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EC Tree
IUBMB Comments Also acts, more slowly, on thiopyrimidines and aromatic thiols. Not identical with EC 2.1.1.9 thiol S-methyltransferase.
The taxonomic range for the selected organisms is: Mus musculus The expected taxonomic range for this enzyme is: Bacteria, Eukaryota, Archaea
Synonyms
thiopurine methyltransferase, thiopurine s-methyltransferase, thiopurine methyl transferase, thiopurine-s-methyl-transferase, s-adenosyl-l-methionine:thiopurine s-methyltransferase, 6-thiopurine s-methyltransferase,
more
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thiopurine S-methyltransferase
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6-thiopurine transmethylase
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mercaptopurine methyltransferase
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thiopurine methyltransferase
thiopurine methyltransferase
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thiopurine methyltransferase
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TPMT
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methyl group transfer
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methyl group transfer
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S-adenosyl-L-methionine:thiopurine S-methyltransferase
Also acts, more slowly, on thiopyrimidines and aromatic thiols. Not identical with EC 2.1.1.9 thiol S-methyltransferase.
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S-adenosyl-L-methionine + 6-mercaptopurine
S-adenosyl-L-homocysteine + 6-methylmercaptopurine
S-adenosyl-L-methionine + 6-thioguanine
S-adenosyl-L-homocysteine + 6-methylthioguanine
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-
-
?
S-adenosyl-L-methionine + a thiopurine
S-adenosyl-L-homocysteine + a thiopurine S-methylether
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-
-
?
S-adenosyl-L-methionine + 2,8-dihydroxy-6-thiopurine
S-adenosyl-L-homocysteine + 2,8-dihydroxy-6-methylthiopurine
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-
-
-
?
S-adenosyl-L-methionine + 2-amino-6-thiopurine
S-adenosyl-L-homocysteine + 2-amino-6-methylthiopurine
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-
-
-
?
S-adenosyl-L-methionine + 2-thiothymine
S-adenosyl-L-homocysteine + 2-methylthiothymine
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-
-
-
?
S-adenosyl-L-methionine + 2-thiouracil
S-adenosyl-L-homocysteine + thiouracil-2-S-methylether
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-
-
-
?
S-adenosyl-L-methionine + 6-mercaptopurine
S-adenosyl-L-homocysteine + 6-methylmercaptopurine
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-
-
-
?
S-adenosyl-L-methionine + 6-thioguanine
S-adenosyl-L-homocysteine + 6-methylthioguanine
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-
-
-
?
S-adenosyl-L-methionine + 6-thiopurine
S-adenosyl-L-homocysteine + 6-methylthiopurine
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preferred substrate
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-
?
S-adenosyl-L-methionine + 6-thiouric acid
S-adenosyl-L-homocysteine + 6-methylthiouric acid
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-
-
-
?
S-adenosyl-L-methionine + a thiopurine
S-adenosyl-L-homocysteine + a thiopurine S-methylether
S-adenosyl-L-methionine + azathioprine
?
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-
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?
S-adenosyl-L-methionine + thioguanine nucleotide
S-adenosyl-L-homocysteine + methylthioguanine
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-
-
-
?
S-adenosyl-L-methionine + thioinosine monophosphate
S-adenosyl-L-homocysteine + methylthioinosine monophosphate
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-
-
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?
S-adenosyl-L-methionine + 6-mercaptopurine
S-adenosyl-L-homocysteine + 6-methylmercaptopurine
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-
-
?
S-adenosyl-L-methionine + 6-mercaptopurine
S-adenosyl-L-homocysteine + 6-methylmercaptopurine
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-
-
-
?
S-adenosyl-L-methionine + a thiopurine
S-adenosyl-L-homocysteine + a thiopurine S-methylether
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-
-
-
?
S-adenosyl-L-methionine + a thiopurine
S-adenosyl-L-homocysteine + a thiopurine S-methylether
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specific for S-adenosyl-L-methionine
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-
?
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S-adenosyl-L-methionine + a thiopurine
S-adenosyl-L-homocysteine + a thiopurine S-methylether
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-
-
?
S-adenosyl-L-methionine + a thiopurine
S-adenosyl-L-homocysteine + a thiopurine S-methylether
S-adenosyl-L-methionine + a thiopurine
S-adenosyl-L-homocysteine + a thiopurine S-methylether
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-
-
-
?
S-adenosyl-L-methionine + a thiopurine
S-adenosyl-L-homocysteine + a thiopurine S-methylether
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specific for S-adenosyl-L-methionine
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-
?
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2-methylthio-4-hydroxypyrimidine
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1.8 mM, 45% inhibition
5-methyl-2,4-dithiopyrimidine
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6-hydroxy-2-thiopurine
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L-cysteine
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1.8 mM, 50% inhibition
L-homocysteine thiolactone
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-
S-adenosyl-L-methionine
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-
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0.00035
6-Mercaptopurine
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0.0056
S-adenosyl-L-methionine
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Uniprot
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mouse
Uniprot
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mouse, strain C57/BL6, GenBank accession number
Uniprot
brenda
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brenda
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brenda
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primary cell
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brenda
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brenda
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brenda
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brenda
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brenda
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brenda
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brenda
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brenda
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brenda
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brenda
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malfunction
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when thiopurine methyltransferase protein activity is low a greater degree of cytotoxicity and DNA damage can occur after thioguanine exposure
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TPMT_MOUSE
240
0
27586
Swiss-Prot
other Location (Reliability: 1 )
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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
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45 - 56
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heat inactivation, 23% of the activity is lost after 20 min at 45°C, 95% activity is lost after 6 min at 56°C
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using a Ni2+-NTA resin and a gel-filtration column
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cDNA cloned and heterologous expressed in rabbit reticulocytes and wheat germ lysate
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
a 8.7 kb fragment encompassing part of exon III through a portion of intron 6 is subcloned into the pZERO-2 vector
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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
medicine
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the murine model recapitulates many clinical features of the human polymorphism and provides a preclinical system for establishing safer regimens of genetically influenced antileukemic drug therapy
medicine
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low enzyme level can lead to greater sensitivity to thiopurine therapy in astroglial cells
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Remy, C.N.
Metabolism of thiopyrimidines and thiopurines
J. Biol. Chem.
238
1078-1084
1963
Mus musculus, Rattus norvegicus, Mus musculus Swiss-Webster
brenda
Van Loon, J.A.; Weinshilboum, R.M.
Thiopurine methyltransferase isozymes in human renal tissue
Drug Metab. Dispos.
18
632-638
1990
Homo sapiens, Mus musculus
brenda
Szumlanski, C.L.; Honchel, R.; Scott, M.C.; Weinshilboum, R.M.
Human liver thiopurine methyltransferase pharmacogenetics: biochemical properties, liver-erythrocyte correlation and presence of isozymes
Pharmacogenetics
2
148-159
1992
Homo sapiens, Mus musculus
brenda
Fessing, M.Y.; Belkov, V.M.; Krynetski, E.Y.; Evans, W.E.
Molecular cloning and functional characterization of the cDNA encoding the murine thiopurine S-methyltransferase (TPMT)
FEBS Lett.
424
143-145
1998
Homo sapiens, Mus musculus (O55060), Mus musculus
brenda
Dervieux, T.; Blanco, J.G.; Krynetski, E.Y.; Vanin, E.F.; Roussel, M.F.; Relling, M.V.
Differing contribution of thiopurine methyltransferase to mercaptopurine versus thioguanine effects in human leukemic cells
Cancer Res.
61
5810-5816
2001
Homo sapiens, Mus musculus
brenda
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
Biochemistry
47
6216-6225
2008
Mus musculus (O55060), Mus musculus, Homo sapiens (P51580), Homo sapiens
brenda
Hartford, C.; Vasquez, E.; Schwab, M.; Edick, M.J.; Rehg, J.E.; Grosveld, G.; Pui, C.H.; Evans, W.E.; Relling, M.V.
Differential effects of targeted disruption of thiopurine methyltransferase on mercaptopurine and thioguanine pharmacodynamics
Cancer Res.
67
4965-4972
2007
Mus musculus
brenda
Hosni-Ahmed, A.; Barnes, J.D.; Wan, J.; Jones, T.S.
Thiopurine methyltransferase predicts the extent of cytotoxicty and DNA damage in astroglial cells after thioguanine exposure
PLoS ONE
6
e29163
2011
Homo sapiens, Mus musculus
brenda