2.1.1.67: thiopurine S-methyltransferase
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For detailed information about thiopurine S-methyltransferase, go to the full flat file.
Word Map on EC 2.1.1.67
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2.1.1.67
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azathioprine
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6-mercaptopurine
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bowel
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pharmacogenetics
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children
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lymphoblastic
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leukemia
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myelosuppression
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erythrocyte
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tpmt*2
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crohn
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thioguanine
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dosing
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s-methylation
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autoimmune
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marrow
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remission
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caucasian
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leukopenia
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myelotoxicity
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ulcerative
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6-methylmercaptopurine
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methotrexate
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ethnic
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inosine
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colitis
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azathioprine-induced
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medicine
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allele-specific
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interindividual
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nudt15
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5-aminosalicylic
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thiopurine-induced
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allopurinol
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pancytopenia
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neutropenia
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dihydropyrimidine
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infliximab
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drug-metabolizing
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pyrophosphohydrolase
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trimodal
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hematotoxicity
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analysis
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nudix
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pemphigus
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diagnostics
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mofetil
- 2.1.1.67
- azathioprine
- 6-mercaptopurine
- bowel
-
pharmacogenetics
- children
- lymphoblastic
- leukemia
-
myelosuppression
- erythrocyte
-
tpmt*2
- crohn
- thioguanine
-
dosing
-
s-methylation
- autoimmune
- marrow
-
remission
-
caucasian
- leukopenia
-
myelotoxicity
-
ulcerative
- 6-methylmercaptopurine
- methotrexate
-
ethnic
- inosine
- colitis
-
azathioprine-induced
- medicine
-
allele-specific
-
interindividual
-
nudt15
-
5-aminosalicylic
-
thiopurine-induced
- allopurinol
- pancytopenia
- neutropenia
- dihydropyrimidine
-
infliximab
-
drug-metabolizing
-
pyrophosphohydrolase
-
trimodal
-
hematotoxicity
- analysis
-
nudix
- pemphigus
- diagnostics
- mofetil
Reaction
Synonyms
6-thiopurine S-methyltransferase, 6-thiopurine transmethylase, mercaptopurine methyltransferase, thiopurine methyl transferase, thiopurine methyltransferase, thiopurine S-methyltransferase, thiopurine-S-methyl-transferase, TMPT, TPMT
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Application
Application on EC 2.1.1.67 - thiopurine S-methyltransferase
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analysis
diagnostics
medicine
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determination of thiopurine S-methyltransferase activity in erythrocytes using 6-thioguanine as substrate and a non-extraction liquid chromatographic technique. This method minimzes sample-handling, reduces inherent imprecision, the possibility of laboratory error and with the potential for further automation, makes it ideal for use in a regional refferal laboratory
analysis
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monitoring of 6-thiopurine S-methyltransferase activity is especially important when patients are treated with 6-thiopurine drugs (drugs in treatment of acute lymphoblastic leukemia), since severe bone marrow toxicity may be induced if patients have deficient 6-thiopurine S-methyltransferase activity. The HPLC-based method enables the rapid screening of 6-6-thiopurine S-methyltransferase activities in patients treated with 6-thiopurines
analysis
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monitoring of TPMT activity may be of benefit to improve thiopurine therapy
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the chip-based miniaturization provides a clinically feasible genotyping platform for one-at-a-time testing
diagnostics
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thiopurine S-methyltransferase genotypes or phenotypes may be a predictive factor for azathioprine-induced toxicities
medicine
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enzyme may be a target for clinically significant drug interactions, the common genetic polymorphism might be a risk factor for the occurence of therapy-dependent secondary leukemia
medicine
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enzyme activity might represent one factor responsible for variations in the therapeutic or toxic effects of thiopurine and thiopyrimidine drugs used clinically to treat recipients of transplanted kidneys and patients with renal disease such as glomerulonephritis
medicine
identification of a novel non-functional allele of the thiopurine S-methyltransferase gene enhances the efficiency of genotyping methods to predict patients at risk of an inadequate response to thiopurine therapy
medicine
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the knowledge of the genetic basis of interindividual variability in thiopurine S-methyltransferase activity could enhance the efficiency of genotyping methods to preduct patients at risk of inadequate response to thiopurine therapy
medicine
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the knowledge of the genetic basis of interindividual variability in thiopurine S-methyltransferase activity could enhance the efficiency of genotyping methods to product patients at risk of inadequate response to thiopurine therapy
medicine
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azathioprine sodium is a purine antagonist commonly used as an adjuvant immunosuppressive agent in treating Pemphigus Vulgaris, mercaptopurine is the active compound, TPMT is the principal inactivation enzyme for this cytotoxic metabolite in hematopoietic tissues
medicine
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detecting TPMT genetic variants before the administration of azathioprine has the potential to prevent serious and costly adverse drug reactions, such as neutropenia
medicine
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evaluation of a possible long-term effect of mesalazine or azathioprine on thiopurine methyltransferase activity is of particular clinical importance because both drugs can to be given for several years in inflammatory bowel disease
medicine
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first case of azathioprine-associated AML linked to low thiopurine S-methyltransferase enzyme activity
medicine
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genetic variation in thiopurine S-methyltransferase is a major factor for wide variation in the metabolism and safety of thiopurine drugs
medicine
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genotyping at diagnosis identifies patients with a homozygous mutant TPMT and may prevent severe and life-threatening toxicity, ALL treatment monitoring should preferentially be based on repeated determinations of intracellular active metabolites, 6-TGN, and methylated metabolites
medicine
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individuals with decreased TPMT activity are at great risk for adverse reactions if treated with conventional thiopurine doses
medicine
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individuals with decreased TPMT activity are at high risk of fatal adverse reactions if treated with conventional thiopurine doses
medicine
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myelosuppression occurs in 2-7% of inflammatory bowel disease patients treated with azothioprine, and can be associated with reduced activity of thiopurine methyltransferase in some patients
medicine
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patients carrying a variant genotype have low TPMT activity and produce elevated levels of 6-thioguanine nucleotides in their red blood cells, 6-TGN accumulation may result in azathioprine-induced bone marrow myelosuppression in the course of treatment with the drug in a standard dosage regimen in patients following renal transplantation
medicine
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patients carrying defective mutations in TMPT gene have elevated thioguanine nucleotides concentrations that finally result in severe or even fatal hematopoietic toxicities when they are treated with standard doses of 6-mercaptopurine
medicine
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patients with inflammatory bowel disease may have different thiopurine dose requirements in relation to thiopurine methyltransferase genotype or phenotype
medicine
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polymorphisms at the thiopurine S-methyltransferase coding gene determine enzyme activity and consequently, the development of toxicity secondary to thiopurines
medicine
single nucleotide polymorphisms are known to be responsible for variations in the metabolism of numerous drugs in humans, thiopurine S-methyltransferase displays polymorphisms with varying prevalence among different populations
medicine
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the goal is to determine which metabolite of azathioprine has the most antiviral activity and to gain a better understanding of how this compound may act in vitro
medicine
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the goal is to determine which metabolite of azathioprine has the most antiviral activity and to gain a better understanding of how this compound may act in vitro
medicine
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the knowledge of the TPMT activity distribution in each population seems relevant, the incidence of hematologic adverse effects associated with azathioprine and 6-mercaptopurine treatment probably depends on that distribution
medicine
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the murine model recapitulates many clinical features of the human polymorphism and provides a preclinical system for establishing safer regimens of genetically influenced antileukemic drug therapy
medicine
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the remarkable change in enzyme activity of TPMT may be explained by differences in the age of red blood cells, as younger erythrocytes have a higher TPMT activity
medicine
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the results suggest that coadministration of thiopurines and various nonsteriodal anti-inflammatory drugs may lead to drug interactions
medicine
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the use of azothioprine and mercaptopurine is limited by toxicity, especially myelosuppression, which is related to activity of the enzyme thiopurine S-methyltransferase
medicine
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thiopurine methyltransferase activity inversely correlated with clinical response to thiopurine treatment in inflammatory bowel disease
medicine
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thiopurine methyltransferase is a genetically moderated key enzyme involved in the metabolism of azathioprine that can be used to stratify individuals into different levels of risk of developing neutropaenia
medicine
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thiopurine methyltransferase is the main enzyme responsible for inactivating toxic products of azathioprine metabolism
medicine
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thiopurine methyltransferase metabolises thiopurine drugs and influences their cytotoxic activity
medicine
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thiopurine S-methyltransferase activity is inversely related to the risk of developing severe hematopoietic toxicity in patients treated with azathioprine
medicine
thiopurine S-methyltransferase is a key enzyme in the detoxification of thiopurine drugs widely used in the treatment of various diseases, such as inflammatory bowel diseases, acute lymphoblastic leukaemia and rheumatic diseases
medicine
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thiopurine S-methyltransferase is an enzyme responsible for the detoxification of the widely used thiopurine drugs
medicine
thiopurine S-methyltransferase modulates the cytotoxic effects of thiopurine prodrugs such as 6-mercaptopurine by methylating them in a reaction using S-adenosyl-L-methionine as the donor
medicine
thiopurine S-methyltransferase modulates the cytotoxic effects of thiopurine prodrugs such as 6-mercaptopurine by methylating them in a reaction using S-adenosyl-L-methionine as the donor
medicine
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while factors other than TPMT status are likely to be involved in azathioprine toxicity, the majority of evidence suggests that TPMT deficiency is a significant independent risk factor for myelotoxicity
medicine
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determination of TPMT and monitoring of thiopurine metabolites allows azathioprine treatment to be optimised
medicine
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induction of thiopurine methyltransferase is associated with recalcitrant disease
medicine
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mercaptopurine dose can be adjusted on the basis of TPMT genotype to mitigate toxicity in pediatric patients with acute lymphoblastic leukemia
medicine
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TPMT activity is a good prediction factor for the toxicity and efficacy of the antileukemic thiopurine therapy
medicine
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low enzyme level can lead to greater sensitivity to thiopurine therapy in astroglial cells
medicine
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low enzyme level can lead to greater sensitivity to thiopurine therapy in astroglial cells
medicine
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thiopurine S-methyltransferase gene polymorphisms are pharmacogenetic markers which enable the individualization of thiopurine drug therapy
medicine
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enzyme polymorphisms are associated with 6-thioguanine levels in patients using azathioprine