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Literature summary for 2.1.1.67 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

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

Inhibitors

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

Synonyms

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

Temperature Optimum [°C]

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

pH Optimum

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

Ki Value [mM]

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

IC50 Value

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