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Literature summary for 3.4.24.15 extracted from

  • Bruce, L.A.; Sigman, J.A.; Randall, D.; Rodriguez, S.; Song, M.M.; Dai, Y.; Elmore, D.E.; Pabon, A.; Glucksman, M.J.; Wolfson, A.J.
    Hydrogen bond residue positioning in the 599-611 loop of thimet oligopeptidase is required for substrate selection (2008), FEBS J., 275, 5607-5617.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.24.15

Protein Variants

Protein Variants Comment Organism
G599A decrease in the activity towards the 7-methoxycoumarin-4-acetyl-Pro-Leu-Gly-Pro-Lys-dinitrophenol and 7-methoxycoumarin-Leu-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Lys(Dnp)-OH substrates, with little effect or in activity towards 7-methoxycoumarin-4-acetyl-[Ala7, Lys(dinitrophenol)9]-bradykinin Rattus norvegicus
G603A increase in preference for the five-residue 7-methoxycoumarin-4-acetyl-Pro-Leu-Gly-Pro-Lys-dinitrophenol substrate and, to a lesser extent, for the 10-residue 7-methoxycoumarin-Leu-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Lys(Dnp)-OH substrate Rattus norvegicus
G603A/G604A increase in preference for the five-residue 7-methoxycoumarin-4-acetyl-Pro-Leu-Gly-Pro-Lys-dinitrophenol substrate and, to a lesser extent, for the 10-residue 7-methoxycoumarin-Leu-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Lys(Dnp)-OH substrate Rattus norvegicus
G603P decrease in catalytic activity towards all substrates tested Rattus norvegicus
G604A decrease in the activity towards the 7-methoxycoumarin-4-acetyl-Pro-Leu-Gly-Pro-Lys-dinitrophenol and 7-methoxycoumarin-Leu-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Lys(Dnp)-OH substrates, with little effect or in activity towards 7-methoxycoumarin-4-acetyl-[Ala7, Lys(dinitrophenol)9]-bradykinin Rattus norvegicus
G611A decrease in the activity towards the 7-methoxycoumarin-4-acetyl-Pro-Leu-Gly-Pro-Lys-dinitrophenol and 7-methoxycoumarin-Leu-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Lys(Dnp)-OH substrates, with little effect or in activity towards 7-methoxycoumarin-4-acetyl-[Ala7, Lys(dinitrophenol)9]-bradykinin Rattus norvegicus
Y605F considerable decrease in catalytic activity Rattus norvegicus
Y605F/Y612F marked decrease in catalytic activity, but neither Y605 nor Y612 is necessary for hydrolysis of 7-methoxycoumarin-4-acetyl-[Ala7, Lys(dinitrophenol)9]-bradykinin Rattus norvegicus
Y612F marked decrease in catalytic activity Rattus norvegicus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.000041
-
 7-methoxycoumarin-4-acetyl-[Ala7, Lys(dinitrophenol)9]-bradykinin mutant G603A/G604A, 23°C, pH 7.8 Rattus norvegicus
0.000054
-
 7-methoxycoumarin-4-acetyl-[Ala7, Lys(dinitrophenol)9]-bradykinin mutant G603A, 23°C, pH 7.8 Rattus norvegicus
0.000057
-
 7-methoxycoumarin-4-acetyl-[Ala7, Lys(dinitrophenol)9]-bradykinin wild-type, 23°C, pH 7.8 Rattus norvegicus
0.00008
-
 7-methoxycoumarin-4-acetyl-[Ala7, Lys(dinitrophenol)9]-bradykinin mutant Y605F, 23°C, pH 7.8 Rattus norvegicus
0.00009
-
 7-methoxycoumarin-4-acetyl-[Ala7, Lys(dinitrophenol)9]-bradykinin mutant G604A, 23°C, pH 7.8 Rattus norvegicus
0.000129
-
 7-methoxycoumarin-4-acetyl-[Ala7, Lys(dinitrophenol)9]-bradykinin mutant G599A, 23°C, pH 7.8 Rattus norvegicus
0.000136
-
 7-methoxycoumarin-4-acetyl-[Ala7, Lys(dinitrophenol)9]-bradykinin mutant G611A, 23°C, pH 7.8 Rattus norvegicus
0.00051
-
 7-methoxycoumarin-4-acetyl-[Ala7, Lys(dinitrophenol)9]-bradykinin mutant Y605FY612F, 23°C, pH 7.8 Rattus norvegicus
0.00057
-
 7-methoxycoumarin-4-acetyl-[Ala7, Lys(dinitrophenol)9]-bradykinin mutant Y612F, 23°C, pH 7.8 Rattus norvegicus
0.0012
-
 (7-methoxycoumarin-4-yl)acetyl-Leu-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Lys(Dnp)-OH wild-type, 23°C, pH 7.8 Rattus norvegicus
0.0021
-
 7-methoxycoumarin-4-acetyl-[Ala7, Lys(dinitrophenol)9]-bradykinin mutant G603P, 23°C, pH 7.8 Rattus norvegicus
0.0025
-
 (7-methoxycoumarin-4-yl)acetyl-Leu-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Lys(Dnp)-OH mutant G599A, 23°C, pH 7.8 Rattus norvegicus
0.0026
-
 (7-methoxycoumarin-4-yl)acetyl-Leu-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Lys(Dnp)-OH mutant G604A, 23°C, pH 7.8 Rattus norvegicus
0.0026
-
 (7-methoxycoumarin-4-yl)acetyl-Leu-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Lys(Dnp)-OH mutant Y612F, 23°C, pH 7.8 Rattus norvegicus
0.0029
-
 (7-methoxycoumarin-4-yl)acetyl-Leu-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Lys(Dnp)-OH mutant G603A, 23°C, pH 7.8 Rattus norvegicus
0.0029
-
 (7-methoxycoumarin-4-yl)acetyl-Leu-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Lys(Dnp)-OH mutant G603P, 23°C, pH 7.8 Rattus norvegicus
0.0031
-
 (7-methoxycoumarin-4-yl)acetyl-Leu-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Lys(Dnp)-OH mutant Y605FY612F, 23°C, pH 7.8 Rattus norvegicus
0.00401
-
 7-methoxycoumarin-4-acetyl-Pro-Leu-Gly-Pro-Lys-dinitrophenol mutant G603A, 23°C, pH 7.8 Rattus norvegicus
0.00408
-
 7-methoxycoumarin-4-acetyl-Pro-Leu-Gly-Pro-Lys-dinitrophenol mutant G599A, 23°C, pH 7.8 Rattus norvegicus
0.0042
-
 (7-methoxycoumarin-4-yl)acetyl-Leu-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Lys(Dnp)-OH mutant Y605F, 23°C, pH 7.8 Rattus norvegicus
0.005
-
 (7-methoxycoumarin-4-yl)acetyl-Leu-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Lys(Dnp)-OH mutant G611A, 23°C, pH 7.8 Rattus norvegicus
0.00543
-
 7-methoxycoumarin-4-acetyl-Pro-Leu-Gly-Pro-Lys-dinitrophenol mutant G603A/G604A, 23°C, pH 7.8 Rattus norvegicus
0.0057
-
 (7-methoxycoumarin-4-yl)acetyl-Leu-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Lys(Dnp)-OH mutant G603A/G604A, 23°C, pH 7.8 Rattus norvegicus
0.00643
-
 7-methoxycoumarin-4-acetyl-Pro-Leu-Gly-Pro-Lys-dinitrophenol mutant G603P, 23°C, pH 7.8 Rattus norvegicus
0.0067
-
 7-methoxycoumarin-4-acetyl-Pro-Leu-Gly-Pro-Lys-dinitrophenol mutant G611A, 23°C, pH 7.8 Rattus norvegicus
0.00788
-
 7-methoxycoumarin-4-acetyl-Pro-Leu-Gly-Pro-Lys-dinitrophenol wild-type, 23°C, pH 7.8 Rattus norvegicus
0.0081
-
 7-methoxycoumarin-4-acetyl-Pro-Leu-Gly-Pro-Lys-dinitrophenol mutant Y605FY612F, 23°C, pH 7.8 Rattus norvegicus
0.0082
-
 7-methoxycoumarin-4-acetyl-Pro-Leu-Gly-Pro-Lys-dinitrophenol mutant Y605F, 23°C, pH 7.8 Rattus norvegicus
0.00825
-
 7-methoxycoumarin-4-acetyl-Pro-Leu-Gly-Pro-Lys-dinitrophenol mutant G604A, 23°C, pH 7.8 Rattus norvegicus
0.009
-
 7-methoxycoumarin-4-acetyl-Pro-Leu-Gly-Pro-Lys-dinitrophenol mutant Y612F, 23°C, pH 7.8 Rattus norvegicus
0.014
-
 (7-methoxycoumarin-4-yl)acetyl-Glu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-OH mutant Y605FY612F, 23°C, pH 7.8 Rattus norvegicus
0.024
-
 (7-methoxycoumarin-4-yl)acetyl-Glu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-OH wild-type, 23°C, pH 7.8 Rattus norvegicus
0.034
-
 (7-methoxycoumarin-4-yl)acetyl-Glu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-OH mutant Y612F, 23°C, pH 7.8 Rattus norvegicus
0.037
-
 (7-methoxycoumarin-4-yl)acetyl-Glu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-OH mutant Y605F, 23°C, pH 7.8 Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(7-methoxycoumarin-4-yl)acetyl-Glu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-OH + H2O
-
 Rattus norvegicus (7-methoxycoumarin-4-yl)acetyl-Glu-His-Trp-Ser-Tyr + Gly-Leu-Arg-Pro-OH
-
 ?
(7-methoxycoumarin-4-yl)acetyl-Leu-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Lys(Dnp)-OH + H2O in wild-type, clear preference for the 7-methoxycoumarin-4-acetyl-[Ala7, Lys(dinitrophenol)9]-bradykinin substrate over 7-methoxycoumarin-4-acetyl-Pro-Leu-Gly-Pro-Lys-dinitrophenol and 7-methoxycoumarin-Leu-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Lys(Dnp)-OH Rattus norvegicus ?
-
 ?
(7-methoxycoumarin-4-yl)actayl-Glu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-OH + H2O
-
 Rattus norvegicus ?
-
 ?
7-methoxycoumarin-4-acetyl-Pro-Leu-Gly-Pro-Lys-dinitrophenol + H2O in wild-type, clear preference for the 7-methoxycoumarin-4-acetyl-[Ala7, Lys(dinitrophenol)9]-bradykinin substrate over 7-methoxycoumarin-4-acetyl-Pro-Leu-Gly-Pro-Lys-dinitrophenol and 7-methoxycoumarin-Leu-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Lys(Dnp)-OH Rattus norvegicus ?
-
 ?
7-methoxycoumarin-4-acetyl-[Ala7, Lys(dinitrophenol)9]-bradykinin + H2O in wild-type, clear preference for the 7-methoxycoumarin-4-acetyl-[Ala7, Lys(dinitrophenol)9]-bradykinin substrate over 7-methoxycoumarin-4-acetyl-Pro-Leu-Gly-Pro-Lys-dinitrophenol and 7-methoxycoumarin-Leu-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Lys(Dnp)-OH Rattus norvegicus ?
-
 ?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.00037
-
 7-methoxycoumarin-4-acetyl-Pro-Leu-Gly-Pro-Lys-dinitrophenol mutant Y612F, 23°C, pH 7.8 Rattus norvegicus
0.00052
-
 (7-methoxycoumarin-4-yl)acetyl-Leu-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Lys(Dnp)-OH mutant Y612F, 23°C, pH 7.8 Rattus norvegicus
0.0015
-
 (7-methoxycoumarin-4-yl)acetyl-Leu-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Lys(Dnp)-OH mutant Y605FY612F, 23°C, pH 7.8 Rattus norvegicus
0.0023
-
 7-methoxycoumarin-4-acetyl-Pro-Leu-Gly-Pro-Lys-dinitrophenol mutant Y605FY612F, 23°C, pH 7.8 Rattus norvegicus
0.0026
-
 7-methoxycoumarin-4-acetyl-Pro-Leu-Gly-Pro-Lys-dinitrophenol mutant G603P, 23°C, pH 7.8 Rattus norvegicus
0.00449
-
 (7-methoxycoumarin-4-yl)acetyl-Leu-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Lys(Dnp)-OH mutant G603P, 23°C, pH 7.8 Rattus norvegicus
0.0086
-
 7-methoxycoumarin-4-acetyl-Pro-Leu-Gly-Pro-Lys-dinitrophenol mutant Y605F, 23°C, pH 7.8 Rattus norvegicus
0.012
-
 (7-methoxycoumarin-4-yl)acetyl-Leu-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Lys(Dnp)-OH mutant Y605F, 23°C, pH 7.8 Rattus norvegicus
0.025
-
 (7-methoxycoumarin-4-yl)acetyl-Glu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-OH mutant Y605FY612F, 23°C, pH 7.8 Rattus norvegicus
0.03
-
 7-methoxycoumarin-4-acetyl-Pro-Leu-Gly-Pro-Lys-dinitrophenol mutant G599A, 23°C, pH 7.8 Rattus norvegicus
0.061
-
 (7-methoxycoumarin-4-yl)acetyl-Glu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-OH mutant Y612F, 23°C, pH 7.8 Rattus norvegicus
0.1
-
 7-methoxycoumarin-4-acetyl-[Ala7, Lys(dinitrophenol)9]-bradykinin mutant Y605FY612F, 23°C, pH 7.8 Rattus norvegicus
0.11
-
 7-methoxycoumarin-4-acetyl-Pro-Leu-Gly-Pro-Lys-dinitrophenol mutant G604A, 23°C, pH 7.8 Rattus norvegicus
0.11
-
 (7-methoxycoumarin-4-yl)acetyl-Leu-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Lys(Dnp)-OH mutant G604A, 23°C, pH 7.8 Rattus norvegicus
0.18
-
 (7-methoxycoumarin-4-yl)acetyl-Leu-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Lys(Dnp)-OH mutant G599A, 23°C, pH 7.8 Rattus norvegicus
0.18
-
 7-methoxycoumarin-4-acetyl-[Ala7, Lys(dinitrophenol)9]-bradykinin mutant G603P, 23°C, pH 7.8 Rattus norvegicus
0.193
-
 7-methoxycoumarin-4-acetyl-Pro-Leu-Gly-Pro-Lys-dinitrophenol mutant G611A, 23°C, pH 7.8 Rattus norvegicus
0.27
-
 7-methoxycoumarin-4-acetyl-[Ala7, Lys(dinitrophenol)9]-bradykinin mutant G603A/G604A, 23°C, pH 7.8 Rattus norvegicus
0.28
-
 7-methoxycoumarin-4-acetyl-[Ala7, Lys(dinitrophenol)9]-bradykinin mutant G603A, 23°C, pH 7.8 Rattus norvegicus
0.3
-
 (7-methoxycoumarin-4-yl)acetyl-Leu-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Lys(Dnp)-OH mutant G611A, 23°C, pH 7.8 Rattus norvegicus
0.3
-
 7-methoxycoumarin-4-acetyl-[Ala7, Lys(dinitrophenol)9]-bradykinin wild-type, 23°C, pH 7.8 Rattus norvegicus
0.33
-
 (7-methoxycoumarin-4-yl)acetyl-Leu-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Lys(Dnp)-OH wild-type, 23°C, pH 7.8 Rattus norvegicus
0.34
-
 7-methoxycoumarin-4-acetyl-[Ala7, Lys(dinitrophenol)9]-bradykinin mutant Y605F, 23°C, pH 7.8 Rattus norvegicus
0.44
-
 7-methoxycoumarin-4-acetyl-Pro-Leu-Gly-Pro-Lys-dinitrophenol wild-type, 23°C, pH 7.8 Rattus norvegicus
0.53
-
 7-methoxycoumarin-4-acetyl-[Ala7, Lys(dinitrophenol)9]-bradykinin mutant G604A, 23°C, pH 7.8 Rattus norvegicus
0.75
-
 7-methoxycoumarin-4-acetyl-[Ala7, Lys(dinitrophenol)9]-bradykinin mutant Y612F, 23°C, pH 7.8 Rattus norvegicus
0.86
-
 7-methoxycoumarin-4-acetyl-[Ala7, Lys(dinitrophenol)9]-bradykinin mutant G599A, 23°C, pH 7.8 Rattus norvegicus
1.22
-
 (7-methoxycoumarin-4-yl)acetyl-Leu-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Lys(Dnp)-OH mutant G603A/G604A, 23°C, pH 7.8 Rattus norvegicus
1.26
-
 (7-methoxycoumarin-4-yl)acetyl-Leu-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Lys(Dnp)-OH mutant G603A, 23°C, pH 7.8 Rattus norvegicus
1.34
-
 7-methoxycoumarin-4-acetyl-[Ala7, Lys(dinitrophenol)9]-bradykinin mutant G611A, 23°C, pH 7.8 Rattus norvegicus
1.4
-
 (7-methoxycoumarin-4-yl)acetyl-Glu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-OH mutant Y605F, 23°C, pH 7.8 Rattus norvegicus
2.32
-
 7-methoxycoumarin-4-acetyl-Pro-Leu-Gly-Pro-Lys-dinitrophenol mutant G603A, 23°C, pH 7.8 Rattus norvegicus
2.44
-
 7-methoxycoumarin-4-acetyl-Pro-Leu-Gly-Pro-Lys-dinitrophenol mutant G603A/G604A, 23°C, pH 7.8 Rattus norvegicus
11.2
-
 (7-methoxycoumarin-4-yl)acetyl-Glu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-OH wild-type, 23°C, pH 7.8 Rattus norvegicus