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Literature summary for 3.4.24.B12 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.B12

Application

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

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Sf9 cells Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
sitting drop method, crystal structure of the catalytic domain of ADAMTS-5 in complex with marimastat, (2R)-N4-hydroxy-2-(3-hydroxybenzyl)-N1-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide or (3R)-N2-(cyclopropylmethyl)-N1-hydroxy-3-(3-hydroxybenzyl)-N4-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-L-aspartamide 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 Q9UNA0
-
-

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-5
-
 Homo sapiens
aggrecanase-2
-
 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
0.000017
-
 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
0.000093
-
 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
0.000106
-
 pH 7.5, 37°C Homo sapiens marimastat