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Literature summary for 2.1.1.67 extracted from

  • Ujiie, S.; Sasaki, T.; Mizugaki, M.; Ishikawa, M.; Hiratsuka, M.
    Functional characterization of 23 allelic variants of thiopurine S-methyltransferase gene (TPMT*2 - *24) (2008), Pharmacogenet. Genomics, 18, 887-893.
    View publication on PubMed

Application

Application Comment Organism
medicine thiopurine S-methyltransferase is an enzyme responsible for the detoxification of the widely used thiopurine drugs Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
into the pCR2.1-TOPO vector, used as a template to generate point mutations, the variants are sequenced and cloned into the mammalian expression vector pCMV6-XL5, into the pENTR/D-TOPO vector and subsequently into the pcDNA-DEST40 vector Homo sapiens

Protein Variants

Protein Variants Comment Organism
A154T variant TPMT*3B Homo sapiens
A154T/Y240C variant TPMT*3A Homo sapiens
A167G variant TPMT*23 Homo sapiens
A80P variant TPMT*2 Homo sapiens
C132Y variant TPMT*11 Homo sapiens
E28V variant TPMT*13 Homo sapiens
G144R variant TPMT*10 Homo sapiens
G36S variant TPMT*24 Homo sapiens
G71R variant TPMT*18 Homo sapiens
H227Q variant TPMT*7 Homo sapiens
K119T variant TPMT*9 Homo sapiens
K122T variant TPMT*19 Homo sapiens
K238E variant TPMT*20 Homo sapiens
L49S variant TPMT*5 Homo sapiens
L69V variant TPMT*21 Homo sapiens
M1V variant TPMT*14 Homo sapiens
Q42E variant TPMT*17 Homo sapiens
R163H variant TPMT*16 Homo sapiens
R163P variant TPMT*22 Homo sapiens
R215H variant TPMT*8 Homo sapiens
S125L variant TPMT*12 Homo sapiens
Y180F variant TPMT*6 Homo sapiens
Y240C variant TPMT*3C Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.056
-
6-thioguanine mutant R215H, variant TPMT*8 Homo sapiens
0.076
-
6-thioguanine mutant K119T, variant TPMT*9 Homo sapiens
0.08
-
6-thioguanine wild-type, variant TPMT*1 Homo sapiens
0.098
-
6-thioguanine mutant A167G, variant TPMT*23 Homo sapiens
0.125
-
6-thioguanine mutant G144R, variant TPMT*10 Homo sapiens
0.127
-
6-thioguanine mutant S125L, variant TPMT*12 Homo sapiens
0.151
-
6-thioguanine mutant A80P, variant TPMT*2 Homo sapiens
0.156
-
6-thioguanine mutant Y240C, variant TPMT*3C Homo sapiens
0.186
-
6-thioguanine mutant K122T, variant TPMT*19 Homo sapiens
0.353
-
6-thioguanine mutant K238E, variant TPMT*20 Homo sapiens
0.485
-
6-thioguanine mutant Y180F, variant TPMT*6 Homo sapiens
0.55
-
6-thioguanine mutant E28V, variant TPMT*13 Homo sapiens
0.6
-
6-thioguanine mutant R163H, variant TPMT*16 Homo sapiens
1.027
-
6-thioguanine mutant H227Q, variant TPMT*7 Homo sapiens
1.094
-
6-thioguanine mutant G36S, variant TPMT*24 Homo sapiens
1.267
-
6-thioguanine mutant Q42E, variant TPMT*17 Homo sapiens
1.45
-
6-thioguanine mutant C132Y, variant TPMT*11 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
-
-
-

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

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
-
enzyme assay of thiopurine S-methyltransferase activity in COS-7 cells Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
enzyme assay of thiopurine S-methyltransferase activity in COS-7 cells Homo sapiens