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Literature summary for 3.4.24.86 extracted from
- Stabilization of the autoproteolysis of TNF-alpha converting enzyme (TACE) results in a novel crystal form suitable for structure-based drug design studies (2006), Protein Eng., 19, 155-161.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expressed in Trichoplusia Ni cells (High-5 cells9) | Homo sapiens |
Crystallization (Commentary)
| Crystallization (Comment) | Organism |
|---|---|
| hanging drop vapour diffusion method with 15% polyethylene glycol 4000, 10% 2-propanol, 100 mM sodium citrate (pH 5.6) | Homo sapiens |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| V353G | highly resistant to autoproteolysis, shows similar kinetic properties to wild type TACE | Homo sapiens |
| V353S | highly resistant to autoproteolysis | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| JMV 390 | - |
Homo sapiens |  |
| TAPI-2 | - |
Homo sapiens | |
Molecular Weight [Da]
| Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
|---|---|---|---|
| 16060 | - |
mature enzyme, estimated from amino acid sequence | Homo sapiens |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| Ni-NTA column chromatography and Superdex-75 gel filtration | Homo sapiens |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| (7-methoxycoumarin-4-yl)-acetyl-KSPLAQA-VRSSSRK(2,4-dinitrophenyl)-NH2 + H2O | - |
Homo sapiens | ? | - |
? | |
| acetyl-SPLAQAVRSSSR-COOH + H2O | - |
Homo sapiens | acetyl-SPLAQA + VRSSSR-COOH | - |
? | |
| additional information | protein in the absence of salt or inhibitor shows a rapid and specific autocleavage between residues Y352-V353 which resides within the surrounding sequence TLGLAYVGSPRN | Homo sapiens | ? | - |
? | |
| proTNF-alpha + H2O | - |
Homo sapiens | soluble TNF-alpha | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| ADAM17 | - |
Homo sapiens |
| TACE | - |
Homo sapiens |
| TNF-alpha converting enzyme | - |
Homo sapiens |
| tumor necrosis factor-alpha converting enzyme | - |
Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.000041 | - |
mutant enzyme V353G | Homo sapiens | TAPI-2 | |
| 0.000043 | - |
wild type enzyme | Homo sapiens | TAPI-2 | |
| 0.00006 | - |
mutant enzyme V353G | Homo sapiens | JMV 390 | |
| 0.000065 | - |
wild type enzyme | Homo sapiens | JMV 390 | |
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Release 2023.1 (January 2023)
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