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Literature summary extracted from

  • Oselin, K.; Anier, K.
    Inhibition of human thiopurine S-methyltransferase by various nonsteroidal anti-inflammatory drugs in vitro: a mechanism for possible drug interactions (2007), Drug Metab. Dispos., 35, 1452-1454.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.1.1.67 medicine the results suggest that coadministration of thiopurines and various nonsteriodal anti-inflammatory drugs may lead to drug interactions Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.1.1.67 celecoxib
-
 Homo sapiens
2.1.1.67 diclofenac
-
 Homo sapiens
2.1.1.67 flurbiprofen
-
 Homo sapiens
2.1.1.67 Ibuprofen
-
 Homo sapiens
2.1.1.67 Ketoprofen
-
 Homo sapiens
2.1.1.67 lornoxicam
-
 Homo sapiens
2.1.1.67 Mefenamic acid
-
 Homo sapiens
2.1.1.67 meloxicam
-
 Homo sapiens
2.1.1.67 nabumetone
-
 Homo sapiens
2.1.1.67 naproxen
-
 Homo sapiens
2.1.1.67 olsalazine
-
 Homo sapiens
2.1.1.67 paracetamol
-
 Homo sapiens
2.1.1.67 piroxicam
-
 Homo sapiens
2.1.1.67 tolfenamic acid
-
 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 erythrocyte
-
 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
-
 Homo sapiens ?
-
 ?

Synonyms

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

Temperature Optimum [°C]

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

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.1.1.67 7.4
-
 TPMT activity assay Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.1.1.67 0.039
-
 Mefenamic acid
-
 Homo sapiens
2.1.1.67 0.05
-
 tolfenamic acid
-
 Homo sapiens
2.1.1.67 0.052
-
 naproxen
-
 Homo sapiens
2.1.1.67 0.172
-
 Ketoprofen
-
 Homo sapiens
2.1.1.67 0.208
-
 olsalazine
-
 Homo sapiens
2.1.1.67 0.722
-
 diclofenac
-
 Homo sapiens
2.1.1.67 1.043
-
 Ibuprofen
-
 Homo sapiens
2.1.1.67 1.41
-
 lornoxicam
-
 Homo sapiens
2.1.1.67 1.524
-
 flurbiprofen
-
 Homo sapiens
2.1.1.67 2.413
-
 celecoxib
-
 Homo sapiens
2.1.1.67 2.589
-
 piroxicam
-
 Homo sapiens
2.1.1.67 4.238
-
 meloxicam
-
 Homo sapiens
2.1.1.67 4.3
-
 nabumetone
-
 Homo sapiens
2.1.1.67 5.162
-
 paracetamol
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.1.1.67 0.039
-
-
 Homo sapiens Mefenamic acid
2.1.1.67 0.063
-
-
 Homo sapiens tolfenamic acid
2.1.1.67 0.079
-
-
 Homo sapiens naproxen
2.1.1.67 1.013
-
-
 Homo sapiens Ketoprofen
2.1.1.67 1.474
-
-
 Homo sapiens olsalazine
2.1.1.67 1.582
-
-
 Homo sapiens diclofenac
2.1.1.67 1.649
-
-
 Homo sapiens flurbiprofen
2.1.1.67 1.968
-
-
 Homo sapiens Ibuprofen
2.1.1.67 2.135
-
-
 Homo sapiens lornoxicam
2.1.1.67 2.416
-
-
 Homo sapiens celecoxib
2.1.1.67 2.589
-
-
 Homo sapiens piroxicam
2.1.1.67 4.292
-
-
 Homo sapiens meloxicam
2.1.1.67 4.341
-
-
 Homo sapiens nabumetone
2.1.1.67 5.168
-
-
 Homo sapiens paracetamol