Results 161 to 170 of about 15,347 (200)
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Journal of Huazhong University of Science and Technology [Medical Sciences], 2012
Carboxylesterases (CESs) play important roles in the metabolism of endogenous and foreign compounds in physiological and pharmacological responses. The aim of this study was to investigate the effect of dexamethasone at different doses on the expression of CES1 and CES2.
Chengliang, Zhang +5 more
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Carboxylesterases (CESs) play important roles in the metabolism of endogenous and foreign compounds in physiological and pharmacological responses. The aim of this study was to investigate the effect of dexamethasone at different doses on the expression of CES1 and CES2.
Chengliang, Zhang +5 more
openaire +2 more sources
Carboxylesterase 1 Polymorphism Impairs Oseltamivir Bioactivation in Humans
Clinical Pharmacology & Therapeutics, 2012Bioactivation of the antiviral agent oseltamivir to active oseltamivir carboxylate is catalyzed by carboxylesterase 1 (CES1). After the screening of 860 healthy Finnish volunteers for the CES1 c.428G>A (p.Gly143Glu, rs121912777) polymorphism, a pharmacokinetic study with 75 mg oseltamivir was carried out in c.428G>A carriers and noncarriers ...
Tarkiainen E. K. +9 more
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Involvement of Carboxylesterase 1 and 2 in the Hydrolysis of Mycophenolate Mofetil
Drug Metabolism and Disposition, 2010Mycophenolate mofetil (MMF) is the ester prodrug of the immunosuppressant agent mycophenolic acid (MPA) and is rapidly activated by esterases after oral administration. However, the role of isoenzymes in MMF hydrolysis remains unclear. Although human plasma, erythrocytes, and whole blood contain MMF hydrolytic activities, the mean half-lives of MMF in ...
Nobuhiro, Fujiyama +5 more
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Carboxylesterase 1 gene polymorphism and methylphenidate response in ADHD
Neuropharmacology, 2009Methylphenidate (MPH) is the most frequently prescribed drug in the treatment of attention deficit hyperactivity disorder (ADHD). Several pharmacogenetic studies suggested that catecholamine candidate genes influence individual MPH-responses, but these results are mostly contradictory.
Zsofia, Nemoda +4 more
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Inhibition of carboxylesterase-1 alters clopidogrel metabolism and disposition
Xenobiotica, 2019Clopidogrel is widely prescribed in patients with cardiovascular disease. Most research has focused on the role of hepatic CYP450 metabolism as the primary source of response variability despite 85-90% of clopidogrel being hydrolyzed by human carboxylesterase-1 (CES1).The purpose of this study is to determine the effects of the known CES1 inhibitor ...
S Casey, Laizure +3 more
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Carboxylesterase 1 (CES1) genetic polymorphisms and oseltamivir activation
European Journal of Clinical Pharmacology, 2012Carboxylesterase 1 (CES1) is the major hepatic hydrolytic enzyme responsible for the metabolism of many therapeutic agents, toxins, and endogenous compounds existing as esters, amides, thioesters, and carbamates. CES1 is coded by the CES1 gene in humans, which consists of three isoforms: CES1A1, CES1A2, and CES1A3.
Hao-Jie, Zhu, John S, Markowitz
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Xenobiotica, 2019
The carboxylesterase drug hydrolysis pathway has been used extensively to improve the oral availability of drugs under the assumption that the high capacity and low substrate specificity of hydrolytic enzymes would ensure rapid, complete, and consistent conversion of prodrugs to their active metabolite.
S Casey, Laizure, Robert B, Parker
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The carboxylesterase drug hydrolysis pathway has been used extensively to improve the oral availability of drugs under the assumption that the high capacity and low substrate specificity of hydrolytic enzymes would ensure rapid, complete, and consistent conversion of prodrugs to their active metabolite.
S Casey, Laizure, Robert B, Parker
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Predominant contributions of carboxylesterase 1 and 2 in hydrolysis of anordrin in humans
Xenobiotica, 20171. Anordrin (2α, 17α-diethynyl-A-nor-5α-androstane-2β, 17β-diol diproprionate) is post-coital contraceptive drug that is on the market in China for more than 30 years. This study aims to elucidate enzymes involved in anordrin hydrolysis, and to evaluate the significant role of carboxylesterases in anordrin hydrolysis in humans. 2.
Jinfang, Jiang +2 more
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Human carboxylesterase 1: from drug metabolism to drug discovery
Biochemical Society Transactions, 2003Human carboxylesterase 1 (hCE1) is a serine esterase involved in both drug metabolism and activation, as well as other biological processes. hCE1 catalyses the hydrolysis of heroin and cocaine, and the transesterification of cocaine in the presence of ethanol to the toxic metabolite cocaethylene.
M R, Redinbo, S, Bencharit, P M, Potter
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European Journal of Clinical Pharmacology, 2012
The aim of this study was to examine whether carboxylesterase 1 (CES1A) genetic polymorphisms affect the pharmacokinetics of oseltamivir.Thirty healthy Japanese male and female subjects ranging in age from 20 to 36 years voluntarily participated in this study.
Yuki, Suzaki +11 more
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The aim of this study was to examine whether carboxylesterase 1 (CES1A) genetic polymorphisms affect the pharmacokinetics of oseltamivir.Thirty healthy Japanese male and female subjects ranging in age from 20 to 36 years voluntarily participated in this study.
Yuki, Suzaki +11 more
openaire +2 more sources