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Literature summary extracted from

  • Dilger, K.; Schaeffeler, E.; Lukas, M.; Strauch, U.; Herfarth, H.; Mueller, R.; Schwab, M.
    Monitoring of thiopurine methyltransferase activity in postsurgical patients with Crohns disease during 1 year of treatment with azathioprine or mesalazine (2007), Ther. Drug Monit., 29, 1-5.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.1.1.67 medicine evaluation of a possible long-term effect of mesalazine or azathioprine on thiopurine methyltransferase activity is of particular clinical importance because both drugs can to be given for several years in inflammatory bowel disease Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
2.1.1.67 TPMT*2 polymorphism, single nucleotide substitution G238C Homo sapiens
2.1.1.67 TPMT*3A polymorphism, single nucleotide substitutions G460A and A719G Homo sapiens
2.1.1.67 TPMT*3B polymorphism, single nucleotide substitution G460A Homo sapiens
2.1.1.67 TPMT*3C polymorphism, single nucleotide substitution A719G Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.1.1.67 mesalazine
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.1.1.67 S-adenosyl-L-methionine + a thiopurine Homo sapiens
-
 S-adenosyl-L-homocysteine + a thiopurine S-methylether
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.1.1.67 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.1.1.67 blood
-
 Homo sapiens
-
2.1.1.67 erythrocyte
-
 Homo sapiens
-

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
2.1.1.67 additional information
-
 thiopurine methyltransferase levels above 23 nmol 6-methylthioguanine/g Hb per h indicates normal enzyme activity Homo sapiens

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-thioguanine
-
 Homo sapiens S-adenosyl-L-homocysteine + 6-methylthioguanine
-
 ?
2.1.1.67 S-adenosyl-L-methionine + a thiopurine
-
 Homo sapiens S-adenosyl-L-homocysteine + a thiopurine S-methylether
-
 ?
2.1.1.67 S-adenosyl-L-methionine + azathioprine azathioprine is converted via a non-enzymatic reaction to mercaptopurine, which is subsequently metabolized through TPMT Homo sapiens S-adenosyl-L-homocysteine + 6-methylmercaptopurine + ?
-
 ?

Synonyms

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