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Literature summary for 2.1.1.67 extracted from
- Characterisation of novel defective thiopurine S-methyltransferase allelic variants (2008), Biochem. Pharmacol., 76, 404-415.
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | thiopurine S-methyltransferase is a key enzyme in the detoxification of thiopurine drugs widely used in the treatment of various diseases, such as inflammatory bowel diseases, acute lymphoblastic leukaemia and rheumatic diseases | Homo sapiens |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| into the yeast expression vector pYeDP60 for transformation of Saccharomyces cerevisiae cells | Homo sapiens |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| C212R | polymorphism c.634T>C, TPMT*25 | Homo sapiens |
| K119T | polymorphism c.356A>C, TPMT*9 | Homo sapiens |
| L69V | polymorphism c.205C>G, TPMT*21 | Homo sapiens |
| Q179H | polymorphism c.537G>T, TPMT*24 | Homo sapiens |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0137 | - |
6-thioguanine | mutant L69V, cytosolic fraction of yeast cells is incubated with 500 microM of 6-TG and 0-400 microM of SAM | Homo sapiens |  |
| 0.03435 | - |
6-thioguanine | wild-type enzyme, cytosolic fraction of yeast cells is incubated with 500 microM of 6-TG and 0-400 microM of SAM | Homo sapiens | |
| 0.0562 | - |
6-thioguanine | mutant L69V, cytosolic fraction of yeast cells is incubated with 0-350 microM of 6-TG and 1mM of SAM | Homo sapiens | |
| 0.0627 | - |
6-thioguanine | wild-type enzyme, cytosolic fraction of yeast cells is incubated with 0-350 microM of 6-TG and 1mM of SAM | Homo sapiens | |
| 0.072 | - |
6-thioguanine | mutant C212R, cytosolic fraction of yeast cells is incubated with 0-350 microM of 6-TG and 1mM of SAM | Homo sapiens | |
| 0.07985 | - |
6-thioguanine | mutant K119T, cytosolic fraction of yeast cells is incubated with 0-350 microM of 6-TG and 1mM of SAM | Homo sapiens | |
| 0.08305 | - |
6-thioguanine | mutant Q179H, cytosolic fraction of yeast cells is incubated with 0-350 microM of 6-TG and 1mM of SAM | Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| cytosol | - |
Homo sapiens | 5829 | - |
Molecular Weight [Da]
| Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
|---|---|---|---|
| 33000 | - |
determined by SDS-PAGE and immunoblotting | Homo sapiens |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| S-adenosyl-L-methionine + a thiopurine | Homo sapiens | - |
S-adenosyl-L-homocysteine + a thiopurine S-methylether | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | P51580 | - |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| cytosolic fractions of transformed Saccharomyces cerevisiae cells are prepared | Homo sapiens |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| S-adenosyl-L-methionine + 6-mercaptopurine | - |
Homo sapiens | S-adenosyl-L-homocysteine + 6-methylmercaptopurine | - |
? | |
| S-adenosyl-L-methionine + 6-thioguanine | - |
Homo sapiens | S-adenosyl-L-homocysteine + 6-methylthioguanine | - |
? | |
| S-adenosyl-L-methionine + a thiopurine | - |
Homo sapiens | S-adenosyl-L-homocysteine + a thiopurine S-methylether | - |
? | |
| S-adenosyl-L-methionine + azathioprine | azathioprine is converted via a non-enzymatic reaction to mercaptopurine, which is subsequently metabolized through TPMT | Homo sapiens | S-adenosyl-L-homocysteine + 6-methylmercaptopurine + ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| thiopurine S-methyltransferase | - |
Homo sapiens |
| TPMT | - |
Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 37 | - |
6-thioguanine S-methylation assay | Homo sapiens |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.4 | - |
6-thioguanine S-methylation assay | Homo sapiens |
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