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Literature summary for 2.1.1.67 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
Search for more literature for 2.1.1.67

Application

Application Comment Organism
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

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

Inhibitors

Inhibitors Comment Organism Structure
mesalazine
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
blood
-
 Homo sapiens
-
erythrocyte
-
 Homo sapiens
-

Specific Activity [micromol/min/mg]

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

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-thioguanine
-
 Homo sapiens S-adenosyl-L-homocysteine + 6-methylthioguanine
-
 ?
S-adenosyl-L-methionine + a thiopurine
-
 Homo sapiens S-adenosyl-L-homocysteine + a thiopurine S-methylether
-
 ?
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

Synonyms Comment Organism
thiopurine methyltransferase
-
 Homo sapiens
TPMT
-
 Homo sapiens