Different hydrolases involved in bioactivation of prodrug - type angiotensin receptor
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چکیده
242 words Introduction: 491 words Discussion: 1168 words Abbreviations: ARB, angiotensin receptor blocker; AM, azilsartan medoxomil; BNPP, bis-p-nitrophenylphosphate; CC, candesartan cilexetil; CES, carboxylesterase; CMBL, carboxymethylenebutenolidase homolog; Km, Michaelis constant; LC-MS/MS, liquid chromatography with tandem mass spectrometry; OM, olmesartan medoxomil; S9, This article has not been copyedited and formatted. The final version may differ from this version. DMD Fast Forward. Published on August 14, 2013 as DOI: 10.1124/dmd.113.053595 at A PE T Jornals on A ril 9, 2017 dm d.aspurnals.org D ow nladed from
منابع مشابه
Different hydrolases involved in bioactivation of prodrug-type angiotensin receptor blockers: carboxymethylenebutenolidase and carboxylesterase 1.
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 i...
متن کاملInterindividual variability of carboxymethylenebutenolidase homolog, a novel olmesartan medoxomil hydrolase, in the human liver and intestine.
Olmesartan medoxomil (OM) is a prodrug-type angiotensin II type 1 receptor antagonist. OM is rapidly converted into its active metabolite olmesartan by multiple hydrolases in humans, and we recently identified carboxymethylenebutenolidase homolog (CMBL) as one of the OM bioactivating hydrolases. In the present study, we further investigated the interindividual variability of mRNA and protein ex...
متن کاملDmd051482 1156..1162
Olmesartan medoxomil (OM) is a prodrug-type angiotensin II type 1 receptor antagonist. OM is rapidly converted into its active metabolite olmesartan by multiple hydrolases in humans, and we recently identified carboxymethylenebutenolidase homolog (CMBL) as one of the OM bioactivating hydrolases. In the present study, we further investigated the interindividual variability of mRNA and protein ex...
متن کاملHuman Carboxymethylenebutenolidase as a Bioactivating Hydrolase of Olmesartan Medoxomil in Liver and Intestine
Olmesartan medoxomil (OM) is a prodrug type angiotensin II type 1 receptor antagonist widely prescribed as an antihypertensive agent. Herein, we describe the identification and characterization of the OM bioactivating enzyme that hydrolyzes the prodrug and converts to its pharmacologically active metabolite olmesartan in human liver and intestine. The protein was purified from human liver cytos...
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Objective(s): Stress alters sensory and cognitive function in humans and animals. Angiotensin (AT) receptors have demonstrated well-established interactions in sets of physiological phenomena. AT1 receptors can play a part in stress-induced activation of hypothalamic-pituitary-adrenal (HPA) axis; besides angiotensinergic neurotransmission plays a pivotal role in stress-evoked physiological resp...
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تاریخ انتشار 2013