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Literature summary for 3.4.21.75 extracted from
- Selective and potent furin inhibitors protect cells from anthrax without significant toxicity (2010), Int. J. Biochem. Cell Biol., 42, 987-995.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expression in Spodoptera frugiperda Sf9 cells using the baculovirus transfection system | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 11-amino-undecanoyl-RARRRKKRT | - |
Homo sapiens |  |
| 4,6-bis(4-guanidinylphenoxy)-1-guanidinyl-3-(4-guanidinylphenylamino)cyclohexane | - |
Homo sapiens | |
| 8-amino-octanoyl-RARRRKKRT | - |
Homo sapiens | |
| acetyl-RARRRKKRT | - |
Homo sapiens | |
| beta-Ala-TPRARRRKKRT-amide | - |
Homo sapiens | |
| cholyl-RARRRKKRT | - |
Homo sapiens | |
| decanoyl-Arg-Val-Lys-Arg-chloromethylketone | - |
Homo sapiens | |
| additional information | EC values of furin inhibitors, overview. Inhibition of cell-surface PA83 processing in cell-based assays, overview | Homo sapiens | |
| N-[5-guanidino-2,4-bis-(4-guanidino-phenoxy)-cyclohexyl]-guanidine | - |
Homo sapiens | |
| N-[5-guanidino-2,4-bis-(5-guanidino-pyridin-2-yloxy)-cyclohexyl]-guanidine | - |
Homo sapiens | |
| RARRRKKRT | - |
Homo sapiens | |
| TPRARRRKKRT | - |
Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| cell surface | - |
Homo sapiens | 9986 | - |
| Golgi apparatus | - |
Homo sapiens | 5794 | - |
| additional information | furin is present both in the intracellular secretory pathway and at the cell surface | Homo sapiens | - |
- |
| secretory vesicle | - |
Homo sapiens | 99503 | - |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Ca2+ | required | Homo sapiens | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| membrane type-1 matrix metalloproteinase proenzyme + H2O | Homo sapiens | intracellular processing in breast carcinoma MCF-MT1-E240A-FLAG cells | membrane type-1 matrix metalloproteinase + propeptide of membrane type-1 matrix metalloproteinase | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| recombinant furin from the stably transfected Sf9 insect cells | Homo sapiens |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| breast cancer cell | - |
Homo sapiens | - |
| glioma cell | - |
Homo sapiens | - |
| HT-1080 cell | - |
Homo sapiens | - |
| MCF-7 cell | - |
Homo sapiens | - |
| U-251 MG cell | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| anthrax protective antigen-83 + H2O | - |
Homo sapiens | ? | - |
? | |
| glycoprotein 160 + H2O | from HIV-1, low activity | Homo sapiens | ? | - |
? | |
| hemagglutinin + H2O | from avian influenza H5N1 virus, high activity | Homo sapiens | ? | - |
? | |
| membrane type-1 matrix metalloproteinase proenzyme + H2O | - |
Homo sapiens | membrane type-1 matrix metalloproteinase + propeptide of membrane type-1 matrix metalloproteinase | - |
? | |
| membrane type-1 matrix metalloproteinase proenzyme + H2O | intracellular processing in breast carcinoma MCF-MT1-E240A-FLAG cells | Homo sapiens | membrane type-1 matrix metalloproteinase + propeptide of membrane type-1 matrix metalloproteinase | - |
? | |
| pyroglutamic acid-RTKR-4-methylcoumarin 7-amide + H2O | - |
Homo sapiens | pyroglutamic acid-RTKR + 7-amino-4-methylcoumarin | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| Proprotein convertase | - |
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 |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0000065 | - |
acetyl-RARRRKKRT | pH 7.5, 37°C | Homo sapiens | |
| 0.000008 | - |
RARRRKKRT | pH 7.5, 37°C | Homo sapiens | |
| 0.0000083 | - |
8-amino-octanoyl-RARRRKKRT | pH 7.5, 37°C | Homo sapiens | |
| 0.0000089 | - |
11-amino-undecanoyl-RARRRKKRT | pH 7.5, 37°C | Homo sapiens | |
| 0.0000152 | - |
cholyl-RARRRKKRT | pH 7.5, 37°C | Homo sapiens | |
| 0.000023 | - |
TPRARRRKKRT | pH 7.5, 37°C | Homo sapiens | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.000023 | - |
pH 7.5, 37°C | Homo sapiens | beta-Ala-TPRARRRKKRT-amide | |
General Information
| General Information | Comment | Organism |
|---|---|---|
| physiological function | furin and related proprotein convertases cleave the multibasic motifs R-X-R/K/X-R in the precursor proteins and, as a result, transform the latent proproteins into biologically active proteins and peptides | Homo sapiens |
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Release 2023.1 (January 2023)
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