Genomes and Genes
Gene Symbol: TPMT
Description: thiopurine S-methyltransferase
Alias: TPMTD, thiopurine S-methyltransferase, S-adenosyl-L-methionine:thiopurine S-methyltransferase
Publications202 found, 100 shown here
- Genotype and allele frequencies of TPMT, NAT2, GST, SULT1A1 and MDR-1 in the Egyptian populationSamar I Hamdy
Department of Pharmaceutical Sciences, Tohoku University Hospital, Sendai, Japan, and Faculty of Pharmacy, Cairo University, Egypt
Br J Clin Pharmacol 55:560-9. 2003The goal of this study was to determine the frequencies of important allelic variants in the TPMT, NAT2, GST, SULT1A1 and MDR-1 genes in the Egyptian population and compare them with the frequencies in other ethnic populations.
- Genetic polymorphism of thiopurine S-methyltransferase: clinical importance and molecular mechanismsE Y Krynetski
Department of Pharmaceutical Sciences, St Jude Children s Research Hospital, Memphis, TN 38105, USA
Pharmacogenetics 6:279-90. 1996Thiopurine S-methyltransferase (TPMT) catalyses the S-methylation of thiopurines such as mercaptopurine and thioguanine...
- Molecular diagnosis of thiopurine S-methyltransferase deficiency: genetic basis for azathioprine and mercaptopurine intoleranceC R Yates
St Jude Children s Research Hospital, Memphis, Tennessee 38105 2794, USA
Ann Intern Med 126:608-14. 1997Thiopurine S-methyltransferase (TPMT) catalyzes the S-methylation (that is, inactivation) of mercaptopurine, azathioprine, and thioguanine and exhibits genetic polymorphism...
- Enhanced proteolysis of thiopurine S-methyltransferase (TPMT) encoded by mutant alleles in humans (TPMT*3A, TPMT*2): mechanisms for the genetic polymorphism of TPMT activityH L Tai
St Jude Children s Research Hospital, 332 North Lauderdale Street, Memphis, TN 38101, USA
Proc Natl Acad Sci U S A 94:6444-9. 1997b>TPMT is a cytosolic enzyme that catalyzes the S-methylation of aromatic and heterocyclic sulfhydryl compounds, including medications such as mercaptopurine and thioguanine...
- Human thiopurine methyltransferase pharmacogenetics: gene sequence polymorphismsD Otterness
Department of Pharmacology, Mayo Medical School Mayo Clinic Mayo Foundation, Rochester, MN 55905, USA
Clin Pharmacol Ther 62:60-73. 1997Thiopurine methyltransferase (TPMT) catalyzes the S-methylation of thiopurine drugs. TPMT activity is regulated by a common genetic polymorphism that is associated with large individual variations in thiopurine toxicity and efficacy...
- Thiopurine methyltransferase alleles in British and Ghanaian populationsM M Ameyaw
University of Aberdeen, Department of Medicine and Therapeutics, Institute of Medical Sciences, Foresterhill, Aberdeen AB25 2ZD, UK
Hum Mol Genet 8:367-70. 1999Thiopurine methyltransferase (TPMT) catalyses the S-methylation of thiopurine drugs such as 6-mercapto-purine, 6-thioguanine and azathioprine...
- The frequency and distribution of thiopurine methyltransferase alleles in Caucasian and Asian populationsE S Collie-Duguid
The University of Aberdeen, Department of Medicine and Therapeutics, Institute of Medical Sciences, Foresterhill, UK
Pharmacogenetics 9:37-42. 1999..The wild-type allele is defined as TPMT*1 and the mutant alleles are TPMT*2 (G238C), TPMT*3A (G460A and A719G), TPMT*3B (G460A) and TPMT*3B (A719G)...
- Genetic analysis of thiopurine methyltransferase polymorphism in a Japanese populationM Hiratsuka
Department of Pharmaceutical Sciences, Tohoku University Hospital, 1 1 Seiryo machi, Aoba ku, Sendai, Japan
Mutat Res 448:91-5. 2000Thiopurine methyltransferase (TPMT) catalyses the S-methylation of thiopurine drugs such as 6-mercaptopurine, 6-thioguanine, and azathiopurine...
- Molecular analysis of thiopurine S-methyltransferase alleles in South-east Asian populationsJan Gowth Chang
Department of Laboratory Medicine, China Medical College Hospital, Taichung, Taiwan
Pharmacogenetics 12:191-5. 2002Thiopurine S-methyltransferase (TPMT) catalyses the S-methylation of thiopurine drugs. In Caucasians, four variant TPMT alleles have been detected in over 80% of individuals with low or intermediate TPMT activity...
- Thiopurine methyltransferase polymorphisms in a multiracial asian population and children with acute lymphoblastic leukemiaS K Y Kham
Department of Pediatrics, National University of Singapore, Singapore
J Pediatr Hematol Oncol 24:353-9. 2002The purpose of this study was to determine the frequency of thiopurine methyltransferase (TPMT) polymorphisms in a multiracial Asian population and to assess its relevance in the management of childhood acute lymphoblastic leukemia (ALL)...
- Azathioprine therapy and adverse drug reactions in patients with inflammatory bowel disease: impact of thiopurine S-methyltransferase polymorphismMatthias Schwab
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Stuttgart, Germany
Pharmacogenetics 12:429-36. 2002..Whereas azathioprine-related pancytopenia has been clearly linked to thiopurine S-methyltransferase (TPMT) polymorphism limited data are available to explain gastrointestinal side effects...
- Thiopurine methyltransferase polymorphisms in a Brazilian populationW L Boson
Departamento de Farmacologia, Universidade Federal de Minas Gerais, Belo Horizonte, Brazil
Pharmacogenomics J 3:178-82. 2003Thiopurine methyltransferase (TPMT) catalyses the S-methylation of thiopurine drugs. Low-activity phenotypes are correlated with several mutations in the TPMT gene...
- Comprehensive analysis of thiopurine S-methyltransferase phenotype-genotype correlation in a large population of German-Caucasians and identification of novel TPMT variantsElke Schaeffeler
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Stuttgart, Germany
Pharmacogenetics 14:407-17. 2004The thiopurine S-methyltransferase (TPMT) genetic polymorphism has a significant clinical impact on the toxicity of thiopurine drugs...
- Molecular analysis of the thiopurine S-methyltransferase alleles in Bolivians and TibetansH F Lu
Department of Molecular Medicine, China Medical University Hospital, Taichung, China
J Clin Pharm Ther 30:491-6. 2005Thiopurine drugs are used as immunosuppressant or cytotoxic drugs. Thiopurine S-methyltransferase (TPMT) methylates and thereby modulates the therapeutic and toxic effects of these drugs...
- Liquid chromatography-tandem mass spectrometry analysis of erythrocyte thiopurine nucleotides and effect of thiopurine methyltransferase gene variants on these metabolites in patients receiving azathioprine/6-mercaptopurine therapyThierry Dervieux
Prometheus Laboratories, San Diego, CA 92121, USA
Clin Chem 51:2074-84. 2005Polymorphic thiopurine S-methyltransferase (TPMT) is a major determinant of thiopurine toxicity.
- TPMT genotype and the use of thiopurines in paediatric inflammatory bowel diseaseG Stocco
Department of Biomedical Sciences, University of Trieste, via L Giorgieri 7, 9, Italy
Dig Liver Dis 37:940-5. 2005..They are metabolised via methylation by thiopurine-S-methyltransferase (TPMT), which displays a genetically determined polymorphic activity...
- Inosine triphosphate pyrophosphatase and thiopurine s-methyltransferase genotypes relationship to azathioprine-induced myelosuppressionZuzana Zelinkova
Laboratory of Experimental Internal Medicine, Department of Gastroenterology and Hepatology, Academic Medical Center, Amsterdam, The Netherlands
Clin Gastroenterol Hepatol 4:44-9. 2006..Mutations in the thiopurine S-methyltransferase (TPMT) and inosine triphosphate pyrophosphatase (ITPA) genes have been associated with the occurrence of AZA-related ..
- Glutathione-S-transferase genotypes and the adverse effects of azathioprine in young patients with inflammatory bowel diseaseGabriele Stocco
Department of Biomedical Sciences, University of Trieste, Trieste, Italy
Inflamm Bowel Dis 13:57-64. 2007..occur in 15%-38% of patients and the majority are not explained by thiopurine-S-methyltransferase (TPMT) deficiency...
- Thiopurine S-methyltransferase activity in three major Asian populations: a population-based study in SingaporeShirley Kow Yin Kham
Department of Paediatrics, National University of Singapore, and Department of Haematology Oncology, National University Hospital, Singapore City, Republic of Singapore
Eur J Clin Pharmacol 64:373-9. 2008The distribution of thiopurine methyltransferase (TPMT) activity in Asian populations has not been well documented...
- Prospective evaluation of the pharmacogenetics of azathioprine in the treatment of inflammatory bowel diseaseA Ansari
Department of Gastroenterology, St Thomas Hospitals Foundation, NHS Trust, London, UK
Aliment Pharmacol Ther 28:973-83. 2008..To investigate whether pharmacogenetic loci or metabolite concentrations explain clinical response or side effects to AZA...
- Duplex pyrosequencing of the TPMT*3C and TPMT*6 alleles in Korean and Vietnamese populationsSang Seop Lee
Department of Pharmacology and PharmacoGenomics Research Center, Inje University College of Medicine, 633 165 Gaegum Dong, Jin gu, Busan 614 735, Republic of Korea
Clin Chim Acta 398:82-5. 2008Thiopurine S-methyltransferase (TPMT) genetic polymorphisms have been studied intensively in relation to thiopurine toxicity...
- Thiopurine S-methyltransferase (TPMT) gene polymorphism in Brazilian children with acute lymphoblastic leukemia: association with clinical and laboratory dataMarcilene Rezende Silva
Department of Paediatrics, Federal University of Minas Gerais, Belo Horizonte, Minas Gerais, Brazil
Ther Drug Monit 30:700-4. 2008The frequency of allele variants of gene TPMT*2, *3A, *3B, and *3C was estimated in a population of 116 Brazilian children with acute lymphoblastic leukemia...
- Thiopurine S-methyltransferase genotype-phenotype concordance: used as a quality assurance tool to help control the phenotype assayLoretta Ford
Department of Clinical Biochemistry, City Hospital, Birmingham, UK
Ann Clin Biochem 46:152-4. 2009As part of the quality control system for our TPMT phenotyping service we monitor the genotype-phenotype concordance for patient samples with deficient and low TPMT activity...
- Thiopurine S-methyltransferase and inosine triphosphate pyrophosphohydrolase genes in Japanese patients with inflammatory bowel disease in whom adverse drug reactions were induced by azathioprine/6-mercaptopurine treatmentKan Uchiyama
Division of Gastroenterology and Hepatology, Department of Internal Medicine, The Jikei University School of Medicine Kashiwa Hospital, 163 1 Kashiwa shita, Kashiwa, Chiba, 277 8567, Japan
J Gastroenterol 44:197-203. 2009..adverse reactions is a reduction in the activities of the metabolizing enzymes thiopurine S-methyltransferase (TPMT) and inosine triphosphate pyrophosphohydrolase (ITPA)...
- [Thiopurine S-methyltransferase gene polymorphism in Chilean blood donors]Luis Alvarez L
Sección de Gastroenterología, Departamento de Medicina Interna, Hospital Clinico Universidad de Chile
Rev Med Chil 137:185-92. 2009Thiopurine S-methyltransferase (TPMT) is a cytosolic enzyme that catalyzes the S-methylation of 6-mercaptopurine and azathioprine. Low-activity phenotypes are correlated with polymorphism in the TPMT gene...
- Adverse reactions to azathioprine cannot be predicted by thiopurine S-methyltransferase genotype in Japanese patients with inflammatory bowel diseaseNoritaka Takatsu
Department of Gastroenterology, Fukuoka University Chikushi Hospital, Fukuoka, Japan
J Gastroenterol Hepatol 24:1258-64. 2009..We examined polymorphism of the thiopurine S-methyltransferase (TPMT) gene to determine whether the TPMT genotype would be a predictive marker for the development of adverse reactions ..
- Thiopurine S-methyltransferase gene polymorphism and 6-mercaptopurine dose intensity in Indian children with acute lymphoblastic leukemiaGauri Kapoor
Department of Pediatric Hematology and Oncology, Rajiv Gandhi Cancer Institute and Research Centre, Sector 5, Rohini, Delhi 110085, India gauri
Leuk Res 34:1023-6. 2010The prevalence of thiopurine S-methyltransferase (TPMT) polymorphism and its association with clinical and hematological toxicities was retrospectively analyzed in 71 Indian children with acute lymphoblastic leukemia (ALL)...
- Influences of thiopurine methyltransferase genotype and activity on thiopurine-induced leukopenia in Korean patients with inflammatory bowel disease: a retrospective cohort studyJae Hak Kim
Department of Internal Medicine, Dongguk University College of Medicine, Goyang si, Korea
J Clin Gastroenterol 44:e242-8. 2010..The purpose of this study was to investigate the relative risk of the thiopurine methyltransferase (TPMT) and inosine triphosphate pyrophosphatase (ITPA) genotypes and TPMT activity for the development of leukopenia in ..
- Thiopurine S-methyltransferase polymorphisms and thiopurine toxicity in treatment of inflammatory bowel diseaseXian Wen Dong
Department of Gastroenterology, Renji Hospital, Shanghai Institute of Digestive Disease, Shanghai Jiao Tong University, School of Medicine, Shanghai 200001, China
World J Gastroenterol 16:3187-95. 2010To evaluate the relationship between thiopurine S-methyltransferase (TPMT) polymorphisms and thiopurine-induced adverse drug reactions (ADRs) in inflammatory bowel disease (IBD).
- Thiopurine methyltransferase genotype-phenotype discordance and thiopurine active metabolite formation in childhood acute lymphoblastic leukaemiaLynne Lennard
Clinical Pharmacology Unit, Department of Human Metabolism, University of Sheffield, Sheffield, UK
Br J Clin Pharmacol 76:125-36. 2013..marrow activity can influence red blood cell (RBC) kinetics, the surrogate tissue for thiopurine methyltransferase (TPMT) measurements...
- Thiopurine-methyltransferase variants in inflammatory bowel disease: prevalence and toxicity in Brazilian patientsAna Teresa P Carvalho
Ana Teresa P Carvalho, Barbara C Esberard, Renata S B Fróes, Ana B Grinman, Disciplina de Gastroenterologia e Endoscopia Digestiva, Universidade do Estado do Rio de Janeiro, Rio de Janeiro, RJ 20551 900, Brazil
World J Gastroenterol 20:3327-34. 2014To analyze the prevalence of thiopurine-methyltransferase (TPMT) genotypes and their association with drug toxicity in inflammatory bowel disease (IBD) patients from southeastern Brazil.
- Thiopurine S-methyltransferase deficiency: two nucleotide transitions define the most prevalent mutant allele associated with loss of catalytic activity in CaucasiansH L Tai
Department of Pharmaceutical Sciences, St Jude Children s Research Hospital, Memphis, TN 38105, USA
Am J Hum Genet 58:694-702. 1996The autosomal recessive trait of thiopurine S-methytransferase (TPMT) deficiency is associated with severe hematopoietic toxicity when patients are treated with standard doses of mercaptopurine, azathioprine, or thioguanine...
- Frequencies of thiopurine S-methyltransferase mutant alleles (TPMT*2, *3A, *3B and *3C) in 151 healthy Japanese subjects and the inheritance of TPMT*3C in the family of a propositusT Kubota
Research Testing Department, SRL, Inc, Hachioji shi, Tokyo, Japan
Br J Clin Pharmacol 51:475-7. 2001To determine the frequencies of four thiopurine S-methyltransferase (TPMT) mutant alleles, TPMT*2, *3A, *3B and *3C in a normal Japanese population.
- Thiopurine S-methyltransferase polymorphisms and the relationship between the mutant alleles and the adverse effects in systemic lupus erythematosus patients taking azathioprineJ B Jun
The Hospital for Rheumatic Diseases, Hanyang University, Seoul, Korea
Clin Exp Rheumatol 23:873-6. 2005The present study sought to elucidate the genetic basis of thiopurine methyltransferase (TPMT) polymorphism and subsequently to investigate the relationship between mutant TPMT and an adverse response observed in Korean patients with ..
- Pharmacokinetics of 6-thioguanine in patients with inflammatory bowel diseaseLuc J J Derijks
Department of Clinical Pharmacy, Maxima Medical Center, Veldhoven, The Netherlands
Ther Drug Monit 28:45-50. 2006..measures included mean 6-TGN concentrations (+/-95% confidence interval [CI95%]) and their associations with TPMT genotype, 6-TG dose, and hematological, hepatic, pancreatic, and efficacy parameters during the 8 week period...
- Thiopurine methyltransferase gene polymorphisms in Chinese patients with inflammatory bowel diseaseQian Cao
Department of Gastroenterology, Sir Run Run Shaw Institute of Clinical Medicine, Sir Run Run Shaw Hospital, Zhejiang University School of Medicine, Hangzhou, China
Digestion 79:58-63. 2009..variability exists in the efficacy and toxicity of the drugs, and this results from thiopurine methyltransferase (TPMT) gene polymorphisms...
- Are patients with intermediate TPMT activity at increased risk of myelosuppression when taking thiopurine medications?Jenny E Higgs
Central Manchester and Manchester Children s University Hospitals NHS Trust, Manchester Royal Infirmary, Manchester, UK
Pharmacogenomics 11:177-88. 2010Thiopurine S-methyltransferase (TPMT) metabolizes thiopurine medications, including azathioprine and 6-mercaptopurine. Absent TPMT activity (i.e...
- The multidrug-resistance protein 4 polymorphism is a new factor accounting for thiopurine sensitivity in Japanese patients with inflammatory bowel diseaseHiromistu Ban
Department of Medicine, Shiga University of Medical Science, Seta Tukinowa, Otsu, Japan
J Gastroenterol 45:1014-21. 2010..In this study, we investigated the association between MRP4 G2269A polymorphism and thiopurine sensitivity in Japanese IBD patients...
- Adverse drug reactions to azathioprine therapy are associated with polymorphism in the gene encoding inosine triphosphate pyrophosphatase (ITPase)Anthony M Marinaki
Purine Research Laboratory, Department of Chemical Pathology and Department of Gastroenterology, Guy s and St Thomas Hospital, London, UK
Pharmacogenetics 14:181-7. 2004..6-MP), occur in 15% to 28% of patients and the majority are not explained by thiopurine methyltransferase (TPMT) deficiency...
- 5-aminosalicylate therapy is associated with higher 6-thioguanine levels in adults and children with inflammatory bowel disease in remission on 6-mercaptopurine or azathioprineScott Hande
Brigham and Women s Hospital, Boston, Massachusetts, USA
Inflamm Bowel Dis 12:251-7. 2006..azathioprine (AZA) or 6-mercaptopurine (6-MP), presumably through the inhibition of thiopurine methyltransferase (TPMT)...
- Thiopurine treatment in inflammatory bowel disease: clinical pharmacology and implication of pharmacogenetically guided dosingAlexander Teml
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Stuttgart, Germany
Clin Pharmacokinet 46:187-208. 2007..The catabolic enzyme thiopurine S-methyltransferase (TPMT) is polymorphically expressed, and currently 23 genetic variants have been described...
- Thiopurine methyltransferase activity combined with 6-thioguanine metabolite levels predicts clinical response to thiopurines in patients with inflammatory bowel diseaseL Y Kwan
Department of Medicine, Cedars Sinai Medical Center, Los Angeles, CA, USA
Dig Liver Dis 40:425-32. 2008..Our aim was to determine if thiopurine methyltransferase enzyme activity and 6-thioguanine nucleotide level monitoring would predict response to therapy with thiopurines in patients with inflammatory bowel disease...
- State-of-the-art: Immunosuppression and biologic therapyWilliam J Sandborn
Inflammatory Bowel Disease Clinic, Division of Gastroenterology and Hepatology, Mayo Clinic, Rochester, MN 55905, USA
Dig Dis 28:536-42. 2010..Clinical practice should change such that combination therapy with an anti-TNF agent and azathioprine replace azathioprine in patients failing first line therapy with mesalamine and/or steroids...
- Analytic aspects of monitoring therapy with thiopurine medicationsVictor W Armstrong
Department of Clinical Chemistry, George August University, D 37075 Goettingen, Germany
Ther Drug Monit 26:220-6. 2004..One person in 300 in white populations has low or undetectable TPMT activity and is at risk for accumulating 6-TGN with the consequence of severe, life-threatening myelosuppression...
- [Thiopurine methyltransferase activity and myelosuppression in inflammatory bowel disease patients treated with azathioprine and 6-mercaptopurine]Javier P Gisbert
Servicio de Aparato Digestivo Hospital Universitario de la Princesa Universidad Autónoma Madrid Spain
Med Clin (Barc) 121:1-5. 2003We aimed at assessing whether there exists a relationship between thiopurine methyltransferase (TPMT) activity and the incidence of adverse events, especially myelotoxicity, in patients with inflammatory bowel disease treated with ..
- Preponderance of thiopurine S-methyltransferase deficiency and heterozygosity among patients intolerant to mercaptopurine or azathioprineW E Evans
St Jude Children s Research Hospital and University of Tennessee, Memphis 38101 0318, USA
J Clin Oncol 19:2293-301. 2001To assess thiopurine S-methyltransferase (TPMT) phenotype and genotype in patients who were intolerant to treatment with mercaptopurine (MP) or azathioprine (AZA), and to evaluate their clinical management.
- Genotypic analysis of thiopurine S-methyltransferase in patients with Crohn's disease and severe myelosuppression during azathioprine therapyJ F Colombel
Service d Hepato Gastroenterologie, Hopital Huriez, CHRU Lille, France
Gastroenterology 118:1025-30. 2000..disease (CD) treated with azathioprine has been attributed to low activity of thiopurine S-methyltransferase (TPMT). Allelic variants of the TPMT gene responsible for changes in the enzyme activity have been characterized...
- Genetic polymorphism of inosine-triphosphate-pyrophosphatase influences mercaptopurine metabolism and toxicity during treatment of acute lymphoblastic leukemia individualized for thiopurine-S-methyl-transferase statusGabriele Stocco
St Jude Children s Research Hospital, Department of Pharmaceutical Sciences, 262 Danny Thomas Place MS 272, Memphis, TN 38105, USA
Expert Opin Drug Saf 9:23-37. 2010Although genetic polymorphisms in the gene encoding human thiopurine methyltransferase (TPMT) are known to have a marked effect on mercaptopurine metabolism and toxicity, there are many patients with wild-type TPMT who develop toxicity...
- 6-thioguanine nucleotide-adapted azathioprine therapy does not lead to higher remission rates than standard therapy in chronic active crohn disease: results from a randomized, controlled, open trialMax Reinshagen
Department of Medicine I, Klinikum Braunschweig, Braunschweig, Germany
Clin Chem 53:1306-14. 2007..A prospective randomized trial in patients with Crohn disease studied whether 6-thioguanine nucleotide (6-TGN) concentration-adapted azathioprine (AZA) therapy is clinically superior to a standard dose of 2.5 mg/kg/day AZA...
- Thiopurine S- methyltransferase [corrected] testing in idiopathic pulmonary fibrosis: a pharmacogenetic cost-effectiveness analysisJared T Hagaman
Department of Internal Medicine, Division of Pulmonary, Critical Care and Sleep Medicine, University of Cincinnati, 231 Albert Sabin Way ML 0564, Cincinnati, OH 45267, USA
Lung 188:125-32. 2010..A genotypic assay, thiopurine S-methyltransferase (TPMT), has been developed that can potentially identify those at risk for developing leukopenia with azathioprine, and ..
- Azathioprine dosed by thiopurine methyltransferase activity for moderate-to-severe atopic eczema: a double-blind, randomised controlled trialSimon J Meggitt
School of Clinical and Laboratory Sciences Dermatological Sciences, University of Newcastle upon Tyne, UK
Lancet 367:839-46. 2006..for moderate-to-severe atopic eczema, and the therapeutic importance of the thiopurine methyltransferase (TPMT) polymorphism (a key determinant of azathioprine-induced myelotoxicity) by using TPMT enzyme activity to establish ..
- Impact of thiopurine methyltransferase activity and 6-thioguanine nucleotide concentrations in patients with chronic inflammatory diseasesJörg Schedel
Department of Internal Medicine I, Division of Rheumatology and Clinical Immunology, University Hospital of Regensburg, D 93042 Regensburg, Germany
Ann N Y Acad Sci 1069:477-91. 2006..chronic inflammatory diseases, the effect of the azathioprine metabolizing enzyme thiopurine methyltransferase (TPMT) activity on incidence of adverse events (AE) was examined...
- Pharmacological monitoring of azathioprine therapyL O Reuther
Dept of Clinical Pharmacology, Gentofte University Hospital, Hellerup, Denmark
Scand J Gastroenterol 38:972-7. 2003..Thiopurine methyltransferase (TPMT) is responsible for the formation of methylated metabolites and lower E-TGN levels, and TPMT genotyping has been ..
- 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 activityXavier Roblin
Department of Gastroenterology, CHU Grenoble, Grenoble, France
Am J Gastroenterol 103:3115-22. 2008..We investigated the threshold value of 6-TGN that may be predictive of AZA refractoriness and its impact on safety profile...
- Monitoring of thiopurine methyltransferase activity in postsurgical patients with Crohn's disease during 1 year of treatment with azathioprine or mesalazineKarin Dilger
Dr Falk Pharma GmbH, Freiburg, Germany
Ther Drug Monit 29:1-5. 2007Thiopurine methyltransferase (TPMT) activity determines biotransformation of azathioprine and, thereby, drug efficacy and safety...
- Pharmacogenetics during standardised initiation of thiopurine treatment in inflammatory bowel diseaseU Hindorf
Department of Clinical Sciences, Division of Gastroenterology, Faculty of Medicine, Lund University, 22185 Lund, Sweden
Gut 55:1423-31. 2006Firm recommendations about the way thiopurine drugs are introduced and the use of thiopurine methyltransferase (TPMT) and metabolite measurements during treatment in inflammatory bowel disease (IBD) are lacking.
- Current use of pharmacogenetic testing: a national survey of thiopurine methyltransferase testing prior to azathioprine prescriptionE A Fargher
North West Genetics Knowledge Park Nowgen, Manchester, UK
J Clin Pharm Ther 32:187-95. 2007..Thiopurine methyltransferase (TPMT) is a genetically moderated key enzyme involved in the metabolism of AZA that can be used to stratify individuals ..
- High 6-thioguanine nucleotide levels and low thiopurine methyltransferase activity in patients with lupus erythematosus treated with azathioprineG Decaux
General Internal Medicine Department, University Hospital Erasme, Brussels, Belgium
Am J Ther 8:147-50. 2001..The 6-TGN levels are known to be affected by the activity of the key enzyme, thiopurine methyltransferase (TPMT), which is under genetic dependence...
- [Thiopurine methyltransferase activity in patients with autoimmune hepatitis]Javier P Gisbert
Servicio de Gastroenterología y Hepatología Hospital Universitario de la Princesa Universidad Autónoma Madrid Spain
Med Clin (Barc) 121:481-4. 2003The measurement of the activity of thiopurine methyltransferase (TPMT) is useful to monitor, on an individual basis, the dose of azathioprine in order to identify patients at risk of myelotoxicity...
- TPMT*26 (208F-->L), a novel mutation detected in a ChineseShirley Kow Yin Kham
Department of Paediatrics, Division of Haematology and Oncology, Yong Loo Lin School of Medicine, National University Health System, National University Hospital, 5 Lower Kent Ridge Road, Singapore
Br J Clin Pharmacol 68:120-3. 2009..These manifestations may be attributed to polymorphisms or mutations in the thiopurine methyltransferase (TPMT) gene that might result in low TPMT enzyme activity...
- IMPDH activity in thiopurine-treated patients with inflammatory bowel disease - relation to TPMT activity and metabolite concentrationsSofie Haglund
Research and Development in Laboratory Medicine, Laboratory Medicine, Ryhov Hospital, Linkoping, Sweden
Br J Clin Pharmacol 65:69-77. 2008..The polymorphic enzyme thiopurine S-methyltransferase (TPMT) is of importance for thiopurine metabolism and occurrence of adverse events...
- Long-term results of TPMT activity monitoring in azathioprine-treated renal allograft recipientsE Thervet
Service de Nephrologie, Hopital Saint Louis, Paris, France
J Am Soc Nephrol 12:170-6. 2001Thiopurine methyltransferase (TPMT) is implicated in the metabolism of azathioprine. The consequences of differential TPMT activity induction by azathioprine on the long-term results after renal transplantation were investigated...
- Pancytopenia due to high 6-methylmercaptopurine levels in a 6-mercaptopurine treated patient with Crohn's diseaseL P L Gilissen
Department of Gastroenterology and Hepatology, University Hospital Maastricht azM, P Debyelaan 25, P O Box 5800, 6202 AZ Maastricht, The Netherlands
Dig Liver Dis 39:182-6. 2007..Genotyping showed a wildtype thiopurine S-methyltransferase TPMT(H/H) (*1/*1) genotype and a wildtype inosine triphosphate pyrophosphatase gene...
- An audit of thiopurine methyltransferase genotyping and phenotyping before intended azathioprine treatment for dermatological conditionsT Vestergaard
Department of Dermatology, Odense University Hospital, Odense, Denmark
Clin Exp Dermatol 35:140-4. 2010Determining thiopurine methyltransferase (TPMT) genotype and phenotype before azathioprine treatment predicts which patients are most likely to develop myelosuppression.
- Should azathioprine and 5-aminosalicylates be coprescribed in inflammatory bowel disease?: an audit of adverse events and outcomeJayshri A Shah
Bristol Royal Infirmary, Bristol, UK
Eur J Gastroenterol Hepatol 20:169-73. 2008..An interaction between azathioprine and 5-aminosalicylates may exist, but the mechanism remains unclear...
- Erythrocyte thiopurine methyl transferase assessment prior to azathioprine use in the UKS A Holme
Department of Dermatology, Royal Gwent Hospital, Newport, Purine Research Laboratory and Department of Gastroenterology, Guy s and St Thomas Hospitals Trust, London, UK
QJM 95:439-44. 2002Individuals with low activity of a key metabolic enzyme, thiopurine methyl transferase (TPMT), are more susceptible to azathioprine-induced myelosuppression.
- TPMT in the treatment of Crohn's disease with azathioprineL Lennard
Academic Unit of Molecular and Clinical Pharmacology, School of Medicine, University of Sheffield, UK
Gut 51:143-6. 2002Azathioprine induced profound myelosuppression linked to TPMT deficiency has now been documented in many patient groups, including those with Crohn's disease...
- Azathioprine as a treatment for severe atopic eczema in children with a partial thiopurine methyl transferase (TPMT) deficiencyLesley Ann Murphy
St Johns Institute of Dermatology, London, United Kingdom
Pediatr Dermatol 20:531-4. 2003Azathioprine is a valuable agent in the treatment of severe childhood atopic eczema. Thiopurine methyl transferase (TPMT) exhibits autosomal codominant polymorphism and plays an important role in the metabolism of azathioprine...
- Cost-effectiveness of thiopurine methyltransferase genotype screening in patients about to commence azathioprine therapy for treatment of inflammatory bowel diseaseJ Winter
Gastroenterology Unit, Gartnavel General Hospital, Glasgow, Scotland
Aliment Pharmacol Ther 20:593-9. 2004..Its use is limited by its side-effect profile. Marrow toxicity occurs in approximately 3.2% of patients and is known to be associated with diminished thiopurine methyltransferase enzyme activity resulting from genetic polymorphisms...
- Azathioprine for atopic dermatitisS J Meggitt
Department of Dermatology, University of Newcastle, Newcastle upon Tyne, UK
Clin Exp Dermatol 26:369-75. 2001..now known to be related to the activity of a key enzyme in azathioprine metabolism, thiopurinemethyltransferase (TPMT)...
- S-adenosylmethionine regulates thiopurine methyltransferase activity and decreases 6-mercaptopurine cytotoxicity in MOLT lymphoblastsMiha Milek
University of Ljubljana, Faculty of Pharmacy, Ljubljana, Slovenia
Biochem Pharmacol 77:1845-53. 2009..Side-effects of thiopurine therapy have been correlated with thiopurine methyltransferase (TPMT) activity...
- Mercaptopurine therapy intolerance and heterozygosity at the thiopurine S-methyltransferase gene locusM V Relling
Department of Pharmaceutical Sciences, St Jude Children s Research Hospital, Memphis, TN 38105, USA
J Natl Cancer Inst 91:2001-8. 1999..are often treated with 6-mercaptopurine, and those with homozygous deficiency in thiopurine S-methyltransferase (TPMT) enzyme activity have an extreme sensitivity to this drug as a result of the accumulation of higher cellular ..
- Increased concentrations of methylated 6-mercaptopurine metabolites and 6-thioguanine nucleotides in human leukemic cells in vitro by methotrexateT Giverhaug
Department of Pharmacology, Institute of Medical Biology, University of Tromsø, Norway
Biochem Pharmacol 55:1641-6. 1998..CCRF-CEM, WI-L2, TBJ, and HL-60 all expressed thiopurine methyltransferase (TPMT) activity...
- The use of denaturing high-pressure liquid chromatography for the detection of mutations in thiopurine methyltransferaseA G Hall
Leukaemia Research Fund Laboratory, University of Newcastle upon Tyne, Newcastle upon Tyne, UK
J Biochem Biophys Methods 47:65-71. 2001The level of expression of the enzyme thiopurine methyltransferase (TPMT) is an important determinant of the metabolism of drugs used both in the treatment of acute leukaemia (6-mercaptopurine and 6-thioguanine) and as an ..
- Intensification of mercaptopurine/methotrexate maintenance chemotherapy may increase the risk of relapse for some children with acute lymphoblastic leukemiaKjeld Schmiegelow
Department of Pediatrics, The University Hospital and The University of Copenhagen, Denmark
J Clin Oncol 21:1332-9. 2003..Methylated MP metabolites (formed by thiopurine methyltransferase [TPMT]) and methotrexate (MTX) polyglutamates can inhibit de novo purine synthesis...
- The pharmacokinetic effect of discontinuation of mesalazine on mercaptopurine metabolite levels in inflammatory bowel disease patientsL P L Gilissen
Department of Gastroenterology and Hepatology, University Hospital Maastricht, Maastricht, The Netherlands
Aliment Pharmacol Ther 22:605-11. 2005..studies suggest interactions between mesalazine (mesalamine) and thiopurines by thiopurine S-methyltransferase (TPMT) inhibition, influencing the balance of hepatotoxic 6-methylmercaptopurine ribonucleotide and immunosuppressive ..
- The effect of thiopurine drugs on DNA methylation in relation to TPMT expressionL A Hogarth
Leukaemia Research Group, Northern Institute for Cancer Research, Newcastle University, Newcastle upon Tyne NE2 4HH, UK
Biochem Pharmacol 76:1024-35. 2008..Thiopurine methyltransferase (TPMT) metabolises thiopurine drugs and influences their cytotoxic activity...
- 6-MP metabolite profiles provide a biochemical explanation for 6-MP resistance in patients with inflammatory bowel diseaseMarla C Dubinsky
Division of Gastroenterology and Genetics, Department of Medicine and Pediatrics, Cedars Sinai Medical Center, UCLA, Los Angeles, California 90048, USA
Gastroenterology 122:904-15. 2002..An inverse correlation between 6-TGN and thiopurine methyltransferase (TPMT) has been described...
- Thiopurine methyltransferase and 6-thioguanine nucleotide measurement: early experience of use in clinical practiceR B Gearry
Department of Medicine, Christchurch School of Medicine and Health Sciences, New Zealand
Intern Med J 35:580-5. 2005..Assessing thiopurine methyltransferase (TPMT) status has been recommended to reduce the risk of serious toxicity...
- The thiopurine methyltransferase genetic polymorphism is associated with thioguanine-related veno-occlusive disease of the liver in children with acute lymphoblastic leukemiaLynne Lennard
Academic Unit of Clinical Pharmacology, University of Sheffield, Sheffield, United Kingdom
Clin Pharmacol Ther 80:375-83. 2006..This trial compared the efficacy and toxicity of thioguanine (INN, thioguanine) versus mercaptopurine...
- Differential effects of targeted disruption of thiopurine methyltransferase on mercaptopurine and thioguanine pharmacodynamicsChristine Hartford
Department of Pharmaceutical Sciences, St Jude Children s Research Hospital, University of Tennessee, Memphis, Tennessee, USA
Cancer Res 67:4965-72. 2007The recessive deficiency in thiopurine methyltransferase (TPMT), caused by germ-line polymorphisms in TPMT, can cause severe toxicity after mercaptopurine...
- Determination of thiopurine methyltransferase phenotype in isolated human erythrocytes using a new simple nonradioactive HPLC methodDessislava Indjova
Department of Clinical Laboratory, Medical University Sofia, Sofia, Bulgaria
Ther Drug Monit 25:637-44. 2003Genetic polymorphism of the S-methylation pathway catalyzed by thiopurine methyltransferase (TPMT) is responsible for variation in the metabolism, toxicity, and therapeutic efficacy of thiopurine drugs...
- Methylated metabolites of 6-mercaptopurine are associated with hepatotoxicityUlrikka Nygaard
The Pediatric Clinic II, The University Hospital of Copenhagen, Rigshospitalet, Copenhagen, Denmark
Clin Pharmacol Ther 75:274-81. 2004....
- [Monitoring of thiopurine methyltransferase and thiopurine metabolites to optimize azathioprine therapy in inflammatory bowel disease]Javier P Gisbert
Servicio de Aparato Digestivo Hospital Universitario de La Princesa Universidad Autónoma Madrid España
Gastroenterol Hepatol 29:568-83. 2006Determination of the activity of thiopurine methyltransferase (TPMT) and of thiopurine metabolites (6-thioguanine and 6-methylmercaptopurine nucleotides) could be useful for individualized monitoring of azathioprine (AZA) and 6-..
- Relationship between 6-mercaptopurine dose and 6-thioguanine nucleotide levels in patients with inflammatory bowel diseaseAhmed Morales
Department of Medicine, University of Pennsylvania, Philadelphia, PA 19104 6021, USA
Inflamm Bowel Dis 13:380-5. 2007..However, many physicians prescribe AZA/6MP using milligrams per kilogram (mg/kg) dosing regimens without measuring 6-TGN levels. The aim of this study was to examine the association between 6MP dose and 6-TGN levels...
- Methotrexate increases red blood cell concentrations of 6-methylmercaptopurine ribonucleotide in rats in vivoT Giverhaug
Department of Pharmacology, University of Tromsø, Norway
Cancer Chemother Pharmacol 40:367-70. 1997..To elucidate the effect of methotrexate (MTX) on 6-mercaptopurine (6-MP) metabolism in rats...
- Analysis of thiopurine methyltransferase variant alleles in childhood acute lymphoblastic leukaemiaH L McLeod
Department of Medicine and Therapeutics, Institute of Medical Sciences, University of Aberdeen, Foresterhill, Aberdeen
Br J Haematol 105:696-700. 1999..efficacy of 6MP is significantly influenced by inactivation by the polymorphic enzyme thiopurine methyltransferase (TPMT). In the general population 89-94% have high TPMT activity, 6-11% have intermediate activity, and approximately 0...
- Thiopurine methyltransferase pharmacogenetics. Cloning of human liver cDNA and a processed pseudogene on human chromosome 18q21.1D Lee
Department of Pharmacology, Mayo Medical School, Rochester, MN 55905 0001, USA
Drug Metab Dispos 23:398-405. 1995Thiopurine methyltransferase (TPMT) is a genetically polymorphic enzyme that catalyzes the S-methylation of thiopurine drugs such as 6-mercaptopurine...
- A single point mutation leading to loss of catalytic activity in human thiopurine S-methyltransferaseE Y Krynetski
Pharmaceutical Department, St Jude Children s Research Hospital, Memphis, TN 38105
Proc Natl Acad Sci U S A 92:949-53. 1995Thiopurine S-methyltransferase (TPMT; S-adenosyl-L-methionine:thiopurine S-methyltransferase, EC 22.214.171.124) activity exhibits genetic polymorphism, with approximately 0...
- Is 6-thioguanine more appropriate than 6-mercaptopurine for children with acute lymphoblastic leukaemia?L Lennard
University of Sheffield Department of Medicine, Royal Hallamshire Hospital, UK
Br J Cancer 68:186-90. 1993The cytotoxic activity of 6-mercaptopurine (6-MP) is affected by thiopurine methyltransferase (TPMT), a genetically regulated and variable intracellular enzyme...
- Human thiopurine methyltransferase: no evidence of activation by its substratesI Stupans
Centre for Pharmaceutical Research, School of Pharmacy and Medical Sciences, University of South Australia, Adelaide
Life Sci 62:343-50. 1998..The effects of 6-thioguanine on 6-mercaptopurine metabolism were determined. 6-Thioguanine was found to be a mixed inhibitor of 6-mercaptopurine methylation...
- Cefazolin administration and 2-methyl-1,3,4-thiadiazole-5-thiol in human tissue: possible relationship to hypoprothrombinemiaThomas C Wood
Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Medical School, Mayo Clinic, Mayo Foundation, Rochester, Minnesota 55905, USA
Drug Metab Dispos 30:1123-8. 2002..S-methylation catalyzed by the genetically polymorphic drug-metabolizing enzyme thiopurine S-methyltransferase (TPMT). Initially, we tested recombinant human TPMT as a "reagent" to S-methylate MTD...
- Thiopurine S-methyltransferase (TPMT) genotype does not predict adverse drug reactions to thiopurine drugs in patients with inflammatory bowel diseaseR B Gearry
Department of Gastroenterology, Christchurch Hospital, Christchurch, New Zealand
Aliment Pharmacol Ther 18:395-400. 2003..The likelihood and type of adverse effect may relate to thiopurine methyltransferase (TPMT) enzyme activity and genotype.
- Thiopurine methyltransferase deficiency and azathioprine intolerance in autoimmune hepatitisAlbert J Czaja
Division of Gastroenterology and Hepatology, Mayo Clinic College of Medicine, Rochester, Minnesota 55905, USA
Dig Dis Sci 51:968-75. 2006..We conclude that routine screening of blood thiopurine methyltransferase levels has a low yield for identifying individual patients at risk for azathioprine toxicity during conventional low dose therapy for autoimmune hepatitis...
- Pharmacogenomics: catechol O-methyltransferase to thiopurine S-methyltransferaseRichard M Weinshilboum
Division of Clinical Pharmacology, Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic College of Medicine, Mayo Clinic, Rochester, Minnesota 55905, USA
Cell Mol Neurobiol 26:539-61. 2006..2. The thiopurine S-methyltransferase (TPMT) genetic polymorphism represents one of the best characterized and most clinically relevant examples of ..
- Pharmacogenomics of drug-metabolizing enzymes and drug transporters in chemotherapyTessa M Bosch
Clinical Pharmacy and Toxicology, Medical Center Rijnmond Zuid, Rotterdam, The Netherlands
Methods Mol Biol 448:63-76. 2008..examples to demonstrate the influence of pharmacogenomics on anticancer therapy are thiopurine methyltransferase (TPMT), UGT (uridine diphosphate glucuronosyltransferase) 1A1*28, and DPD (dihydropyrimidine dehydrogenase) *2A, ..
- Thiopurine S-methyltransferase genotypic analysis in autoimmune bullous diseasesMaud Bezier
Department of Dermatology, Hopital Robert Debre, Centre Hospitalier de Reims, avenue du Général Koenig, 51092 Reims Cedex, France
Eur J Dermatol 18:512-7. 2008Thiopurine S-methyltransferase (TPMT) activity is inversely related to the risk of developing severe hematopoietic toxicity in patients treated with azathioprine...
- Molecular dynamics simulation of a human thiopurine S-methyltransferase complexed with 6-mercaptopurine modelWanwimon Mokmak
National Center for Genetic Engineering and Biotechnology, National Science and Technology Development Agency, 113 Thailand Science Park, Phahonyothin Road, Klong 1, Klongluang, Pathumthani 12120, Thailand
Bioinformation 4:59-62. 2009Human thiopurine S-methyltransferase (TPMT) is an essential protein in 6-mercaptopurine (6MP) drug metabolism...
- Functional analysis of the role of the TPMT gene promoter VNTR polymorphism in TPMT gene transcriptionBranka Zukic
Institute for Molecular Genetics and Genetic Engineering, Laboratory of Molecular Hematology, Vojvode Stepe 444a, 11010 Belgrade, Serbia
Pharmacogenomics 11:547-57. 2010Thiopurine S-methyltransferase (TPMT) activity is polymorphic, and a trimodal distribution has been demonstrated in Caucasians (low, intermediate and high methylator groups)...
- Monitoring of azathioprine metabolites in pediatric patients with autoimmune hepatitisThi Mai Hoang Nguyen
Universite de Lyon, Département de Pharmacie Clinique, de Pharmacocinétique et d Evaluation du Médicament, Lyon, France
Ther Drug Monit 32:433-7. 2010..6-Thioguanine nucleotides (6-TGN) and 6-methyl mercaptopurine nucleotides (6-MeMPN) concentrations and TPMT activity were determined by high-performance liquid chromatography...
- Characterization of a novel sequence variant, TPMT*28, in the human thiopurine methyltransferase geneMalin Lindqvist Appell
Department of Medical and Health Sciences, Faculty of Health Sciences, Linkoping University, Linkoping, Sweden
Pharmacogenet Genomics 20:700-7. 2010The activity of the human enzyme thiopurine methyltransferase (TPMT) varies greatly between individuals because of genetic polymorphism...
- Multi-site Trial of Azathioprine Dosing in Crohn DiseaseStephen Hanauer; Fiscal Year: 2003..In a competing enzymatic pathway, thiopurine methyltransferase (TPMT) catalyzes formation of 6-methyl-mercaptopurine ribonucleotides (6-MMPR), metabolites that are therapeutically ..
- Multi-site Trial of Azathioprine Dosing in Crohn DiseaseStephen Hanauer; Fiscal Year: 2004..In a competing enzymatic pathway, thiopurine methyltransferase (TPMT) catalyzes formation of 6-methyl-mercaptopurine ribonucleotides (6-MMPR), metabolites that are therapeutically ..
- Ethnic Differences in Survival after Childhood ALLSmita Bhatia; Fiscal Year: 2009..We will control for polymorphisms in TPMT, and other genetic polymorphisms (in transporters, repair enzymes, HPRT, etc...
- LC-ELECTROSPRAY QUADRUPOLE ION TRAP MASS SPECTROMETERDominic Desiderio; Fiscal Year: 2000..wild-type and mutant forms of thiopurine methyltransferase (for the investigation of the genetic polymorphism of TPMT); and (lii) mismatch repair proteins (in the study of their involvement in the determination of thiopurine ..
- Drug Metabolism, DNA Repair & Second CancersDebra Friedman; Fiscal Year: 2003..The findings of this research can be applied to the development of preventive strategies of second malignant neoplasms and other adverse long-term health-related outcomes for cancer survivors. ..
- SULFATE CONJUGATION AND DRUG METABOLISMRichard Weinshilboum; Fiscal Year: 2007....
- Anticancer Agent Pharmacodynamics in Acute LeukemiaMary Relling; Fiscal Year: 2006..We have also identified a clinical genetic host factor, low thiopurine methyltransferase (TPMT) activity, that predisposed patients treated with thiopurines and etoposide to development of topoisomerase II ..
- The Natural History of Pediatric Crohn's DiseaseMarla Dubinsky; Fiscal Year: 2008..abstract_text> ..
- Parental Expression of Immune Responses In Pediatric Crohn's DiseaseMarla Dubinsky; Fiscal Year: 2008..unreadable] [unreadable]..
- Metabolism and Pharmacogenetics in MDMA-Induced ToxicityRafael de la Torre; Fiscal Year: 2009..A study will compare MDMA toxicity when co-adminsitered with the MRP1 inhibitor probenecid. ..