Application | Comment | Organism |
---|---|---|
medicine | thiopurine S-methyltransferase modulates the cytotoxic effects of thiopurine prodrugs such as 6-mercaptopurine by methylating them in a reaction using S-adenosyl-L-methionine as the donor | Homo sapiens |
medicine | thiopurine S-methyltransferase modulates the cytotoxic effects of thiopurine prodrugs such as 6-mercaptopurine by methylating them in a reaction using S-adenosyl-L-methionine as the donor | Mus musculus |
Cloned (Comment) | Organism |
---|---|
the full-length coding region is amplified by PCR from a eukaryotic expression plasmid and cloned into the pET-28a vector for expression in Escherichia coli BL21DE3 cells | Homo sapiens |
the full-length coding region is amplified by PCR from a eukaryotic expression plasmid and cloned into the pET-28a vector for expression in Escherichia coli BL21DE3 cells | Mus musculus |
Crystallization (Comment) | Organism |
---|---|
two crystal structures of murine TPMT are determined, as a binary complex with the product S-adenosyl-L-homocysteine and as a ternary complex with S-adenosyl-L-homocysteine and the substrate 6-mercaptopurine, to 1.8 and 2.0 A resolution, respectively | Mus musculus |
Protein Variants | Comment | Organism |
---|---|---|
R152A | mutant to probe, whether this residue is important for catalysis | Homo sapiens |
R152A/R226A | mutant to probe, whether this residue is important for catalysis | Homo sapiens |
R152E | mutant to probe, whether this residue is important for catalysis | Homo sapiens |
R152H | mutant to probe, whether this residue is important for catalysis | Homo sapiens |
R226A | mutant to probe, whether this residue is important for catalysis | Homo sapiens |
R226E | mutant to probe, whether this residue is important for catalysis | Homo sapiens |
R226H | mutant to probe, whether this residue is important for catalysis | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.00035 | - |
6-Mercaptopurine | - |
Mus musculus | |
0.00068 | - |
6-Mercaptopurine | wild-type | Homo sapiens | |
0.00091 | - |
6-Mercaptopurine | mutant R226H | Homo sapiens | |
0.0012 | - |
6-Mercaptopurine | mutant R226E | Homo sapiens | |
0.00143 | - |
6-Mercaptopurine | mutant R152H | Homo sapiens | |
0.00161 | - |
6-Mercaptopurine | mutant R226A | Homo sapiens | |
0.00273 | - |
6-Mercaptopurine | mutant R152A | Homo sapiens | |
0.00463 | - |
6-Mercaptopurine | mutant R152E | Homo sapiens | |
0.0056 | - |
S-adenosyl-L-methionine | - |
Mus musculus | |
0.00632 | - |
6-Mercaptopurine | mutant R152A/R226A | Homo sapiens | |
0.0148 | - |
S-adenosyl-L-methionine | mutant R226E | Homo sapiens | |
0.0185 | - |
S-adenosyl-L-methionine | wild-type | Homo sapiens | |
0.0197 | - |
S-adenosyl-L-methionine | mutant R226A | Homo sapiens | |
0.0199 | - |
S-adenosyl-L-methionine | mutant R226H | Homo sapiens | |
0.0237 | - |
S-adenosyl-L-methionine | mutant R152H | Homo sapiens | |
0.0254 | - |
S-adenosyl-L-methionine | mutant R152A | Homo sapiens | |
0.0445 | - |
S-adenosyl-L-methionine | mutant R152E | Homo sapiens | |
0.0463 | - |
S-adenosyl-L-methionine | mutant R152A/R226A | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P51580 | - |
- |
Mus musculus | O55060 | - |
- |
Purification (Comment) | Organism |
---|---|
using a Ni2+-NTA resin and a gel-filtration column | Homo sapiens |
using a Ni2+-NTA resin and a gel-filtration column | Mus musculus |
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-mercaptopurine | - |
Mus musculus | S-adenosyl-L-homocysteine + 6-methylmercaptopurine | - |
? |
Synonyms | Comment | Organism |
---|---|---|
thiopurine S-methyltransferase | - |
Homo sapiens |
thiopurine S-methyltransferase | - |
Mus musculus |
TPMT | - |
Homo sapiens |
TPMT | - |
Mus musculus |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
TPMT activity assay | Homo sapiens |
37 | - |
TPMT activity assay | Mus musculus |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
6.5 | - |
TPMT activity assay | Homo sapiens |
6.5 | - |
TPMT activity assay | Mus musculus |