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Literature summary for 3.4.24.82 extracted from

  • Tortorella, M.D.; Tomasselli, A.G.; Mathis, K.J.; Schnute, M.E.; Woodard, S.S.; Munie, G.; Williams, J.M.; Caspers, N.; Wittwer, A.J.; Malfait, A.M.; Shieh, H.S.
    Structural and inhibition analysis reveals the mechanism of selectivity of a series of aggrecanase inhibitors (2009), J. Biol. Chem., 284, 24185-24191.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.24.82

Application

Application Comment Organism
medicine design and development for potent and selective inhibitors of ADAMTS-4 and ADAMTS-5, which will be required for chronic osteoarthritis therapy Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Sf9 cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(2R)-N4-hydroxy-2-(3-hydroxybenzyl)-N1-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide
-
 Homo sapiens
(3R)-N2-(cyclopropylmethyl)-N1-hydroxy-3-(3-hydroxybenzyl)-N4-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-L-aspartamide
-
 Homo sapiens
marimastat
-
 Homo sapiens
additional information design and development for potent and selective inhibitors of ADAMTS-4 and ADAMTS-5 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
aggrecan + H2O Homo sapiens ADAMTS-4 and ADAMTS-5 are the proteases responsible for the endogenous aggrecanase activity observed in IL-1beta stimulated bovine cartilage ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
aggrecan + H2O ADAMTS-4 and ADAMTS-5 are the proteases responsible for the endogenous aggrecanase activity observed in IL-1beta stimulated bovine cartilage Homo sapiens ?
-
 ?
aggrecan + H2O cleavage at the Glu373-Ala374 site of aggrecan is measured Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
ADAMTS-4
-
 Homo sapiens
aggrecanase-1
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
 assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000003
-
 pH 7.5, 37°C Homo sapiens (3R)-N2-(cyclopropylmethyl)-N1-hydroxy-3-(3-hydroxybenzyl)-N4-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-L-aspartamide
0.000065
-
 pH 7.5, 37°C Homo sapiens (2R)-N4-hydroxy-2-(3-hydroxybenzyl)-N1-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide
0.000079
-
 pH 7.5, 37°C Homo sapiens marimastat