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Literature summary for 3.4.24.18 extracted from

  • Bylander, J.E.; Bertenshaw, G.P.; Matters, G.L.; Hubbard, S.J.; Bond, J.S.
    Human and mouse homo-oligomeric meprin A metalloendopeptidase: substrate and inhibitor specificities (2007), Biol. Chem., 388, 1163-1172.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
actinonin
-
Homo sapiens
actinonin
-
Mus musculus
captopril
-
Homo sapiens
CGS 27023A
-
Homo sapiens
CGS 27023A
-
Mus musculus
CONA 65
-
Homo sapiens
CONA 65
-
Mus musculus
CONA 68
-
Homo sapiens
CONA 68
-
Mus musculus
CONA 71
-
Homo sapiens
CONA 71
-
Mus musculus
CONA 73
-
Homo sapiens
CONA 73
-
Mus musculus
doxycycline
-
Homo sapiens
doxycycline
-
Mus musculus
GM6001 Ilomastat Homo sapiens
GM6001 Ilomastat Mus musculus
homophenylalanine hydroxamate
-
Homo sapiens
homophenylalanine hydroxamate
-
Mus musculus
Pro-Leu-Gly hydroxamate
-
Homo sapiens
Pro-Leu-Gly hydroxamate
-
Mus musculus
TNF-a processing enzyme inhibitor TAPI-2 Homo sapiens
TNF-alpha processing enzyme inhibitor TAPI-2 Mus musculus
tyrosine hydroxamate
-
Homo sapiens
tyrosine hydroxamate
-
Mus musculus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.018
-
protein PTH12-34 hydrolysis in 20 mM Tris-HCl, 150 mM NaCl, pH 7.5 between 8-30 min Homo sapiens
0.0223
-
alpha-MSH meprin A hydrolysis in 20 mM Tris-HCl, 150 mM NaCl, pH 7.5 between 8-30 min Mus musculus
0.0296
-
protein GRP meprin A hydrolysis in 20 mM Tris-HCl, 150 mM NaCl, pH 7.5 between 8-30 min Mus musculus
0.0306
-
Substance P meprin A hydrolysis in 20 mM Tris-HCl, 150 mM NaCl, pH 7.5 between 8-30 min Mus musculus
0.0339
-
secretin hydrolysis in 20 mM Tris-HCl, 150 mM NaCl, pH 7.5 between 8-30 min Homo sapiens
0.0413
-
Substance P hydrolysis in 20 mM Tris-HCl, 150 mM NaCl, pH 7.5 between 8-30 min Homo sapiens
0.0565
-
luteinizing hormone releasing hormone LHRH hydrolysis in 20 mM Tris-HCl, 150 mM NaCl, pH 7.5 between 8-30 min Homo sapiens
0.0672
-
protein PTH12-34 meprin A hydrolysis in 20 mM Tris-HCl, 150 mM NaCl, pH 7.5 between 8-30 min Mus musculus
0.0732
-
orcokinin hydrolysis in 20 mM Tris-HCl, 150 mM NaCl, pH 7.5 between 8-30 min Homo sapiens
0.101
-
bradykinin meprin A hydrolysis in 20 mM Tris-HCl, 150 mM NaCl, pH 7.5 between 8-30 min Mus musculus
0.11
-
GRP hydrolysis in 20 mM Tris-HCl, 150 mM NaCl, pH 7.5 between 8-30 min Homo sapiens
0.111
-
secretin meprin A hydrolysis in 20 mM Tris-HCl, 150 mM NaCl, pH 7.5 between 8-30 min Mus musculus
0.125
-
bradykinin hydrolysis in 20 mM Tris-HCl, 150 mM NaCl, pH 7.5 between 8-30 min Homo sapiens
0.156
-
luteinizing hormone releasing hormone LHRH meprin A hydrolysis in 20 mM Tris-HCl, 150 mM NaCl, pH 7.5 for between 8-30 min Mus musculus
0.2
-
gastrin hydrolysis in 20 mM Tris-HCl, 150 mM NaCl, pH 7.5 between 8-30 min Homo sapiens
0.292
-
alpha-MSH hydrolysis in 20 mM Tris-HCl, 150 mM NaCl, pH 7.5 between 8-30 min Homo sapiens

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
86000
-
monomeric molecular mass of a meprin alpha-subunit Mus musculus
86000
-
monomeric molecular mass of a meprin alpha-subunit Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Mus musculus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HEK-293 cell
-
Homo sapiens
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
2.9
-
specific activity of homo-oligomeric meprin A against PTH Homo sapiens
4.2
-
specific activity of homo-oligomeric meprin A against PTH Mus musculus
2700
-
specific activity of homo-oligomeric meprin A against gelatin Homo sapiens
20500
-
specific activity of homo-oligomeric meprin A against azocasein Mus musculus
20800
-
specific activity of homo-oligomeric meprin A against azocasein Homo sapiens
25000
-
specific activity of homo-oligomeric meprin A against gelatin Mus musculus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
alpha-MSH + H2O
-
Mus musculus ?
-
?
alpha-MSH + H2O
-
Homo sapiens ?
-
?
bradykinin + H2O
-
Mus musculus ?
-
?
bradykinin + H2O
-
Homo sapiens ?
-
?
gastrin + H2O
-
Homo sapiens ?
-
?
GRP + H2O
-
Homo sapiens ?
-
?
luteinizing hormone releasing hormone LHRH + H2O
-
Mus musculus ?
-
?
luteinizing hormone releasing hormone LHRH + H2O
-
Homo sapiens ?
-
?
orcokinin + H2O
-
Homo sapiens ?
-
?
protein GRP + H2O
-
Mus musculus ?
-
?
protein GRP + H2O
-
Homo sapiens ?
-
?
protein LHRH + H2O
-
Mus musculus ?
-
?
protein LHRH + H2O
-
Homo sapiens ?
-
?
protein PTH12-34 + H2O
-
Mus musculus ?
-
?
protein PTH12-34 + H2O
-
Homo sapiens ?
-
?
Secretin + H2O
-
Mus musculus ?
-
?
Secretin + H2O
-
Homo sapiens ?
-
?
Substance P + H2O
-
Mus musculus ?
-
?
Substance P + H2O
-
Homo sapiens ?
-
?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.4
-
gastrin
-
Homo sapiens
3.7
-
bradykinin
-
Homo sapiens
4.4
-
secretin
-
Mus musculus
4.6
-
parathyphoid hormone 12-34
-
Homo sapiens
5.1
-
protein LHRH
-
Homo sapiens
5.2
-
Substance P
-
Homo sapiens
6.3
-
orcokinin
-
Homo sapiens
8.4
-
secretin
-
Homo sapiens
10.5
-
protein PTH12-34
-
Mus musculus
12.1
-
Substance P
-
Mus musculus
16.5
-
alpha-MSH
-
Homo sapiens
16.6
-
bradykinin
-
Mus musculus
19.6
-
protein GRP
-
Homo sapiens
24.6
-
protein GRP
-
Mus musculus
39.4
-
protein LHRH
-
Mus musculus
45.4
-
alpha-MSH
-
Mus musculus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0033
-
-
Mus musculus CONA 65
0.005
-
-
Homo sapiens actinonin
0.008
-
-
Mus musculus CGS 27023A
0.016
-
-
Homo sapiens CGS 27023A
0.04
-
-
Mus musculus CONA 68
0.05
-
-
Homo sapiens CONA 68
0.06
-
Ilomastat Homo sapiens GM6001
0.065
-
-
Homo sapiens CONA 73
0.08
-
-
Homo sapiens TNF-alpha processing enzyme inhibitor
0.1
-
-
Homo sapiens tyrosine hydroxamate
0.1
-
-
Homo sapiens homophenylalanine hydroxamate
0.17
-
-
Homo sapiens CONA 71
0.18
-
-
Mus musculus actinonin
0.25
-
-
Mus musculus CONA 71
0.31
-
-
Mus musculus CONA 73
0.4
-
-
Homo sapiens Pro-Leu-Gly hydroxamate
0.6
-
Ilomastat Mus musculus GM6001
0.8
-
-
Mus musculus homophenylalanine hydroxamate
0.8
-
-
Mus musculus TNF-alpha processing enzyme inhibitor
1.1
-
-
Mus musculus tyrosine hydroxamate
2
-
-
Homo sapiens CONA 65
12
-
-
Homo sapiens doxycycline
16
-
-
Mus musculus Pro-Leu-Gly hydroxamate
20
-
-
Mus musculus doxycycline
40
-
-
Homo sapiens captopril