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Literature summary for 2.1.1.67 extracted from
- Individualization of thiopurine therapy: thiopurine S-methyltransferase and beyond (2009), Pharmacogenomics, 10, 1309-1322.
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | TPMT activity is a good prediction factor for the toxicity and efficacy of the antileukemic thiopurine therapy | Homo sapiens |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| A154T | mutant shows decreased TPMT activity | Homo sapiens |
| A154T/Y240C | mutant shows decreased TPMT activity | Homo sapiens |
| A167G | mutant shows decreased TPMT activity | Homo sapiens |
| A80P | mutant shows decreased TPMT activity | Homo sapiens |
| C132Y | mutant shows decreased TPMT activity | Homo sapiens |
| C212R | mutant shows decreased TPMT activity | Homo sapiens |
| E28V | mutant shows decreased TPMT activity | Homo sapiens |
| G144R | mutant shows decreased TPMT activity | Homo sapiens |
| G36S | mutant shows decreased TPMT activity | Homo sapiens |
| G71R | mutant shows decreased TPMT activity | Homo sapiens |
| H227Q | mutant shows decreased TPMT activity | Homo sapiens |
| K119T | mutant shows decreased TPMT activity | Homo sapiens |
| K122T | mutant shows normal TPMT activity | Homo sapiens |
| K238E | mutant shows decreased TPMT activity | Homo sapiens |
| L49S | mutant shows decreased TPMT activity | Homo sapiens |
| L69V | mutant shows decreased TPMT activity | Homo sapiens |
| Q42E | mutant shows decreased TPMT activity | Homo sapiens |
| R163H | mutant shows decreased TPMT activity | Homo sapiens |
| R163P | mutant shows decreased TPMT activity | Homo sapiens |
| R215H | mutant shows decreased TPMT activity | Homo sapiens |
| S125L | mutant shows decreased TPMT activity | Homo sapiens |
| Y180F | mutant shows decreased TPMT activity | Homo sapiens |
| Y240C | mutant shows decreased TPMT activity | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| additional information | low levels of methionine can result in low S-adenosyl-L-methionine levels and consequently decreased TPMT activity | Homo sapiens |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| additional information | Homo sapiens | S-adenosyl-L-methionine and sinefungin prevent degradation of TPMT by stabilizing ist native structure | ? | - |
? |  |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| erythrocyte | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| additional information | S-adenosyl-L-methionine and sinefungin prevent degradation of TPMT by stabilizing ist native structure | Homo sapiens | ? | - |
? | |
| S-adenosyl-L-methionine + 6-mercaptopurine | TPMT deactivates 6-mercaptopurine by methylation | Homo sapiens | S-adenosyl-L-homocysteine + 6-methylmercaptopurine | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| TPMT | - |
Homo sapiens |
Expression
| Organism | Comment | Expression |
|---|---|---|
| Homo sapiens | S-adenosyl-L-methionine has no effect on TPMT mRNA expression | additional information |
| Homo sapiens | smokers have significantly higher TPMT activity than nonsmokers | up |
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