoromethyl)phenoxy]phenyl]sulfonyl)tetrahydro-2H-pyran-4-carboxamide

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Release 2023.1 (January 2023)