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Information on EC 3.4.24.82 - ADAMTS-4 endopeptidase and Organism(s) Rattus norvegicus and UniProt Accession Q9ESP7

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EC Tree
     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.24 Metalloendopeptidases
                3.4.24.82 ADAMTS-4 endopeptidase
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This record set is specific for:
Rattus norvegicus
UNIPROT: Q9ESP7 not found.
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The taxonomic range for the selected organisms is: Rattus norvegicus
The enzyme appears in selected viruses and cellular organisms
Reaction Schemes
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Glutamyl endopeptidase; bonds cleaved include -Thr-Glu-Gly-Glu373-/-Ala-Arg-Gly-Ser- in the interglobular domain of mammalian aggrecan
Synonyms
adamts-4, adamts4, adamts-1, aggrecanase-1, aggrecanase 1, adamts 4, agg-1, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
aggrecanase-1
-
a disintegrin and metalloproteinase with thrombospondin motifs-4
-
-
ADAMTS-4
-
-
aggrecanase-1
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of peptide bond
-
-
-
-
CAS REGISTRY NUMBER
COMMENTARY hide
147172-61-0
-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
brevican + H2O
?
show the reaction diagram
-
-
-
?
neurocan + H2O
?
show the reaction diagram
-
-
-
?
phosphacan + H2O
?
show the reaction diagram
-
-
-
?
aggrecan + H2O
fragments of aggrecan
show the reaction diagram
recombinant Agg1 + H2O
fragments of recombinant Agg1
show the reaction diagram
-
rAGG1 is composed of the complete interglobular domain, i.e. IGD, of human aggrecan, flanked by the marker sequences FLAG at the amino terminus and human immunglobulin G1 constant region at the C-terminus
-
?
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
aggrecan + H2O
fragments of aggrecan
show the reaction diagram
-
-
-
-
?
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
interleukin-1beta
lower mRNA level of aggrecan
-
(2R)-2-(biphenyl-4-ylsulfonyl)-3-(1H-indol-2-yl)propanoic acid
-
IC50: 0.0028 mM
(2R)-2-(biphenyl-4-ylsulfonyl)-3-phenylpropanoic acid
-
IC50: 0.0043 mM
(2R)-2-(biphenyl-4-ylsulfonyl)pentanedioic acid
-
IC50: 0.0011 mM
(2R)-2-(biphenyl-4-ylsulfonyl)propanoic acid
-
IC50: 0.0055 mM
3-[(biphenyl-4-ylsulfonyl)amino]-4-methylpentanoic acid
-
IC50: 0.1 mM
N-(biphenyl-3-ylsulfonyl)-D-valine
-
IC50: 0.1 mM
N-(biphenyl-4-ylsulfonyl)-D-valine
-
IC50: 0.003 mM
N-(biphenyl-4-ylsulfonyl)-L-valine
-
IC50: 0.1 mM
N-(biphenyl-4-ylsulfonyl)-N-(pyridin-3-ylmethyl)-D-valine
-
IC50: 0.012 mM
N-(biphenyl-4-ylsulfonyl)-N-methyl-D-valine
-
IC50: 0.0016 mM
N-([4'-[(1-benzofuran-2-ylcarbonyl)amino]biphenyl-4-yl]sulfonyl)-D-valine
-
IC50: 0.0075 mM
N-([4'-[(1-benzofuran-2-ylcarbonyl)oxy]biphenyl-4-yl]sulfonyl)-D-valine
-
IC50: 0.00035 mM
N-([4'-[(furan-2-yloxy)carbonyl]biphenyl-4-yl]sulfonyl)-D-valine
-
IC50: 0.0116 mM
N-([4'-[(Z)-2-(1-benzofuran-2-yl)ethenyl]biphenyl-4-yl]sulfonyl)-D-valine
-
IC50: 0.0004 mM
N-([4'-[2-(1-benzofuran-2-yl)-2-oxoethyl]biphenyl-4-yl]sulfonyl)-D-valine
-
IC50: 0.0038 mM
N-[(2'-aminobiphenyl-4-yl)sulfonyl]-D-valine
-
IC50: 0.05 mM
N-[(2'-hydroxybiphenyl-4-yl)sulfonyl]-D-valine
-
IC50: 0.02 mM
N-[(2-aminobiphenyl-4-yl)sulfonyl]-D-valine
-
IC50: 0.03 mM
N-[(3'-hydroxybiphenyl-4-yl)sulfonyl]-D-valine
-
IC50: 0.009 mM
N-[(4'-hydroxybiphenyl-4-yl)sulfonyl]-D-valine
-
IC50: 0.0046 mM
N-[(4'-[[(3-methyl-1-benzofuran-2-yl)carbonyl]oxy]biphenyl-4-yl)sulfonyl]-D-valine
-
IC50: 0.000086 mM
N-[(4'-[[(3-methyl-1-benzofuran-2-yl)oxy]methyl]biphenyl-4-yl)sulfonyl]-D-valine
-
IC50: 0.0007 mM
N-[[4'-(1-benzofuran-2-ylmethoxy)biphenyl-4-yl]sulfonyl]-D-valine
-
IC50: 0.0014 mM
tissue inhibitor of metalloproteinases 3
-
-
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
tumour necrosis factor
-
-
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0028
(2R)-2-(biphenyl-4-ylsulfonyl)-3-(1H-indol-2-yl)propanoic acid
Rattus norvegicus
-
IC50: 0.0028 mM
0.0043
(2R)-2-(biphenyl-4-ylsulfonyl)-3-phenylpropanoic acid
Rattus norvegicus
-
IC50: 0.0043 mM
0.0011
(2R)-2-(biphenyl-4-ylsulfonyl)pentanedioic acid
Rattus norvegicus
-
IC50: 0.0011 mM
0.0055
(2R)-2-(biphenyl-4-ylsulfonyl)propanoic acid
Rattus norvegicus
-
IC50: 0.0055 mM
0.1
3-[(biphenyl-4-ylsulfonyl)amino]-4-methylpentanoic acid
Rattus norvegicus
-
IC50: 0.1 mM
0.1
N-(biphenyl-3-ylsulfonyl)-D-valine
Rattus norvegicus
-
IC50: 0.1 mM
0.003
N-(biphenyl-4-ylsulfonyl)-D-valine
Rattus norvegicus
-
IC50: 0.003 mM
0.1
N-(biphenyl-4-ylsulfonyl)-L-valine
Rattus norvegicus
-
IC50: 0.1 mM
0.012
N-(biphenyl-4-ylsulfonyl)-N-(pyridin-3-ylmethyl)-D-valine
Rattus norvegicus
-
IC50: 0.012 mM
0.0016
N-(biphenyl-4-ylsulfonyl)-N-methyl-D-valine
Rattus norvegicus
-
IC50: 0.0016 mM
0.0075
N-([4'-[(1-benzofuran-2-ylcarbonyl)amino]biphenyl-4-yl]sulfonyl)-D-valine
Rattus norvegicus
-
IC50: 0.0075 mM
0.00035
N-([4'-[(1-benzofuran-2-ylcarbonyl)oxy]biphenyl-4-yl]sulfonyl)-D-valine
Rattus norvegicus
-
IC50: 0.00035 mM
0.0116
N-([4'-[(furan-2-yloxy)carbonyl]biphenyl-4-yl]sulfonyl)-D-valine
Rattus norvegicus
-
IC50: 0.0116 mM
0.0004
N-([4'-[(Z)-2-(1-benzofuran-2-yl)ethenyl]biphenyl-4-yl]sulfonyl)-D-valine
Rattus norvegicus
-
IC50: 0.0004 mM
0.0038
N-([4'-[2-(1-benzofuran-2-yl)-2-oxoethyl]biphenyl-4-yl]sulfonyl)-D-valine
Rattus norvegicus
-
IC50: 0.0038 mM
0.05
N-[(2'-aminobiphenyl-4-yl)sulfonyl]-D-valine
Rattus norvegicus
-
IC50: 0.05 mM
0.02
N-[(2'-hydroxybiphenyl-4-yl)sulfonyl]-D-valine
Rattus norvegicus
-
IC50: 0.02 mM
0.03
N-[(2-aminobiphenyl-4-yl)sulfonyl]-D-valine
Rattus norvegicus
-
IC50: 0.03 mM
0.009
N-[(3'-hydroxybiphenyl-4-yl)sulfonyl]-D-valine
Rattus norvegicus
-
IC50: 0.009 mM
0.0046
N-[(4'-hydroxybiphenyl-4-yl)sulfonyl]-D-valine
Rattus norvegicus
-
IC50: 0.0046 mM
0.000086
N-[(4'-[[(3-methyl-1-benzofuran-2-yl)carbonyl]oxy]biphenyl-4-yl)sulfonyl]-D-valine
Rattus norvegicus
-
IC50: 0.000086 mM
0.0007
N-[(4'-[[(3-methyl-1-benzofuran-2-yl)oxy]methyl]biphenyl-4-yl)sulfonyl]-D-valine
Rattus norvegicus
-
IC50: 0.0007 mM
0.0014
N-[[4'-(1-benzofuran-2-ylmethoxy)biphenyl-4-yl]sulfonyl]-D-valine
Rattus norvegicus
-
IC50: 0.0014 mM
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
cell culture, expression of aggrecanase-1 mRNA is induced if cells are treated with beta-amyloid
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
physiological function
ADAMTS-4 digests proteoglycans, and reverses their inhibition of neurite outgrowth. Local administration of ADAMTS-4 significantly promotes motor function recovery after spinal cord injury. The ADAMTS-4-treated spinal cord exhibits enhanced axonal regeneration/sprouting after spinal cord injury
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
ATS4_RAT
630
0
68385
Swiss-Prot
Mitochondrion (Reliability: 5)
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
68000
x * 68000, SDS-PAGE
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
?
x * 68000, SDS-PAGE
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Hughes, C.E.; Buttner, F.H.; Eidenmuller, B.; Caterson, B.; Bartnik, E.
Utilization of a recombinant substrate rAgg1 to study the biochemical properties of aggrecanase in cell culture systems
J. Biol. Chem.
272
20269-20274
1997
Bos taurus, Rattus norvegicus
Manually annotated by BRENDA team
Satoh, K.; Suzuki, N.; Yokota, H.
ADAMTS-4 (a disintegrin and metalloproteinase with thrombospondin motifs) is transcriptionally induced in beta-amyloid treated rat astrocytes
Neurosci. Lett.
289
177-180
2000
Rattus norvegicus (Q9ESP7)
Manually annotated by BRENDA team
Xiang, J.S.; Hu, Y.; Rush, T.S.; Thomason, J.R.; Ipek, M.; Sum, P.E.; Abrous, L.; Sabatini, J.J.; Georgiadis, K.; Reifenberg, E.; Majumdar, M.; Morris, E.A.; Tam, S.
Synthesis and biological evaluation of biphenylsulfonamide carboxylate aggrecanase-1 inhibitors
Bioorg. Med. Chem. Lett.
16
311-316
2006
Rattus norvegicus
Manually annotated by BRENDA team
Cross, A.K.; Haddock, G.; Stock, C.J.; Allan, S.; Surr, J.; Bunning, R.A.; Buttle, D.J.; Woodroofe, M.N.
ADAMTS-1 and -4 are up-regulated following transient middle cerebral artery occlusion in the rat and their expression is modulated by TNF in cultured astrocytes
Brain Res.
1088
19-30
2006
Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Cross, A.K.; Haddock, G.; Surr, J.; Plumb, J.; Bunning, R.A.; Buttle, D.J.; Woodroofe, M.N.
Differential expression of ADAMTS-1, -4, -5 and TIMP-3 in rat spinal cord at different stages of acute experimental autoimmune encephalomyelitis
J. Autoimmun.
26
16-23
2006
Rattus norvegicus
Manually annotated by BRENDA team
Wang, Z.H.; Yang, Z.Q.; He, X.J.; Wang, L.; Li, L.X.; Tu, J.B.
Effects of RNAi-mediated inhibition of aggrecanase-1 and aggrecanase-2 on rat costochondral chondrocytes in vitro
Acta Pharmacol. Sin.
29
1215-1226
2008
Rattus norvegicus (Q9ESP7)
Manually annotated by BRENDA team
Tauchi, R.; Imagama, S.; Natori, T.; Ohgomori, T.; Muramoto, A.; Shinjo, R.; Matsuyama, Y.; Ishiguro, N.; Kadomatsu, K.
The endogenous proteoglycan-degrading enzyme ADAMTS-4 promotes functional recovery after spinal cord injury
J. Neuroinflammation
9
53
2012
Rattus norvegicus (Q9ESP7)
Manually annotated by BRENDA team