Lars-Göran Mårtensson - Linköping University

Pharmacogenetic studies of thiopurines focus - AVHANDLINGAR.SE

Thiopurine methyltransferase (TPMT) is involved in the metabolism of mercaptopurine and subject to genetic polymorphism, with heterozygous individuals having intermediate and homozygous mutant individuals having very low TPMT activity. Thiopurine drugs are widely used in the treatment of acute lymphoblastic leukemia (ALL), autoimmune diseases, inflammatory bowel disease, and posttransplant organ rejection. The inactivation of thiopurine drugs is primarily catalyzed by an enzyme called thiopurine methyltransferase (TPMT). Thiopurine S-methyltransferase deficiency. Changes in the TPMT gene cause TPMT deficiency, which is a reduction in the activity of the TPMT enzyme. Without enough of this enzyme, the body cannot "turn off" thiopurine drugs by metabolizing them into inactive compounds.

Thiopurine methyltransferase

We explored the risk of second cancer in relation to protocols, risk group, thiopurine methyltransferase (TPMT) activity, ALL high hyperdiploidy (HeH), and t(12 Lars-Göran Mårtensson, Malin Lindqvist Appell (2020) Pharmacogenetic studies of thiopurine methyltransferase genotype-phenotype concordance and effect Clinical pharmacogenetics implementation consortium guidelines for thiopurine methyltransferase genotype and thiopurine dosing. Clin Pharmacol Ther 2011 Pharmacokinetics, dose adjustments, and 6-mercaptopurine/ methotrexate drug interactions in two patients with thiopurine methyltransferase deficiency. Lindqvist, Malin, 1976- (författare); Pharmacogenetic studies of thiopurines : focus on thiopurine methyltransferase / Malin Lindqvist. 2005; BokAvhandling.

Xanthine.

Akademiska laboratoriet

Journal The impact of thiopurine drugs on the natural history and surgical outcome of Characterisation and utility of thiopurine methyltransferase and thiopurine metabolite measurements in autoimmune hepatitis. J Hepatol. av P Malmborg · 2021 — metabolite testing and thiopurine methyltransferase determination in pediatric IBD. J Pediatr.

[The usefulness of pharmacogenetics for a more - PubMed

PLoS Current. 3:RRN12362011. View Article: Google Scholar. 17 Hindorf U and Appell ML: Genotyping should be considered the primary choice for pre-treatment evaluation of thiopurine methyltransferase function. Thiopurine S-methyltransferase deficiency.

2011 Mar; 89(3):387-391. 21270794 Thiopurine methyl transferase (TPMT) is a cytoplasmic transmethylase enzyme found in mammalian species. TPMT catalyzes the S-methylation of aromatics and heterocyclic sulfhydryl compounds, including medications, such as mercaptopurine, thioguanine, and azathioprine ( Elion, 1989 ).
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Clin Pharmacol Ther. 2011 Mar; 89(3):387-391. 21270794 Thiopurine S-methyltransferase (TPMT; S-adenosyl-L-methionine:thiopurine S-methyltransferase; EC 2.1.1.67) catalyzes the S-methylation of aromatic and heterocyclic sulfhydryl compounds, including the antineoplastic agents 6-mercaptopurine (6MP) and 6-thioguanine (6TG), and the immunosuppressant azathioprine (AZA) (Tai et al., 1996). Background and Aims.

From GHR Thiopurine S-methyltransferase (TPMT) deficiency is a condition characterized by significantly reduced activity of an enzyme that helps the body process drugs called thiopurines. These drugs, which include 6-thioguanine, 6-mercaptopurine, and … Catalyzes the S-methylation of thiopurine drugs such as 6-mercaptopurine (also called mercaptopurine, 6-MP or its brand name Purinethol) using S-adenosyl-L-methionine as the methyl donor (PubMed: 18484748 ). TPMT activity modulates the cytotoxic effects of thiopurine prodrugs.
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Pharmacogenetic studies of thiopurine methyltransferase

A thiopurine S-methyltransferase that is encoded in the genome of human. Protein Ontology Catalyzes the S-methylation of thiopurine drugs such as 6-mercaptopurine (also called mercaptopurine, 6-MP or its brand name Purinethol) and 6-thioguanine (also called tioguanine or 6-TG) using S-adenosyl-L-methionine as the methyl donor (PMID: 657528 , PMID: 18484748 ). Approximately 0.3% of the population has a profound genetic deficiency of thiopurine methyltransferase, the major route for detoxification of thiopurines used in immunosuppression and oncology. These patients develop severe marrow suppression if given usual doses of a thiopurine drug or prodrug. The mean thiopurine methyltransferase activity was 12.14 units in the sulfasalazine subgroup and 12.43 units in the mesalazine subgroup.

Thiopurinmetyltransferaspolymorfismer hos en brasiliansk

A gene called TPMT (thiopurine S-methyltransferase) is Describe how reduced function genetic variants in the enzyme, thiopurine methyltransferase (TPMT), result in increased toxicity of the drug, 6- mercaptopurine. And then through an enzyme called thiopurine methyl transferase or TPMT, is bio -inactivated. From the TIMP intermediate, you can either go through the TPMT These drugs are metabolized by the enzyme TPMT (thiopurine methyltransferase ).

6MP metabolites. 6-thioguanine nucleotides. HGPRT. Thiopurine methyltransferase. Xanthine. Characterisation and utility of thiopurine methyltransferase and thiopurine metabolite measurements in autoimmune hepatitis. Journal of Hepatology, Vol. 52, (1) DPSVGDRVIREAPCPVLVEVREGDAQGS >sp|Q9I011|TPMT_PSEAE Thiopurine S-methyltransferase OS=Pseudomonas aeruginosa (strain ATCC 15692 Assessment of thiopurine methyltransferase activity in patients prescribed azathioprine or other thiopurine-based drugs.