Methylation of 6-mercaptopurine and 6-thioguanine by thiopurine S-methyltransferase A comparison of activity in red blood cell samples of 199 blood donors: A …
T Kröplin, H Iven - European journal of clinical pharmacology, 2000 - Springer
T Kröplin, H Iven
European journal of clinical pharmacology, 2000•SpringerAbstract Objectives: To compare 6-mercaptopurine (6-MP) and 6-thioguanine (6-TG) as
substrates for the methylation reaction catalysed by the enzyme thiopurine S-
methyltransferase (TPMT). Methods: TPMT activity in haemolysed red blood cells of healthy
blood donors was determined twice, using the same experimental setting and equal molar
concentrations of 6-TG and 6-MP as substrates. After extraction, the reaction products 6-
methyl-TG and 6-methyl-MP were quantified using specific high-performance liquid …
substrates for the methylation reaction catalysed by the enzyme thiopurine S-
methyltransferase (TPMT). Methods: TPMT activity in haemolysed red blood cells of healthy
blood donors was determined twice, using the same experimental setting and equal molar
concentrations of 6-TG and 6-MP as substrates. After extraction, the reaction products 6-
methyl-TG and 6-methyl-MP were quantified using specific high-performance liquid …
Abstract
Objectives: To compare 6-mercaptopurine (6-MP) and 6-thioguanine (6-TG) as substrates for the methylation reaction catalysed by the enzyme thiopurine S-methyltransferase (TPMT).
Methods: TPMT activity in haemolysed red blood cells of healthy blood donors was determined twice, using the same experimental setting and equal molar concentrations of 6-TG and 6-MP as substrates. After extraction, the reaction products 6-methyl-TG and 6-methyl-MP were quantified using specific high-performance liquid chromatography procedures.
Results: The medians of the TPMT activities from 199 blood donors were 54.4 nmol 6-MTG g−1Hb h−1 when measured with 6-TG as the substrate and 35.8 nmol 6-MMP g−1 Hb h−1 when measured with 6-MP. The correlation coefficient for the 199 pairs of values was 0.8695. On average, TPMT activity was 34% lower with 6-MP as substrate than with 6-TG as substrate.
Springer
