Preliminary communicationEnzymatic thiolysis of azathioprine
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Pharmacogenomics in gastroenterology
2023, Pharmacogenomics: from Discovery to Clinical ImplementationDrug Metabolism: Phase II Enzymes
2022, Comprehensive PharmacologyThe 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 :Indeed, as patients with higher GSTs activity have an increased metabolic activity during the treatment with AZA, the metabolites induced leucopenia are accrescence. Since AZA are mainly metalized by multiple GST (4,23–25), including GTSM1, GSTT1, GSTP1 and GSTA1, we hypothesized that the four genetic polymorphisms of might lead to increased ADR to AZA therapy in IBD patients. This investigation shows that there is a significant association between GSTP1, GSTM1 wild genotype and AZA–related leucopenia.
Glutathione transferases in the bioactivation of azathioprine
2014, Advances in Cancer ResearchCitation Excerpt :The pharmacological action of azathioprine is based on the release of 6-MP effected by the chemical elimination of the imidazole moiety. Glutathione is the most abundant low-molecular-mass thiol in the cell (Josephy & Mannervik, 2006), and the thiolysis of azathioprine by glutathione has been established as the pivotal biotransformation in crude liver preparations (Kaplowitz, 1976). Although the original work suggested the involvement of GST activity, it was not until studies involving purified enzymes were performed that the overwhelming contribution of the enzymatic reaction was established (Eklund et al., 2006).
Hepatotoxicity of immunosuppressive drugs
2013, Drug-Induced Liver DiseaseStructural Determinants of Glutathione Transferases with Azathioprine Activity Identified by DNA Shuffling of Alpha Class Members
2008, Journal of Molecular Biology