EC Number   |
Application |
Reference |
|---|
   2.1.1.9 | medicine |
clopidogrel, a thienopyridine antiplatelet prodrug, is metabolized by oxidation to 2-oxo-clopidogrel, followed by conversion to its pharmacologically active thiol metabolite. In liver microsomes, thiol isomers H3 and H4 are further S-methylated, and the S-methylation is inhibited by 2,3-dichloromethyl benzylamine, indicating the involvement of thiol S-methyltransferase. The intrinsic clearance value for the S-methylation of H3 in microsomes is 98.1fold higher than that for H4. The stereoselective formation of H3 from 2-oxo-clopidogrel and the stereoselective S-methylation of H3 may lead to the similar exposure levels of H3 and H4 previously reported in humans |
733711 |
| 2.1.1.9 | medicine |
enzyme activity in cholestatic liver |
441356 |
| 2.1.1.9 | medicine |
enzyme activity in inflammatory bowel disease |
441596 |
| 2.1.1.9 | medicine |
in some patients with type 2 diabetes mellitus who are treated with 11beta-hydroxysteroid dehydrogenase inhibitor BI 187004, the plasma exposure of N-methylbenzimidazole metabolite 1-(1-methyl-1H-benzimidazole-5-carbonyl)-1,2,3,4,5,5a,10,10a-octahydroindeno[2,1-b]azepine-7-carbonitrile is 7fold higher than in the other patients. Thiol S-transferase catalyzes the formation of the metabolite |
756561 |
| 2.1.1.9 | more |
a few changes in key residues are sufficient to convert an OMT into a S-methyltransferase |
676510 |
