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Literature summary for 3.4.24.B12 extracted from

  • Tortorella, M.D.; Arner, E.C.; Hills, R.; Easton, A.; Korte-Sarfaty, J.; Fok, K.; Wittwer, A.J.; Liu, R.Q.; Malfait, A.M.
    Alpha2-macroglobulin is a novel substrate for ADAMTS-4 and ADAMTS-5 and represents an endogenous inhibitor of these enzymes (2004), J. Biol. Chem., 279, 17554-17561.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Drosophila SF9 cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(S)-2-dimethylamino-N-hydroxy-3,3-dimethyl-4-[(4-phenoxyphenyl)-sulfonyl]-butanamide SC81956, potent inhibitor of ADAMTS-5 Homo sapiens
alpha2-Macroglobulin after 10 min 100% and 68% inhibition at concentrations of 2.5 and 7.5 nM, respectively, similar results when using 25 and 75 nM Homo sapiens
BB-16 (2S,5R,6S)-3-Aza-4-oxo-10-oxa-5-hexyl-2-(methylcarboxamido)-10-paracyclophane-6-N-hydroxycarboxamide Homo sapiens
additional information [3S-[3R*,2-[2R*,2-(R*,S*)]-hexahydro-2-(2-[2-(hydroxyamino)-1-methyl-2-oxyethyl])-4-methyl-1-oxypentyl]-N-methyl]-3-pyridazinecarboxamide, i.e.XS309 is inactive at less than 0.01 mM in blocking ADAMTS-5 Homo sapiens
tissue inhibitor of matrix metalloproteinases-3 TIMP-3 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
aggrecan + H2O
-
Homo sapiens ?
-
?
alpha2-macroglobulin + H2O
-
Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
ADAMTS-5
-
Homo sapiens
aggrecanase 2
-
Homo sapiens