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Information on EC 2.1.1.67 - thiopurine S-methyltransferase and Organism(s) Homo sapiens

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EC Tree
     2 Transferases
         2.1 Transferring one-carbon groups
             2.1.1 Methyltransferases
                2.1.1.67 thiopurine S-methyltransferase
IUBMB Comments
Also acts, more slowly, on thiopyrimidines and aromatic thiols. Not identical with EC 2.1.1.9 thiol S-methyltransferase.
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Select one or more organisms in this record: ?
This record set is specific for:
Homo sapiens
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Word Map
The taxonomic range for the selected organisms is: Homo sapiens
The expected taxonomic range for this enzyme is: Bacteria, Eukaryota, Archaea
Synonyms
thiopurine methyltransferase, thiopurine s-methyltransferase, thiopurine methyl transferase, 6-thiopurine s-methyltransferase, thiopurine-s-methyl-transferase, s-adenosyl-l-methionine:thiopurine s-methyltransferase, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
6-thiopurine S-methyltransferase
-
-
6-thiopurine transmethylase
-
-
-
-
mercaptopurine methyltransferase
-
-
-
-
thiopurine methyl transferase
-
-
thiopurine methyltransferase
thiopurine S-methyltransferase
thiopurine-S-methyl-transferase
-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
methyl group transfer
PATHWAY SOURCE
PATHWAYS
SYSTEMATIC NAME
IUBMB Comments
S-adenosyl-L-methionine:thiopurine S-methyltransferase
Also acts, more slowly, on thiopyrimidines and aromatic thiols. Not identical with EC 2.1.1.9 thiol S-methyltransferase.
CAS REGISTRY NUMBER
COMMENTARY hide
67339-09-7
-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
S-(5'-adenosyl)-L-methionine-d3 disulfate salt + 6-mercaptopurine
S-adenosyl-L-homocysteine + 6-(d3-methyl)mercaptopurine
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 2-aminothiophenol
S-adenosyl-L-homocysteine + 2-methylsulfanylphenylamine
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 2-bromothiophenol
S-adenosyl-L-homocysteine + 1-bromo-2-methylsulfanylbenzene
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 2-mercaptoethanol
S-adenosyl-L-homocysteine + 2-methylmercaptoethanol
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 2-methoxythiophenol
S-adenosyl-L-homocysteine + 1-methoxy-2-methylsulfanylbenzene
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 2-thiouracil
S-adenosyl-L-homocysteine + thiouracil-2-S-methylether
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 3-methoxythiophenol
S-adenosyl-L-homocysteine + 1-methylsulfanyl-3-methoxybenzene
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 4-(aminomethoxy)thiophenol
S-adenosyl-L-homocysteine + 1-aminomethoxy-4-methylsulfanylbenzene
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 4-bromothiophenol
S-adenosyl-L-homocysteine + 1-bromo-4-methylsulfanylbenzene
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 4-chlorothiophenol
S-adenosyl-L-homocysteine + 1-chloro-4-methylsulfanylbenzene
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 4-fluorothiophenol
S-adenosyl-L-homocysteine + 1-fluoro-4-methylsulfanylbenzene
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 4-methoxythiophenol
S-adenosyl-L-homocysteine + 1-methoxy-4-methylsulfanylbenzene
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 4-methylthiophenol
S-adenosyl-L-homocysteine + 1-methyl-4-methylsulfanylbenzene
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 4-nitrothiophenol
S-adenosyl-L-homocysteine + 1-methylsulfanyl-4-nitrobenzene
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 4-thiobenzoate
S-adenosyl-L-homocysteine + 4-methylsulfanyl benzoate
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 6-hydroxy-8-mercaptopurine
S-adenosyl-L-homocysteine + 6-hydroxy-8-methylmercaptopurine
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 6-mercaptopurine
?
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 6-mercaptopurine
S-adenosyl-L-homocysteine + 6-methylmercaptopurine
show the reaction diagram
S-adenosyl-L-methionine + 6-mercaptopurine nucleoside
S-adenosyl-L-homocysteine + 6-methylmercaptopurine nucleoside
show the reaction diagram
-
inactivation
-
-
?
S-adenosyl-L-methionine + 6-mercaptopurine-riboside
S-adenosyl-L-homocysteine + 6-methylmercaptopurine-riboside
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 6-mercaptopurine-riboside-5'-monophosphate
S-adenosyl-L-homocysteine + 6-methylmercaptopurine-riboside-5'-monophosphate
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 6-mercaptopurine-riboside-5'-triphosphate
S-adenosyl-L-homocysteine + 6-methylmercaptopurine-riboside-5'-triphosphate
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 6-selenoguanine-riboside
S-adenosyl-L-homocysteine + 6-methylselenoguanine-riboside
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 6-selenopurine
S-adenosyl-L-homocysteine + 6-methylselenopurine
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 6-selenopurine-riboside
S-adenosyl-L-homocysteine + 6-methylselenopurine-riboside
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 6-thiodeoxyguanosine
S-adenosyl-L-homocysteine + 6-thiodeoxyguanosine S-methylether
show the reaction diagram
-
-
-
-
r
S-adenosyl-L-methionine + 6-thiodeoxyguanosine monophosphate
S-adenosyl-L-homocysteine + 6-methylthiodeoxyguanosine monophosphate
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 6-thiodeoxyinosine
S-adenosyl-L-homocysteine + 6-thiodeoxyinosine S-methylether
show the reaction diagram
-
-
-
-
r
S-adenosyl-L-methionine + 6-thiodeoxyinosine monophosphate
S-adenosyl-L-homocysteine + 6-methyl thiodeoxyinosine monophosphate
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 6-thioguanine
?
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 6-thioguanine
S-adenosyl-L-homocysteine + 6-methylthioguanine
show the reaction diagram
S-adenosyl-L-methionine + 6-thioguanine monophosphate
S-adenosyl-L-homocysteine + 6-methylthioguanine monophosphate
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 6-thioguanine-riboside
S-adenosyl-L-homocysteine + 6-methylthioguanine-riboside
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 6-thioguanine-riboside-5'-monophosphate
S-adenosyl-L-homocysteine + 6-methylthioguanine-riboside-5'-monophosphate
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 6-thioguanosine monophosphate
S-adenosyl-L-homocysteine + 6-methyl thioguanosine monophosphate
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 6-thioinosine
S-adenosyl-L-homocysteine + 6-methylmercaptopurine riboside
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 6-thioinosine 5'-monophosphate
S-adenosyl-L-homocysteine + 6-methylmercaptopurine ribonucleotide
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 6-thioinosine diphosphate
S-adenosyl-L-homocysteine + 6-methylthioinosine diphosphate
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 6-thioinosine monophosphate
S-adenosyl-L-homocysteine + 6-methyl thioinosine monophosphate
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 6-thioinosine monophosphate
S-adenosyl-L-homocysteine + 6-methylthioinosine monophosphate
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 6-thioinosine triphosphate
S-adenosyl-L-homocysteine + 6-methylthioinosine triphosphate
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 6-thioinosine-monophosphate
S-adenosyl-L-homocysteine + 6-methylmercaptopurine-ribonucleotide
show the reaction diagram
-
-
consisting of 6-methyl-thioinosine-monophosphate, -diphosphate and triphosphate
-
?
S-adenosyl-L-methionine + 6-thiopurine
S-adenosyl-L-homocysteine + 6-methylthiopurine
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 7-methyl-6-mercaptopurine
S-adenosyl-L-homocysteine + ?
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 8-hydroxy-6-mercaptopurine
S-adenosyl-L-homocysteine + 8-hydroxy-6-methylmercaptopurine
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 9(n-propyl)6-thioguanine
S-adenosyl-L-homocysteine + 9(n-propyl)6-methylthioguanine
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 9-(n-butyl)-6-mercaptopurine
S-adenosyl-L-homocysteine + 9-(n-butyl)-6-methylmercaptopurine
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 9-ethyl-6-mercaptopurine
S-adenosyl-L-homocysteine + 9-ethyl-6-methylmercaptopurine
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + a thiopurine
S-adenosyl-L-homocysteine + a thiopurine S-methylether
show the reaction diagram
S-adenosyl-L-methionine + azathioprine
?
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + azathioprine
S-adenosyl-L-homocysteine + 6-methylmercaptopurine + ?
show the reaction diagram
S-adenosyl-L-methionine + azathioprine
S-adenosyl-L-homocysteine + ?
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + mercaptopurine
S-adenosyl-L-homocysteine + methylmercaptopurine
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + thioguanine nucleotide
S-adenosyl-L-homocysteine + methylthioguanine
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + thioinosine monophosphate
S-adenosyl-L-homocysteine + methylthioinosine monophosphate
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + thioinosine triphosphate
S-adenosyl-L-homocysteine + methylthioinosine triphosphate
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + thiopurine
S-adenosyl-L-homocysteine + methylthiopurine
show the reaction diagram
-
-
-
-
?
additional information
?
-
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
S-adenosyl-L-methionine + 6-mercaptopurine
S-adenosyl-L-homocysteine + 6-methylmercaptopurine
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + 6-thiopurine
S-adenosyl-L-homocysteine + 6-methylthiopurine
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + a thiopurine
S-adenosyl-L-homocysteine + a thiopurine S-methylether
show the reaction diagram
additional information
?
-
-
S-adenosyl-L-methionine and sinefungin prevent degradation of TPMT by stabilizing ist native structure
-
-
?
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Mg2+
-
baseline activity 102%
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
2,8-dihydroxy-6-mercaptopurine
-
-
2-Hydroxy-6-mercaptopurine
-
-
3,4,5-triiodobenzoic acid
-
-
3,4-dimethoxy-5-hydroxybenzoic acid
-
-
3,4-dimethoxybenzoic acid
-
-
3,5-dichlorobenzoic acid
-
-
3,5-dihydroxy-4-methoxybenzoic acid
-
-
3,5-dimethylbenzoic acid
-
-
3,5-dinitrobenzoic acid
-
-
3-bromo-5-hydroxy-4-methoxybenzoic acid
-
-
3-chloro-5-hydroxy-4-methoxybenzoic acid
-
-
3-hydroxy-4,5-dimethoxybenzoic acid
-
-
3-hydroxy-4-methoxy-5-(dimethylamino)benzoic acid
-
-
3-hydroxy-4-methoxy-5-nitrobenzoic acid
-
-
3-hydroxy-4-methoxybenzoic acid
-
-
3-hydroxy-5-iodo-4-methoxybenzoic acid
-
-
4-hydroxy-3-methoxybenzoic acid
-
-
5-amino-salicylic acid
-
-
5-Aminosalicylate
-
-
6-Mercaptopurine
6-methylmercaptopurine
-
-
6-thioguanine
-
mixed inhibitor of 6-mercaptopurine methylation
Azathioprine
-
IC50: 0.43-0.532 mM
bendroflumethiazide
-
-
benzoic acid
celecoxib
-
-
diclofenac
-
-
Ethacrynic acid
-
-
flurbiprofen
-
-
Furosemide
Ibuprofen
-
-
Ketoprofen
-
-
lornoxicam
-
-
Mefenamic acid
-
-
meloxicam
-
-
mesalazine
-
-
N-ethylmaleimide
-
-
nabumetone
-
-
naproxen
-
-
olsalazine
-
-
paracetamol
-
-
piretanide
-
IC50: 0.3-0.313 mM
piroxicam
-
-
S-adenosyl-L-homocysteine
-
-
sulfasalazine
-
-
sulphasalazine
-
-
testosterone
-
IC50: 0.03-0.072 mM
tolfenamic acid
-
-
trichlormethiazide
-
-
tropolone
-
-
additional information
-
low levels of methionine can result in low S-adenosyl-L-methionine levels and consequently decreased TPMT activity
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
S-adenosyl-L-methionine
-
S-adenosyl-L-methionine acts as a positive modulator of TPMT activity, the effect of S-adenosyl-L-methionine appears to be restricted to protein stabilisation rather than an increase of TPMT expression
SKF-525A
-
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
168
2-mercaptoethanol
-
-
2
2-Thiouracil
-
-
0.138
6-hydroxy-8-mercaptopurine
-
-
0.00068 - 0.99
6-Mercaptopurine
1.17
6-mercaptopurine-riboside
-
-
1.27
6-mercaptopurine-riboside-5'-monophosphate
-
-
0.89
6-mercaptopurine-riboside-5'-triphosphate
-
-
0.139
6-selenoguanine-riboside
-
-
0.0291
6-selenopurine
-
-
0.0518
6-selenopurine-riboside
-
-
0.1314
6-thiodeoxyguanosine
-
recombinant enzyme, expressed in yeast
0.0127
6-thiodeoxyinosine
-
recombinant enzyme, expressed in yeast
0.0137 - 1.45
6-thioguanine
0.761
6-thioguanine-riboside
-
-
1.04
6-thioguanine-riboside-5'-monophosphate
-
-
0.0261
6-thioguanosine
-
recombinant enzyme, expressed in yeast
0.0271
6-thioguanosine 5-monophosphate
-
recombinant enzyme, expressed in yeast
0.0551
6-thioinosine
-
recombinant enzyme, expressed in yeast
0.0257
6-thioinosine 5'-monophosphate
-
recombinant enzyme, expressed in yeast
0.231
7-methyl-6-mercaptourine
-
-
0.0961
8-hydroxy-6-mercaptopurine
-
-
0.292
9-(n-butyl)6-mercaptopurine
-
-
0.159
9-(n-propyl)-6-thioguanine
-
-
0.372
9-ethyl-6-mercaptopurine
-
-
0.0024 - 0.0463
S-adenosyl-L-methionine
additional information
additional information
-
various thiophenols as substrates, Km 0.0008-0.0078
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.027
2-Hydroxy-6-mercaptopurine
-
-
0.01 - 0.0113
3,4-dimethoxy-5-hydroxybenzoic acid
0.00802 - 0.0113
6-Mercaptopurine
0.45 - 0.9
6-thioguanine
2.413
celecoxib
-
-
0.722
diclofenac
-
-
1.524
flurbiprofen
-
-
1.043
Ibuprofen
-
-
0.172
Ketoprofen
-
-
1.41
lornoxicam
-
-
0.039
Mefenamic acid
-
-
4.238
meloxicam
-
-
4.3
nabumetone
-
-
0.052
naproxen
-
-
0.208
olsalazine
-
-
5.162
paracetamol
-
-
2.589
piroxicam
-
-
0.00075
S-adenosyl-L-homocysteine
-
-
0.05
tolfenamic acid
-
-
0.85
tropolone
-
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.43 - 0.532
Azathioprine
Homo sapiens
-
IC50: 0.43-0.532 mM
2.416
celecoxib
Homo sapiens
-
-
1.582
diclofenac
Homo sapiens
-
-
1.649
flurbiprofen
Homo sapiens
-
-
0.015 - 0.019
Furosemide
Homo sapiens
-
IC50: 0.015-0.019 mM, has the potential to inhibit thiopurine S-methyltransferase in patients with chronic inflammatory bowel disease
1.968
Ibuprofen
Homo sapiens
-
-
1.013
Ketoprofen
Homo sapiens
-
-
2.135
lornoxicam
Homo sapiens
-
-
0.039
Mefenamic acid
Homo sapiens
-
-
4.292
meloxicam
Homo sapiens
-
-
4.341
nabumetone
Homo sapiens
-
-
0.079
naproxen
Homo sapiens
-
-
1.474
olsalazine
Homo sapiens
-
-
5.168
paracetamol
Homo sapiens
-
-
0.3 - 0.313
piretanide
Homo sapiens
-
IC50: 0.3-0.313 mM
2.589
piroxicam
Homo sapiens
-
-
0.03 - 0.072
testosterone
Homo sapiens
-
IC50: 0.03-0.072 mM
0.063
tolfenamic acid
Homo sapiens
-
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
0.00000716
-
TMPT reference activity after recovery of the bone marrow suppression
0.00003033
-
elevated TPMT activity during the recovery phase of a bone marrow suppression, following the pancytopenic period
1.03
-
-
additional information
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.5
-
TPMT activity assay
pH RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
3.5 - 8.6
-
-
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
embryonic kidney cell line with inducible thiopurine methyltransferase
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
TPMT_HUMAN
245
0
28180
Swiss-Prot
other Location (Reliability: 1)
Q6I929_HUMAN
246
0
28398
TrEMBL
other Location (Reliability: 1)
A0A024QZW0_HUMAN
245
0
28180
TrEMBL
other Location (Reliability: 1)
Q9BS45_HUMAN
245
0
28233
TrEMBL
other Location (Reliability: 1)
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
30000
-
2 isozymes, gel filtration
33000
determined by SDS-PAGE and immunoblotting
35000
-
x * 35000, SDS-PAGE
36000
-
gel filtration
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
?
-
x * 35000, SDS-PAGE
monomer
-
-
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
238G>C
460G>A
460G>A/719A>G
-
TPMT*3A polymorphism, low or no TPMT activity
539A>T
-
TPMT variant
719A>G
A154T
A154T/Y240C
A154Y
-
thiopurine S-methyltransferase polymorphism, G to A transition at position 460
A167G
A179G/G460A
the variant is associated with low enzyme activity
A180P
-
the mutation affects TMPT activity
A719G
C132Y
C212R
C216T
the mutant exhibits reduced activity compared to the wild type enzyme
E98X
-
the mutation affects TMPT activity
F208L
-
the mutation is associated with a decrease in enzyme activity
G144R
G238C
G460A
H227Q
K119T
K122T
K238E
Q179H
polymorphism c.537G>T, TPMT*24
R152A
mutant to probe, whether this residue is important for catalysis
R152A/R226A
mutant to probe, whether this residue is important for catalysis
R152E
mutant to probe, whether this residue is important for catalysis
R152H
mutant to probe, whether this residue is important for catalysis
R163H
R163P
R215H
R226A
mutant to probe, whether this residue is important for catalysis
R226E
mutant to probe, whether this residue is important for catalysis
R226H
mutant to probe, whether this residue is important for catalysis
S125L
TPMT*2
TPMT*23
-
polymorphism, single nucleotide substitution, C500G
TPMT*3A
TPMT*3B
TPMT*3C
Y107D
the mutant shows less than 10% activity compared to the wild type enzyme, the variant allozyme shows a striking decrease in both immunoreactive protein level and enzyme activity after transient expression in COS-1 cells, the mutant is less stable than the wild type TPMT allozyme
Y180F
Y240C
additional information
TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
46.4
melting temperature of the wild type enzyme without ligand
46.8
melting temperature of the wild type enzyme in complex with S-adenosyl-L-methionine
55
-
the melting temperature of the wild type enzyme is at 55°C
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
S-adenosyl-L-methionine is responsible for direct stabilization of the enzyme
-
STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
80°C, activity in cell lysate is stable during storage
-
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
2 isozymes
-
cytosolic fractions of transformed Saccharomyces cerevisiae cells are prepared
Ni-NTA column chromatography and Superdex 200 gel filtration
Ni-NTA column chromatography and Superdex S200 gel filtration
partially
-
using a Ni2+-NTA resin and a gel-filtration column
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
baculovirus expressed
-
cDNA cloning, heterologous expression in yeast
-
enhanced green fluorescent protein-tagged enzyme is expressed in Escherichia coli, Jurkat, Hep-G2, and HEK-293 cells
-
expressed in COS-1 cells
expressed in Escherichia coli BL21-Codon Plus (DE3)-RIL cells
expressed in Escherichia coli BL21-CodonPlus (DE3)-RIL cells
for cloning of the TPMT fragment the TOPO TA cloning kit is used
-
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
-
into the yeast expression vector pYeDP60 for transformation of Saccharomyces cerevisiae cells
retroviral gene transfer
-
the full-length coding region is amplified by PCR from a eukaryotic expression plasmid and cloned into the pET-28a vector for expression in Escherichia coli BL21DE3 cells
to assess the functional effect of the trinucleotide repeat variants in the promoter, the wild-type and variant TPMT promoters are amplified and cloned into the promoter-less pGL3-Basic vector
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
azathioprine therapy can raise TPMT activity
-
decreased activity of TPMT is associated with hematopoietic toxicity after administration of standard doses of 6- mercaptopurine or azathioprine
-
longitudinal induction of thiopurine methyltransferase activity is observed during 6-thioguanine treatment
-
S-adenosyl-L-methionine has no effect on TPMT mRNA expression
-
smokers have significantly higher TPMT activity than nonsmokers
-
the restriction of L-methionine in cell growth media reversibly decreases enzyme activity and protein levels
-
TPMT activity is significantly higher in wild type children than in wild type adults (18-68 years), wild type infants from 0.08-5 years has a 9% higher average TPMT activity than the other wild type groups, only in children from 0.08-2 years is the TPMT activity higher in males than in females
-
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
analysis
diagnostics
medicine
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Woodson, L.C.; Weinshilboum, R.M.
Human kidney thiopurine methyltransferase. Purification and biochemical properties
Biochem. Pharmacol.
32
819-826
1983
Homo sapiens
Manually annotated by BRENDA team
Ames, M.M.; Selassie, C.D.; Woodson, L.C.; Van Loon, J.A.; Hansch, C.; Weinshilboum, R.M.
Thiopurine methyltransferase: structure-activity relationships for benzoic acid inhibitors and thiophenol substrates
J. Med. Chem.
29
354-358
1986
Homo sapiens
Manually annotated by BRENDA team
Van Loon, J.A.; Weinshilboum, R.M.
Thiopurine methyltransferase isozymes in human renal tissue
Drug Metab. Dispos.
18
632-638
1990
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Szumlanski, C.L.; Honchel, R.; Scott, M.C.; Weinshilboum, R.M.
Human liver thiopurine methyltransferase pharmacogenetics: biochemical properties, liver-erythrocyte correlation and presence of isozymes
Pharmacogenetics
2
148-159
1992
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Deininger, M.; Szumlanski, C.L.; Otterness, D.M.; Van Loon, J.; Ferber, W.; Weinshilboum, R.M.
Purine substrates for human thiopurine methyltransferase
Biochem. Pharmacol.
48
2135-2138
1994
Homo sapiens
Manually annotated by BRENDA team
Krynetski, E.Y.; Krynetskaia, N.F.; Yanishevski, Y.; Evans, W.E.
Methylation of mercaptopurine, thioguanine, and their nucleotide metabolites by heterologously expressed human thiopurine S-methyltransferase
Mol. Pharmacol.
47
1141-1147
1995
Homo sapiens
Manually annotated by BRENDA team
Krynetski, E.Y.; Schuetz, J.D.; Galpin, A.J.; Pui, C.H.; Relling, M.V.; Evans, W.E.
A single point mutation leading to loss of catalytic activity in human thiopurine S-methyltransferase
Proc. Natl. Acad. Sci. USA
92
949-953
1995
Homo sapiens
Manually annotated by BRENDA team
Lysaa, R.A.; Giverhaug, T.; Wold, H.L.; Aarbakke, J.
Inhibition of human thiopurine methyltransferase by furosemide, bendroflumethiazide and trichlormethiazide
Eur. J. Clin. Pharmacol.
49
393-396
1996
Homo sapiens
Manually annotated by BRENDA team
Stupans, I.; Kirlich, A.; McKinnon, R.A.
Human thiopurine methyltransferase: no evidence of activation by its substrates
Life Sci.
62
343-350
1997
Homo sapiens
Manually annotated by BRENDA team
Fessing, M.Y.; Belkov, V.M.; Krynetski, E.Y.; Evans, W.E.
Molecular cloning and functional characterization of the cDNA encoding the murine thiopurine S-methyltransferase (TPMT)
FEBS Lett.
424
143-145
1998
Homo sapiens, Mus musculus (O55060), Mus musculus
Manually annotated by BRENDA team
Kroeplin, T.; Iven, H.
Methylation of 6-mercaptopurine and 6-thioguanine by thiopurine S-methyltransferase. A comparison of activity in red blood cell samples of 199 blood donors
Eur. J. Clin. Pharmacol.
56
343-345
2000
Homo sapiens
Manually annotated by BRENDA team
Dervieux, T.; Blanco, J.G.; Krynetski, E.Y.; Vanin, E.F.; Roussel, M.F.; Relling, M.V.
Differing contribution of thiopurine methyltransferase to mercaptopurine versus thioguanine effects in human leukemic cells
Cancer Res.
61
5810-5816
2001
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Weinshilboum, R.
Thiopurine pharmacogenetics: Clinical and molecular studies of thiopurine methyltransferase
Drug Metab. Dispos.
29
601-605
2001
Homo sapiens
Manually annotated by BRENDA team
Keizer-Garritsen, J.J.; Brouwer, C.; Lambooy, L.H.; Ter Riet, P.; Bokkerink, J.P.; Trijbels, F.J.; De Abreu, R.A.
Measurement of thiopurine S-methyltransferase activity in human blood samples based on high-performance liquid chromatography: reference values in erythrocytes from children
Ann. Clin. Biochem.
40
86-93
2003
Homo sapiens
Manually annotated by BRENDA team
Hamdan-Khalil, R.; Allorge, D.; Lo-Guidice, J.M.; Cauffiez, C.; Chevalier, D.; Spire, C.; Houdret, N.; Libersa, C.; Lhermitte, M.; Colombel, J.F.; Gala, J.L.; Broly, F.
In vitro characterization of four novel non-functional variants of the thiopurine S-methyltransferase
Biochem. Biophys. Res. Commun.
309
1005-1010
2003
Homo sapiens
Manually annotated by BRENDA team
Hamdan-Khalil, R.; Gala, J.L.; Allorge, D.; Lo-Guidice, J.M.; Horsmans, Y.; Houdret, N.; Broly, F.
Identification and functional analysis of two rare allelic variants of the thiopurine S-methyltransferase gene, TPMT*16 and TPMT*19
Biochem. Pharmacol.
69
525-529
2005
Homo sapiens (P51580), Homo sapiens
Manually annotated by BRENDA team
Brouwer, C.; de Abreu, R.A.; Keizer-Garritsen, J.J.; Lambooy, L.H.; Ament, K.; ter Riet, P.G.; van Wering, E.R.; Trijbels, F.J.; Veerman, A.J.; Hoogerbrugge, P.M.; Bokkerink, J.P.
Thiopurine methyltransferase in acute lymphoblastic leukaemia: biochemical and molecular biological aspects
Eur. J. Cancer
41
613-623
2005
Homo sapiens
Manually annotated by BRENDA team
Xin, H.W.; Fischer, C.; Schwab, M.; Klotz, U.
Thiopurine S-methyltransferase as a target for drug interactions
Eur. J. Clin. Pharmacol.
61
395-398
2005
Homo sapiens
Manually annotated by BRENDA team
Ford, L.T.; Berg, J.D.
Determination of thiopurine S-methyltransferase activity in erythrocytes using 6-thioguanine as substrate and a non-extraction liquid chromatographic technique
J. Chromatogr. B
798
111-115
2003
Homo sapiens
Manually annotated by BRENDA team
Winter, J.W.; Gaffney, D.; Shapiro, D.; Spooner, R.J.; Marinaki, A.M.; Sanderson, J.D.; Mills, P.R.
Assessment of thiopurine methyltransferase enzyme activity is superior to genotype in predicting myelosuppression following azathioprine therapy in patients with inflammatory bowel disease
Aliment. Pharmacol. Ther.
25
1069-1077
2007
Homo sapiens
Manually annotated by BRENDA team
Winter, J.W.; Marinaki, A.M.; Sanderson, J.D.; Mills, P.R.
TPMT genotype and the response to azathioprine in inflammatory bowel disease: authors reply to comments
Aliment. Pharmacol. Ther.
26
1084-1085
2007
Homo sapiens
Manually annotated by BRENDA team
Palmieri, O.; Latiano, A.; Bossa, F.; Vecchi, M.; DInca, R.; Guagnozzi, D.; Tonelli, F.; Cucchiara, S.; Valvano, M.R.; Latiano, T.; Andriulli, A.; Annese, V.
Sequential evaluation of thiopurine methyltransferase, inosine triphosphate pyrophosphatase, and HPRT1 genes polymorphisms to explain thiopurines toxicity and efficacy
Aliment. Pharmacol. Ther.
26
737-745
2007
Homo sapiens
Manually annotated by BRENDA team
Roblin, X.; Biroulet, L.P.; Phelip, J.M.; Nancey, S.; Flourie, B.
A 6-Thioguanine Nucleotide Threshold Level of 400 pmol/8 x 10(8) Erythrocytes Predicts Azathioprine Refractoriness in Patients With Inflammatory Bowel Disease and Normal TPMT Activity
Am. J. Gastroenterol.
102
1-8
2007
Homo sapiens
Manually annotated by BRENDA team
Tumer, T.B.; Ulusoy, G.; Adali, O.; Sahin, G.; Gozdasoglu, S.; Arinc, E.
The low frequency of defective TPMT alleles in Turkish population: a study on pediatric patients with acute lymphoblastic leukemia
Am. J. Hematol.
82
906-910
2007
Homo sapiens
Manually annotated by BRENDA team
Yenson, P.R.; Forrest, D.; Schmiegelow, K.; Dalal, B.I.
Azathioprine-associated acute myeloid leukemia in a patient with Crohns disease and thiopurine S-methyltransferase deficiency
Am. J. Hematol.
83
80-83
2008
Homo sapiens
Manually annotated by BRENDA team
Litos, I.K.; Emmanouilidou, E.; Glynou, K.M.; Laios, E.; Ioannou, P.C.; Christopoulos, T.K.; Kampa, M.; Castanas, E.; Gravanis, A.
Rapid genotyping of CYP2D6, CYP2C19 and TPMT polymorphisms by primer extension reaction in a dipstick format
Anal. Bioanal. Chem.
389
1849-1857
2007
Homo sapiens (P51580)
Manually annotated by BRENDA team
Firooz, A.; Ghandi, N.; Hallaji, Z.; Chams-Davatchi, C.; Valikhani, M.; Karbakhsh Davari, M.
Role of thiopurine methyltransferase activity in the safety and efficacy of azathioprine in the treatment of pemphigus vulgaris
Arch. Dermatol.
144
1143-1147
2008
Homo sapiens
Manually annotated by BRENDA team
Hogarth, L.A.; Redfern, C.P.; Teodoridis, J.M.; Hall, A.G.; Anderson, H.; Case, M.C.; Coulthard, S.A.
The effect of thiopurine drugs on DNA methylation in relation to TPMT expression
Biochem. Pharmacol.
76
1024-1035
2008
Homo sapiens
Manually annotated by BRENDA team
Garat, A.; Cauffiez, C.; Renault, N.; Lo-Guidice, J.M.; Allorge, D.; Chevalier, D.; Houdret, N.; Chavatte, P.; Loriot, M.A.; Gala, J.L.; Broly, F.
Characterisation of novel defective thiopurine S-methyltransferase allelic variants
Biochem. Pharmacol.
76
404-415
2008
Homo sapiens (P51580), Homo sapiens
Manually annotated by BRENDA team
Peng, Y.; Feng, Q.; Wilk, D.; Adjei, A.A.; Salavaggione, O.E.; Weinshilboum, R.M.; Yee, V.C.
Structural basis of substrate recognition in thiopurine s-methyltransferase
Biochemistry
47
6216-6225
2008
Mus musculus (O55060), Mus musculus, Homo sapiens (P51580), Homo sapiens
Manually annotated by BRENDA team
Haglund, S.; Taipalensuu, J.; Peterson, C.; Almer, S.
IMPDH activity in thiopurine-treated patients with inflammatory bowel disease - relation to TPMT activity and metabolite concentrations
Br. J. Clin. Pharmacol.
65
69-77
2008
Homo sapiens
Manually annotated by BRENDA team
Tamm, R.; Oselin, K.; Kallassalu, K.; Magi, R.; Anier, K.; Remm, M.; Metspalu, A.
Thiopurine S-methyltransferase (TPMT) pharmacogenetics: three new mutations and haplotype analysis in the Estonian population
Clin. Chem. Lab. Med.
46
974-979
2008
Homo sapiens
Manually annotated by BRENDA team
Zhang, L.; Song, D.; Zhang, W.; Zhao, J.; Jia, L.; Xing, D.
Efficient screening method of the thiopurine methyltransferase polymorphisms for patients considering taking thiopurine drugs in a Chinese Han population in Henan Province (central China)
Clin. Chim. Acta
376
45-51
2007
Homo sapiens
Manually annotated by BRENDA team
Lee, S.S.; Kim, W.Y.; Jang, Y.J.; Shin, J.G.
Duplex pyrosequencing of the TPMT3C and TPMT6 alleles in Korean and Vietnamese populations
Clin. Chim. Acta
398
82-85
2008
Homo sapiens
Manually annotated by BRENDA team
Gardiner, S.J.; Gearry, R.B.; Begg, E.J.; Zhang, M.; Barclay, M.L.
Thiopurine dose in intermediate and normal metabolizers of thiopurine methyltransferase may differ three-fold
Clin. Gastroenterol. Hepatol.
6; 654-60
quiz 604
2008
Homo sapiens
Manually annotated by BRENDA team
Jones, T.S.; Yang, W.; Evans, W.E.; Relling, M.V.
Using HapMap tools in pharmacogenomic discovery: the thiopurine methyltransferase polymorphism
Clin. Pharmacol. Ther.
81
729-734
2007
Homo sapiens
Manually annotated by BRENDA team
Gisbert, J.P.; Gomollon, F.; Cara, C.; Luna, M.; Gonzalez-Lama, Y.; Pajares, J.M.; Mate, J.; Guijarro, L.G.
Thiopurine methyltransferase activity in Spain: a study of 14,545 patients
Dig. Dis. Sci.
52
1262-1269
2007
Homo sapiens
Manually annotated by BRENDA team
Kwan, L.Y.; Devlin, S.M.; Mirocha, J.M.; Papadakis, K.A.
Thiopurine methyltransferase activity combined with 6-thioguanine metabolite levels predicts clinical response to thiopurines in patients with inflammatory bowel disease
Dig. Liver Dis.
40
425-432
2008
Homo sapiens
Manually annotated by BRENDA team
Oselin, K.; Anier, K.
Inhibition of human thiopurine S-methyltransferase by various nonsteroidal anti-inflammatory drugs in vitro: a mechanism for possible drug interactions
Drug Metab. Dispos.
35
1452-1454
2007
Homo sapiens
Manually annotated by BRENDA team
Oliveira, E.; Quental, S.; Alves, S.; Amorim, A.; Prata, M.J.
Do the distribution patterns of polymorphisms at the thiopurine S-methyltransferase locus in sub-Saharan populations need revision? Hints from Cabinda and Mozambique
Eur. J. Clin. Pharmacol.
63
703-706
2007
Homo sapiens
Manually annotated by BRENDA team
Kham, S.K.; Soh, C.K.; Liu, T.C.; Chan, Y.H.; Ariffin, H.; Tan, P.L.; Yeoh, A.E.
Thiopurine S-methyltransferase activity in three major Asian populations: a population-based study in Singapore
Eur. J. Clin. Pharmacol.
64
373-379
2008
Homo sapiens
Manually annotated by BRENDA team
Bezier, M.; Reguiai, Z.; Vitry, F.; Broly, F.; Bernard, P.
Thiopurine S-methyltransferase genotypic analysis in autoimmune bullous diseases
Eur. J. Dermatol.
18
512-517
2008
Homo sapiens
Manually annotated by BRENDA team
Perri, D.; Cole, D.E.; Friedman, O.; Piliotis, E.; Mintz, S.; Adhikari, N.K.
Azathioprine and diffuse alveolar haemorrhage: the pharmacogenetics of thiopurine methyltransferase
Eur. Respir. J.
30
1014-1017
2007
Homo sapiens
Manually annotated by BRENDA team
Richard, V.S.; Al-Ismail, D.; Salamat, A.
Should we test TPMT enzyme levels before starting azathioprine?
Hematology
12
359-360
2007
Homo sapiens
Manually annotated by BRENDA team
Compagni, A.; Bartoli, S.; Buehrlen, B.; Fattore, G.; Ibarreta, D.; de Mesa, E.G.
Avoiding adverse drug reactions by pharmacogenetic testing: a systematic review of the economic evidence in the case of TPMT and AZA-induced side effects
Int. J. Technol. Assess. Health Care
24
294-302
2008
Homo sapiens
Manually annotated by BRENDA team
Fargher, E.A.; Tricker, K.; Newman, W.; Elliott, R.; Roberts, S.A.; Shaffer, J.L.; Bruce, I.; Payne, K.
Current use of pharmacogenetic testing: a national survey of thiopurine methyltransferase testing prior to azathioprine prescription
J. Clin. Pharm. Ther.
32
187-195
2007
Homo sapiens
Manually annotated by BRENDA team
Fakhoury, M.; Andreu-Gallien, J.; Mahr, A.; Medard, Y.; Azougagh, S.; Vilmer, E.; Jacqz-Aigrain, E.
Should TPMT genotype and activity be used to monitor 6-mercaptopurine treatment in children with acute lymphoblastic leukaemia?
J. Clin. Pharm. Ther.
32
633-639
2007
Homo sapiens
Manually annotated by BRENDA team
Hoover, S.; Striker, R.
Thiopurines inhibit bovine viral diarrhea virus production in a thiopurine methyltransferase-dependent manner
J. Gen. Virol.
89
1000-1009
2008
Bos taurus, Homo sapiens
Manually annotated by BRENDA team
Rutherford, K.; Daggett, V.
Four human thiopurine s-methyltransferase alleles severely affect protein structure and dynamics
J. Mol. Biol.
379
803-814
2008
Homo sapiens
Manually annotated by BRENDA team
Chowdhury, J.; Kagiala, G.V.; Pushpakom, S.; Lauzon, J.; Makin, A.; Atrazhev, A.; Stickel, A.; Newman, W.G.; Backhouse, C.J.; Pilarski, L.M.
Microfluidic platform for single nucleotide polymorphism genotyping of the thiopurine S-methyltransferase gene to evaluate risk for adverse drug events
J. Mol. Diagn.
9
521-529
2007
Homo sapiens
Manually annotated by BRENDA team
Tamori, A.; Shinzaki, M.; Kosaka, S.; Hayashi, T.; Iwai, S.; Enomoto, M.; Habu, D.; Sakaguchi, H.; Kawada, N.; Hino, M.; Shiomi, S.; Nishiguchi, S.
Thiopurine S-methyltransferase gene polymorphism in Japanese patients with autoimmune liver diseases
Liver Int.
27
95-100
2007
Homo sapiens
Manually annotated by BRENDA team
Taja-Chayeb, L.; Vidal-Millan, S.; Gutierrez, O.; Ostrosky-Wegman, P.; Duenas-Gonzalez, A.; Candelaria, M.
Thiopurine S-methyltransferase gene (TMPT) polymorphisms in a Mexican population of healthy individuals and leukemic patients
Med. Oncol.
25
56-62
2008
Homo sapiens
Manually annotated by BRENDA team
Slanar, O.; Bortlik, M.; Buzkova, H.; Donoval, R.; Pechandova, K.; Sebesta, I.; Lukas, M.; Perlik, F.
Polymorphisms of the TPMT gene in the Czech healthy population and patients with inflammatory bowel disease
Nucleosides Nucleotides Nucleic Acids
27
835-838
2008
Homo sapiens
Manually annotated by BRENDA team
Lindqvist, M.; Skoglund, K.; Karlgren, A.; Soederkvist, P.; Peterson, C.; Kidhall, I.; Almer, S.
Explaining TPMT genotype/phenotype discrepancy by haplotyping of TPMT*3A and identification of a novel sequence variant, TPMT*23
Pharmacogenet. Genomics
17
891-895
2007
Homo sapiens
Manually annotated by BRENDA team
Roberts, R.L.; Gearry, R.B.; Bland, M.V.; Sies, C.W.; George, P.M.; Burt, M.; Marinaki, A.M.; Arenas, M.; Barclay, M.L.; Kennedy, M.A.
Trinucleotide repeat variants in the promoter of the thiopurine S-methyltransferase gene of patients exhibiting ultra-high enzyme activity
Pharmacogenet. Genomics
18
434-438
2008
Homo sapiens
Manually annotated by BRENDA team
Ujiie, S.; Sasaki, T.; Mizugaki, M.; Ishikawa, M.; Hiratsuka, M.
Functional characterization of 23 allelic variants of thiopurine S-methyltransferase gene (TPMT*2 - *24)
Pharmacogenet. Genomics
18
887-893
2008
Homo sapiens
Manually annotated by BRENDA team
Cooper, S.C.; Ford, L.T.; Berg, J.D.; Lewis, M.J.
Ethnic variation of thiopurine S-methyltransferase activity: a large, prospective population study
Pharmacogenomics
9
303-309
2008
Homo sapiens
Manually annotated by BRENDA team
Chrzanowska, M.; Kurzawski, M.; Dro?dzik, M.; Mazik, M.; Oko, A.; Czekalski, S.
Thiopurine S-methyltransferase phenotype-genotype correlation in hemodialyzed patients
Pharmacol. Rep.
58
973-978
2006
Homo sapiens
Manually annotated by BRENDA team
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
Ther. Drug Monit.
29
1-5
2007
Homo sapiens
Manually annotated by BRENDA team
de Boer, N.K.; van Bodegraven, A.A.; de Graaf, P.; van der Hulst, R.W.; Zoetekouw, L.; van Kuilenburg, A.B.
Paradoxical elevated thiopurine S-methyltransferase activity after pancytopenia during azathioprine therapy: potential influence of red blood cell age
Ther. Drug Monit.
30
390-393
2008
Homo sapiens
Manually annotated by BRENDA team
Alvarez Beltran, M.; Infante Pina, D.; Tormo Carnice, R.; Segarra Canton, O.; Redecillas Ferreiro, S.
Optimising azathioprine treatment: determination of thiopurine methyltransferase activity and thiopurine metabolites
An. Pediatr. (Barc. )
70
126-131
2009
Homo sapiens
Manually annotated by BRENDA team
el-Azhary, R.A.; Farmer, S.A.; Drage, L.A.; Rogers, R.S.; McEvoy, M.T.; Davis, M.D.; Bridges, A.G.; Gibson, L.E.
Thioguanine nucleotides and thiopurine methyltransferase in immunobullous diseases: optimal levels as adjunctive tools for azathioprine monitoring
Arch. Dermatol.
145
644-652
2009
Homo sapiens
Manually annotated by BRENDA team
Milek, M.; Karas Kuzelicki, N.; Smid, A.; Mlinaric-Rascan, I.
S-adenosylmethionine regulates thiopurine methyltransferase activity and decreases 6-mercaptopurine cytotoxicity in MOLT lymphoblasts
Biochem. Pharmacol.
77
1845-1853
2009
Homo sapiens
Manually annotated by BRENDA team
Feng, Q.; Vannaprasaht, S.; Peng, Y.; Angsuthum, S.; Avihingsanon, Y.; Yee, V.C.; Tassaneeyakul, W.; Weinshilboum, R.M.
Thiopurine S-methyltransferase pharmacogenetics: Functional characterization of a novel rapidly degraded variant allozyme
Biochem. Pharmacol.
79
1053-1061
2009
Homo sapiens (P51580), Homo sapiens
Manually annotated by BRENDA team
Kham, S.K.; Soh, C.K.; Aw, D.C.; Yeoh, A.E.
TPMT*26 (208F-->L), a novel mutation detected in a Chinese
Br. J. Clin. Pharmacol.
68
120-123
2009
Homo sapiens
Manually annotated by BRENDA team
Tsui, N.
Multiple thiopurine S-methyltransferase variation detection: A step toward personalized medicine
Clin. Chem.
54
1598-1599
2008
Homo sapiens
Manually annotated by BRENDA team
Schaeffeler, E.; Zanger, U.M.; Eichelbaum, M.; Asante-Poku, S.; Shin, J.G.; Schwab, M.
Highly multiplexed genotyping of thiopurine S-methyltransferase variants using MALD-TOF mass spectrometry: reliable genotyping in different ethnic groups
Clin. Chem.
54
1637-1647
2008
Homo sapiens
Manually annotated by BRENDA team
Vestergaard, T.; Bygum, A.
An audit of thiopurine methyltransferase genotyping and phenotyping before intended azathioprine treatment for dermatological conditions
Clin. Exp. Dermatol.
35
140-144
2010
Homo sapiens
Manually annotated by BRENDA team
Gisbert, J.
Role of monitoring thiopurine methyltransferase (TPMT) activity in the individualized therapy with azathioprine or 6-mercaptopurine
Curr. Pharmacogenomics Person. Med.
6
33-44
2008
Homo sapiens
-
Manually annotated by BRENDA team
Egle, R.; Milek, M.; Mlinaric-Rascan, I.; Fahr, A.; Kristl, J.
A novel gene delivery system for stable transfection of thiopurine-S-methyltransferase gene in versatile cell types
Eur. J. Pharm. Biopharm.
69
23-30
2008
Homo sapiens
Manually annotated by BRENDA team
Stocco, G.; Crews, K.R.; Evans, W.E.
Genetic polymorphism of inosine-triphosphate-pyrophosphatase influences mercaptopurine metabolism and toxicity during treatment of acute lymphoblastic leukemia individualized for thiopurine-S-methyl-transferase status
Expert. Opin. Drug Saf.
9
23-37
2010
Homo sapiens
Manually annotated by BRENDA team
Cheon, J.H.; Kim, J.H.; Kim, B.Y.; Kim, S.W.; Hong, S.Y.; Eun, C.S.; Hong, S.S.; Byeon, J.S.; Kim, T.I.; Han, D.S.; Yang, S.K.; Lee, K.R.; Kim, W.H.
Allele frequency of thiopurine methyltransferase and inosine triphosphate pyrophosphatase gene polymorphisms in Korean patients with inflammatory bowel diseases
Hepatogastroenterology
56
421-423
2009
Homo sapiens
Manually annotated by BRENDA team
Tomkova, J.; Friedecky, D.; Polynkova, A.; Adam, T.
Capillary electrophoresis determination of thiopurine methyl transferase activity in erythrocytes
J. Chromatogr. B
877
1943-1945
2009
Homo sapiens
Manually annotated by BRENDA team
Gonzalez-Del Angel, A.; Bermadez-Lapez, C.; Alcantara-Ortigoza, M.; Vela-Amieva, M.; Castillo-Cruz, R.; Martinez, V.; Torres-Espadola, L.
Thiopurine S-methyltransferase (TPMT) genetic polymorphisms in Mexican newborns
J. Clin. Pharm. Ther.
34
703-708
2009
Homo sapiens
Manually annotated by BRENDA team
Hindorf, U.; Jahed, K.; Bergquist, A.; Verbaan, H.; Prytz, H.; Wallerstedt, S.; Werner, M.; Olsson, R.; Bjoernsson, E.; Peterson, C.; Almer, S.H.
Characterisation and utility of thiopurine methyltransferase and thiopurine metabolite measurements in autoimmune hepatitis
J. Hepatol.
52
106-111
2010
Homo sapiens
Manually annotated by BRENDA team
Schmiegelow, K.; Forestier, E.; Kristinsson, J.; Soederhaell, S.; Vettenranta, K.; Weinshilboum, R.; Wesenberg, F.; Wesenberg, F.
Thiopurine methyltransferase activity is related to the risk of relapse of childhood acute lymphoblastic leukemia: results from the NOPHO ALL-92 study
Leukemia
23
557-564
2009
Homo sapiens
Manually annotated by BRENDA team
Sheffield, L.J.; Irving, P.; Gupta, A.; Byron, K.; Macrae, F.A.; Phillimore, H.; Dronavalli, M.; Rose, R.; George, P.; Walmsley, T.; Dixon, B.; Poole, S.; Dooley, M.; Sparrow, M.
Thiopurine methyltransferase and thiopurine metabolite testing in patients with inflammatory bowel disease who are taking thiopurine drugs
Pharmacogenomics
10
1091-1099
2009
Homo sapiens
Manually annotated by BRENDA team
Karas-Kuzelicki, N.; Mlinaric-Rascan, I.
Individualization of thiopurine therapy: thiopurine S-methyltransferase and beyond
Pharmacogenomics
10
1309-1322
2009
Homo sapiens
Manually annotated by BRENDA team
Serpe, L.; Calvo, P.L.; Muntoni, E.; DAntico, S.; Giaccone, M.; Avagnina, A.; Baldi, M.; Barbera, C.; Curti, F.; Pera, A.; Eandi, M.; Zara, G.P.; Canaparo, R.
Thiopurine S-methyltransferase pharmacogenetics in a large-scale healthy Italian-Caucasian population: differences in enzyme activity
Pharmacogenomics
10
1753-1765
2009
Homo sapiens
Manually annotated by BRENDA team
Silva, M.R.; de Oliveira, B.M.; Viana, M.B.; Murao, M.; Romanha, A.J.
Thiopurine S-methyltransferase (TPMT) gene polymorphism in Brazilian children with acute lymphoblastic leukemia: association with clinical and laboratory data
Ther. Drug Monit.
30
700-704
2008
Homo sapiens
Manually annotated by BRENDA team
Milek, M.; Smid, A.; Tamm, R.; Kuzelicki, N.K.; Metspalu, A.; Mlinaric-Rascan, I.
Post-translational stabilization of thiopurine S-methyltransferase by S-adenosyl-L-methionine reveals regulation of TPMT*1 and *3C allozymes
Biochem. Pharmacol.
83
969-976
2012
Homo sapiens
Manually annotated by BRENDA team
Wennerstrand, P.; Dametto, P.; Hennig, J.; Klingstedt, T.; Skoglund, K.; Lindqvist Appell, M.; Martensson, L.G.
Structural characteristics determine the cause of the low enzyme activity of two thiopurine S-methyltransferase allelic variants: a biophysical characterization of TPMT*2 and TPMT*5
Biochemistry
51
5912-5920
2012
Homo sapiens
Manually annotated by BRENDA team
Pavlovic, S.; Zukic, B.
Individualized therapy: Role of thiopurine S-methyltransferase protein and genetic variants
J. Med. Biochem.
29
150-155
2010
Homo sapiens
-
Manually annotated by BRENDA team
Hosni-Ahmed, A.; Barnes, J.D.; Wan, J.; Jones, T.S.
Thiopurine methyltransferase predicts the extent of cytotoxicty and DNA damage in astroglial cells after thioguanine exposure
PLoS ONE
6
e29163
2011
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Kasirer, Y.; Mevorach, R.; Renbaum, P.; Algur, N.; Soiferman, D.; Beeri, R.; Rachman, Y.; Segel, R.; Turner, D.
Thiopurine S-methyltransferase (TPMT) activity is better determined by biochemical assay versus genotyping in the Jewish population
Digest. Dis. Sci.
59
1207-1212
2014
Homo sapiens (P51580)
Manually annotated by BRENDA team
Wennerstrand, P.; Martensson, L.G.; Soederhaell, S.; Zimdahl, A.; Appell, M.L.
Methotrexate binds to recombinant thiopurine S-methyltransferase and inhibits enzyme activity after high-dose infusions in childhood leukaemia
Eur. J. Clin. Pharmacol.
69
1641-1649
2013
Homo sapiens (P51580), Homo sapiens
Manually annotated by BRENDA team
Roberts, R.L.; Wallace, M.C.; Drake, J.M.; Stamp, L.K.
Identification of a novel thiopurine S-methyltransferase allele (TPMT 37)
Pharmacogenet. Genomics
24
320-323
2014
Homo sapiens (P51580)
Manually annotated by BRENDA team
Wennerstrand, P.; Blissing, A.; Martensson, L.G.
In vitro protein stability of two naturally occurring thiopurine S-methyltransferase variants biophysical characterization of TPMT*6 and TPMT*8
ACS Omega
2
4991-4999
2017
Homo sapiens (P51580)
Manually annotated by BRENDA team
Citterio-Quentin, A.; El Mahmoudi, A.; Perret, T.; Conway, A.; Ryan, A.; Beringer, A.; Lachaux, A.; Boulieu, R.
Red Blood cell IMPDH activity in adults and children with or without azathioprine Relationship between thiopurine metabolites, ITPA and TPMT activities
Basic Clin. Pharmacol. Toxicol.
124
600-606
2019
Homo sapiens
Manually annotated by BRENDA team
Mei, S.; Li, X.; Gong, X.; Zhang, X.; Li, X.; Yang, L.; Zhu, L.; Zhou, H.; Liu, Y.; Zhou, A.; Zhang, X.; Zhao, Z.
Comparison of 6-mercaptopurine with 6-thioguanine for the analysis of thiopurine S-methyltransferase activity in human erythrocyte by LC-MS/MS
Biomed. Chromatogr.
31
e3959
2017
Homo sapiens
Manually annotated by BRENDA team
Ma, J.; Sies, C.W.; Pike, L.S.
Analytical and clinical validation of an LC-MS/MS method to measure thiopurine S-methyltransferase activity by quantifying d3-6-MMP
Clin. Biochem.
54
100-105
2018
Homo sapiens
Manually annotated by BRENDA team
Rieger, H.; Schmidt, P.; Schaeffeler, E.; Abe, M.; Schiffhauer, M.; Schwab, M.; von Ahsen, N.; Zurek, G.; Kirchherr, H.; Shipkova, M.; Wieland, E.
Validation of a high-performance liquid chromatography method for thiopurine S-methyltransferase activity in whole blood using 6-mercaptopurine as substrate
Clin. Chem. Lab. Med.
56
803-809
2018
Homo sapiens
Manually annotated by BRENDA team
Pashazadeh, P.; Marjani, A.; Asadi, J.; Khoshnia, M.
Thiopurine methyltransferase genetic polymorphisms and activity and metabolic products of azathioprine in patients with inflammatory bowel disease
Endocr. Metab. Immune Disord. Drug Targets
19
541-547
2019
Homo sapiens
Manually annotated by BRENDA team
Illamola, S.M.; Echaabi, A.K.; Mazeron, C.; Deshayes, S.; Loriot, M.A.; Pallet, N.
Development and validation of a UPLC-UV method for the quantification of thiopurine methyltransferase enzyme activity in human erythrocytes
J. Chromatogr. B Analyt. Technol. Biomed. Life Sci.
1113
91-97
2019
Homo sapiens
Manually annotated by BRENDA team
Pecher, D.; Dokupilova, S.; Zelinkova, Z.; Peppelenbosch, M.; Mikusova, V.; Mikus, P.
Determination of thiopurine S-methyltransferase activity by hydrophilic interaction liquid chromatography hyphenated with mass spectrometry
J. Pharm. Biomed. Anal.
142
244-251
2017
Homo sapiens
Manually annotated by BRENDA team