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Literature summary for 2.1.1.67 extracted from

  • Karas-Kuzelicki, N.; Mlinaric-Rascan, I.
    Individualization of thiopurine therapy: thiopurine S-methyltransferase and beyond (2009), Pharmacogenomics, 10, 1309-1322.
    View publication on PubMed

Application

Application Comment Organism
medicine TPMT activity is a good prediction factor for the toxicity and efficacy of the antileukemic thiopurine therapy Homo sapiens

Protein Variants

Protein Variants Comment Organism
A154T mutant shows decreased TPMT activity Homo sapiens
A154T/Y240C mutant shows decreased TPMT activity Homo sapiens
A167G mutant shows decreased TPMT activity Homo sapiens
A80P mutant shows decreased TPMT activity Homo sapiens
C132Y mutant shows decreased TPMT activity Homo sapiens
C212R mutant shows decreased TPMT activity Homo sapiens
E28V mutant shows decreased TPMT activity Homo sapiens
G144R mutant shows decreased TPMT activity Homo sapiens
G36S mutant shows decreased TPMT activity Homo sapiens
G71R mutant shows decreased TPMT activity Homo sapiens
H227Q mutant shows decreased TPMT activity Homo sapiens
K119T mutant shows decreased TPMT activity Homo sapiens
K122T mutant shows normal TPMT activity Homo sapiens
K238E mutant shows decreased TPMT activity Homo sapiens
L49S mutant shows decreased TPMT activity Homo sapiens
L69V mutant shows decreased TPMT activity Homo sapiens
Q42E mutant shows decreased TPMT activity Homo sapiens
R163H mutant shows decreased TPMT activity Homo sapiens
R163P mutant shows decreased TPMT activity Homo sapiens
R215H mutant shows decreased TPMT activity Homo sapiens
S125L mutant shows decreased TPMT activity Homo sapiens
Y180F mutant shows decreased TPMT activity Homo sapiens
Y240C mutant shows decreased TPMT activity Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
additional information low levels of methionine can result in low S-adenosyl-L-methionine levels and consequently decreased TPMT activity Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens S-adenosyl-L-methionine and sinefungin prevent degradation of TPMT by stabilizing ist native structure ?
-
?

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.
additional information S-adenosyl-L-methionine and sinefungin prevent degradation of TPMT by stabilizing ist native structure Homo sapiens ?
-
?
S-adenosyl-L-methionine + 6-mercaptopurine TPMT deactivates 6-mercaptopurine by methylation Homo sapiens S-adenosyl-L-homocysteine + 6-methylmercaptopurine
-
?

Synonyms

Synonyms Comment Organism
TPMT
-
Homo sapiens

Expression

Organism Comment Expression
Homo sapiens S-adenosyl-L-methionine has no effect on TPMT mRNA expression additional information
Homo sapiens smokers have significantly higher TPMT activity than nonsmokers up