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Literature summary for 2.1.1.67 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 PubMed
Search for more literature for 2.1.1.67

Application

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(Commentary)

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 (Commentary)

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

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 [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

Organism UniProt Comment Textmining
Homo sapiens P51580
-
-
Mus musculus O55060
-
-

Purification (Commentary)

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 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-mercaptopurine
-
 Mus musculus S-adenosyl-L-homocysteine + 6-methylmercaptopurine
-
 ?

Synonyms

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

Temperature Optimum [°C]

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

pH Optimum

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