International Journal of Immunopharmacology
Serum azathioprine and 6-mercaptopurine levels and immunosuppressive activity after azathioprine in uremic patients
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The impact of glutathione S-transferase genotype and phenotype on the adverse drug reactions to azathioprine in patients with inflammatory bowel diseases
2015, Journal of Pharmacological SciencesCitation Excerpt :After oral application of AZA, very little it is detectable in patient plasma (26–28). Similar observations have been reported in mice (29) and the rhesus monkey (30). It was that indicated erythrocytes play a major role in this step in vivo.
Glutathione transferases in the bioactivation of azathioprine
2014, Advances in Cancer ResearchCitation Excerpt :The steady-state kinetic parameters were determined and were similar for all except A2*E, which had three- to fourfold higher kcat and kcat/KM values (Zhang et al., 2010). Assuming in vivo azathioprine concentrations < 10 μM (Odlind et al., 1986) and KM values > 1 mM, the data indicated that the activation rate under physiological conditions is proportional to kcat/KM. Variant A2*E turned out to catalyze this reaction three- to fourfold faster than the other variants of A2-2 and about sixfold faster than GSTs A1-1 and M1-1.
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