Different hydrolases involved in bioactivation of prodrug-type angiotensin receptor blockers: carboxymethylenebutenolidase and carboxylesterase 1.

@article{Ishizuka2013DifferentHI,
  title={Different hydrolases involved in bioactivation of prodrug-type angiotensin receptor blockers: carboxymethylenebutenolidase and carboxylesterase 1.},
  author={Tomoko Ishizuka and Yasushi Yoshigae and Nobuyuki Murayama and Takashi Izumi},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2013},
  volume={41 11},
  pages={1888-95}
}
Olmesartan medoxomil (OM) is a prodrug-type angiotensin II type 1 receptor blocker (ARB). We recently identified carboxymethylenebutenolidase homolog (CMBL) as the responsible enzyme for OM bioactivation in humans. In the present study, we compared the bioactivating properties of OM with those of other prodrug-type ARBs, candesartan cilexetil (CC) and azilsartan medoxomil (AM), by focusing on interspecies differences and tissue specificity. In in-vitro experiments with pooled tissue subcellular… CONTINUE READING
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