Results 211 to 220 of about 22,222 (249)

Carboxylesterase 1 (CES1) genetic polymorphisms and oseltamivir activation

European Journal of Clinical Pharmacology, 2012
Carboxylesterase 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
openaire   +2 more sources

Is genetic variability in carboxylesterase-1 and carboxylesterase-2 drug metabolism an important component of personalized medicine?

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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Anti-Influenza Prodrug Oseltamivir Is Activated by Carboxylesterase Human Carboxylesterase 1, and the Activation Is Inhibited by Antiplatelet Agent Clopidogrel

The Journal of Pharmacology and Experimental Therapeutics, 2006
Oseltamivir is the main medicine recommended by the World Health Organization in anticipation of next influenza pandemic. This anti-influenza viral agent is an ester prodrug, and the antiviral activity is achieved by its hydrolytic metabolite: oseltamivir carboxylate.
Shi, Deshi, Yang, Jian, Yang, Dongfang, LeCluyse, Edward L., Black, Chris, You, Li, Akhlaghi, Fatemeh, Yan, Bingfang   +7 more
openaire   +3 more sources

Predominant contributions of carboxylesterase 1 and 2 in hydrolysis of anordrin in humans

Xenobiotica, 2017
1. 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, Xiaoyan, Chen, Dafang, Zhong   +2 more
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Human carboxylesterase 1: from drug metabolism to drug discovery

Biochemical Society Transactions, 2003
Human 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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The effect of carboxylesterase 1 (CES1) polymorphisms on the pharmacokinetics of oseltamivir in humans

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, Naoto, Uemura, Makoto, Takada, Tetsuji, Ohyama, Akiko, Itohda, Takuya, Morimoto, Hiromitsu, Imai, Hajime, Hamasaki, Akihiro, Inano, Masakiyo, Hosokawa, Masato, Tateishi, Kyoichi, Ohashi   +11 more
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Does Clopidogrel Decrease the Efficacy of Carboxylesterase‐1 Prodrugs?

The FASEB Journal, 2020
It has previously been reported that clopidogrel is a potent inhibitor of the carboxylesterase‐1 (CES1) mediated hydrolysis of oseltamivir to its active metabolite based on in vitro inhibition studies. However, clopidogrel undergoes extensive first‐pass hepatic metabolism resulting in 85% of the dose being ...
Steven C. Laizure, Hui He, Roert B. Parker   +2 more
openaire   +1 more source

Binding and Hydrolysis of Meperidine by Human Liver Carboxylesterase hCE-1

The Journal of Pharmacology and Experimental Therapeutics, 1999
Human liver carboxylesterases catalyze the hydrolysis of apolar drug or xenobiotic esters into more soluble acid and alcohol products for elimination. Two carboxylesterases, hCE-1 and hCE-2, have been purified and characterized with respect to their role in cocaine and heroin hydrolysis. The binding of meperidine (Demerol) and propoxyphene (Darvon) was
J, Zhang, J C, Burnell, N, Dumaual, W F, Bosron   +3 more
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Nevadensin is a naturally occurring selective inhibitor of human carboxylesterase 1

International Journal of Biological Macromolecules, 2018
Human carboxylesterase 1 (hCE1) is a key enzyme responsible for the hydrolysis of a wide range of endogenous and xenobiotic esters, but the highly selective inhibitors against hCE1 are rarely reported. This study aimed to assess the inhibitory effects of natural flavonoids against hCE1 and to find potential specific hCE1 inhibitors.
Ya-Qiao, Wang, Zi-Miao, Weng, Tong-Yi, Dou, Jie, Hou, Dan-Dan, Wang, Le-Le, Ding, Li-Wei, Zou, Yang, Yu, Jing, Chen, Hui, Tang, Guang-Bo, Ge   +10 more
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Abstract 174: Carboxylesterase 1 in Lipid Metabolism and Obesity

Arteriosclerosis, Thrombosis, and Vascular Biology, 2012
Over-expression of human carboxylesterase 1 (CES1) in macrophages has been shown to increase hydrolysis of cholesterol esters and protect against atherosclerosis. However, the role of CES1 in other tissues and the physiological functions of CES1 are largely unknown. In this report, we investigated the role of CES1 in the liver.
Jiesi Xu, Liya Yin, Xuemei Ge, Yanqiao Zhang   +3 more
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