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Literature summary extracted from

  • Peng, Y.; Feng, Q.; Wilk, D.; Adjei, A.A.; Salavaggione, O.E.; Weinshilboum, R.M.; Yee, V.C.
    Structural basis of substrate recognition in thiopurine s-methyltransferase (2008), Biochemistry, 47, 6216-6225.
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
2.1.1.67 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
2.1.1.67 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(Commentary)

EC Number Cloned (Comment) Organism
2.1.1.67 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
2.1.1.67 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 (Commentary)

EC Number Crystallization (Comment) Organism
2.1.1.67 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

EC Number Protein Variants Comment Organism
2.1.1.67 R152A mutant to probe, whether this residue is important for catalysis Homo sapiens
2.1.1.67 R152A/R226A mutant to probe, whether this residue is important for catalysis Homo sapiens
2.1.1.67 R152E mutant to probe, whether this residue is important for catalysis Homo sapiens
2.1.1.67 R152H mutant to probe, whether this residue is important for catalysis Homo sapiens
2.1.1.67 R226A mutant to probe, whether this residue is important for catalysis Homo sapiens
2.1.1.67 R226E mutant to probe, whether this residue is important for catalysis Homo sapiens
2.1.1.67 R226H mutant to probe, whether this residue is important for catalysis Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.1.1.67 0.00035
-
 6-Mercaptopurine
-
 Mus musculus
2.1.1.67 0.00068
-
 6-Mercaptopurine wild-type Homo sapiens
2.1.1.67 0.00091
-
 6-Mercaptopurine mutant R226H Homo sapiens
2.1.1.67 0.0012
-
 6-Mercaptopurine mutant R226E Homo sapiens
2.1.1.67 0.00143
-
 6-Mercaptopurine mutant R152H Homo sapiens
2.1.1.67 0.00161
-
 6-Mercaptopurine mutant R226A Homo sapiens
2.1.1.67 0.00273
-
 6-Mercaptopurine mutant R152A Homo sapiens
2.1.1.67 0.00463
-
 6-Mercaptopurine mutant R152E Homo sapiens
2.1.1.67 0.0056
-
 S-adenosyl-L-methionine
-
 Mus musculus
2.1.1.67 0.00632
-
 6-Mercaptopurine mutant R152A/R226A Homo sapiens
2.1.1.67 0.0148
-
 S-adenosyl-L-methionine mutant R226E Homo sapiens
2.1.1.67 0.0185
-
 S-adenosyl-L-methionine wild-type Homo sapiens
2.1.1.67 0.0197
-
 S-adenosyl-L-methionine mutant R226A Homo sapiens
2.1.1.67 0.0199
-
 S-adenosyl-L-methionine mutant R226H Homo sapiens
2.1.1.67 0.0237
-
 S-adenosyl-L-methionine mutant R152H Homo sapiens
2.1.1.67 0.0254
-
 S-adenosyl-L-methionine mutant R152A Homo sapiens
2.1.1.67 0.0445
-
 S-adenosyl-L-methionine mutant R152E Homo sapiens
2.1.1.67 0.0463
-
 S-adenosyl-L-methionine mutant R152A/R226A Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
2.1.1.67 Homo sapiens P51580
-
-
2.1.1.67 Mus musculus O55060
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.1.1.67 using a Ni2+-NTA resin and a gel-filtration column Homo sapiens
2.1.1.67 using a Ni2+-NTA resin and a gel-filtration column Mus musculus

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.1.1.67 S-adenosyl-L-methionine + 6-mercaptopurine
-
 Homo sapiens S-adenosyl-L-homocysteine + 6-methylmercaptopurine
-
 ?
2.1.1.67 S-adenosyl-L-methionine + 6-mercaptopurine
-
 Mus musculus S-adenosyl-L-homocysteine + 6-methylmercaptopurine
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.1.1.67 thiopurine S-methyltransferase
-
 Homo sapiens
2.1.1.67 thiopurine S-methyltransferase
-
 Mus musculus
2.1.1.67 TPMT
-
 Homo sapiens
2.1.1.67 TPMT
-
 Mus musculus

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.1.1.67 37
-
 TPMT activity assay Homo sapiens
2.1.1.67 37
-
 TPMT activity assay Mus musculus

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.1.1.67 6.5
-
 TPMT activity assay Homo sapiens
2.1.1.67 6.5
-
 TPMT activity assay Mus musculus