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Literature summary for 3.4.21.73 extracted from
- Nonproteolytic induction of catalytic activity into the single-chain form of urokinase-type plasminogen activator by dipeptides (2009), Biochemistry, 48, 9606-9617.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| Ile-Ile | an Ile-Ile or Ile-Val dipeptide can induce limited enzyme activity in the single-chain zymogen form of uPA or its K158A variant, which cannot be activated proteolytically | Homo sapiens |  |
| Ile-Val | an Ile-Ile or Ile-Val dipeptide can induce limited enzyme activity in the single-chain zymogen form of uPA or its K158A variant, which cannot be activated proteolytically | Homo sapiens | |
| additional information | the enzyme is initially synthesized as single-chain proenzyme with an activity that is many orders of magnitude lower than those of the mature enzyme. Proteolytic cleavage of an exposed loop liberates a new amino terminus that inserts into a hydrophobic pocket and forms a stabilizing salt bridge with a ubiquitously conserved aspartate residue, resulting in a conformational change organizing the mature oxyanion hole | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 4-aminobenzamidine | competitive, no inhibition of the pro-uPA | Homo sapiens | |
| amiloride | competitive, no inhibition of the pro-uPA | Homo sapiens | |
| Glu-Gly-Arg-chloromethyl ketone | - |
Homo sapiens | |
| plasminogen activator inhibitor-1 | i.e. PAI-1, recombinantly expressed with an N-terminal His6-tag and purified from Escherichia coli cells, labeled with N,N0-dimethyl-N-(iodoacetyl)-N0-(7-nitrobenz-2-oxa-1,3-diazol-4-yl)ethylenediamine, i.e. P9-NBD-labeled PAI-1. Slow formation of a covalent serpin-protease complex between single-chain uPA and PAI-1 is significantly accelerated in the presence of specific dipeptide sequences | Homo sapiens | |
| upain-1 | competitive, no inhibition of the pro-uPA | Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | kinetic effects of dipeptides on the catalytic activity of single-chain uPA and two-chain uPA toward the chromogenic substrate S-2444, overview | Homo sapiens | |
| 0.1 | - |
pyroGlu-Gly-Arg-4-nitroanilide | pH 7.4, 37°C, pro-uPA | Homo sapiens | |
| 0.13 | - |
pyroGlu-Gly-Arg-4-nitroanilide | pH 7.4, 37°C, mature uPA | Homo sapiens | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| plasminogen + H2O | Homo sapiens | - |
plasmin + ? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Posttranslational Modification
| Posttranslational Modification | Comment | Organism |
|---|---|---|
| proteolytic modification | the enzyme is initially synthesized as single-chain proenzyme with an activity that is many orders of magnitude lower than those of the mature enzyme. Proteolytic cleavage of an exposed loop liberates a new amino terminus that inserts into a hydrophobic pocket and forms a stabilizing salt bridge with a ubiquitously conserved aspartate residue, resulting in a conformational change organizing the mature oxyanion hole | Homo sapiens |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| commercial preparation | recombinant two-chain and single-chain enzyme | Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| plasminogen + H2O | - |
Homo sapiens | plasmin + ? | - |
? | |
| pyroGlu-Gly-Arg-4-nitroanilide + H2O | i.e. S-2444, a chromogenic substrate | Homo sapiens | pyroGlu-Gly-Arg + 4-nitroaniline | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| uPA | - |
Homo sapiens |
| Urokinase-type plasminogen activator | - |
Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 37 | - |
assay at | Homo sapiens |
Turnover Number [1/s]
| Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.73 | - |
pyroGlu-Gly-Arg-4-nitroanilide | pH 7.4, 37°C, pro-uPA | Homo sapiens | |
| 773 | - |
pyroGlu-Gly-Arg-4-nitroanilide | pH 7.4, 37°C, mature uPA | Homo sapiens | |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.4 | - |
assay at | Homo sapiens |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | kinetic effects of dipeptides on the inhibition of single-chain uPA and two-chain uPA, overview. Stopped-flow kinetics of P9-NBD-labeled PAI-1, 25°C, overview | Homo sapiens | |
| 0.0022 | - |
upain-1 | pH 7.4, 37°C, mature uPA | Homo sapiens | |
| 0.005 | - |
amiloride | pH 7.4, 37°C, mature uPA | Homo sapiens | |
| 0.0395 | - |
4-aminobenzamidine | pH 7.4, 37°C, mature uPA | Homo sapiens | |
kcat/KM [mM/s]
| kcat/KM Value [1/mMs-1] | kcat/KM Value Maximum [1/mMs-1] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.12 | - |
pyroGlu-Gly-Arg-4-nitroanilide | pH 7.4, 37°C, pro-uPA | Homo sapiens | |
| 99 | - |
pyroGlu-Gly-Arg-4-nitroanilide | pH 7.4, 37°C, mature uPA | Homo sapiens | |
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