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Does Clopidogrel Decrease the Efficacy of Carboxylesterase‐1 Prodrugs?
The FASEB Journal, 2020It 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 +2 more
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Binding and Hydrolysis of Meperidine by Human Liver Carboxylesterase hCE-1
The Journal of Pharmacology and Experimental Therapeutics, 1999Human 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 +3 more
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Nevadensin is a naturally occurring selective inhibitor of human carboxylesterase 1
International Journal of Biological Macromolecules, 2018Human 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 +10 more
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Abstract 174: Carboxylesterase 1 in Lipid Metabolism and Obesity
Arteriosclerosis, Thrombosis, and Vascular Biology, 2012Over-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 +3 more
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[Progress in the structure and function of human carboxylesterase 1].
Sheng wu gong cheng xue bao = Chinese journal of biotechnology, 2014Human carboxylesterase 1 (HCE1), belonging to a multigene serine hydrolase family, is a major liver carboxylesterase responsible for the hydrolysis and metabolism of various xenobiotics. It also plays an important role in the transportation and metabolism of endogenous cholesterol ester and free fatty acid, and is closely associated with the ...
Jinying, Tong +5 more
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Carboxylesterase 1 (Ces1): from monocyte marker to major player
Journal of Clinical Pathology, 2010There are few, if any, enzymes that have been studied by, and have importance in, so many and varied disciplines as has monocyte esterase/Ces 1. In this review its involvement in the fields of histochemistry, haematology, toxicology, pharmacology, therapeutics, and tumour cell killing, immune surveillance and malignant disease, is briefly described.
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Pharmacological and physiological roles of the carboxylesterase 1 enzyme complex
2023The mammalian carboxylesterase 1 (Ces1/CES1) proteins are enzymes that break down a large number of (pro)drugs. The activity of these enzymes in the body can influence how effective a certain (pro)drug is. Ces1/CES1 enzymes are also known to affect lipid metabolism, thus affecting susceptibility to obesity-related metabolic disease.
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(−)‐FR182877 Is a Potent and Selective Inhibitor of Carboxylesterase‐1
Angewandte Chemie International Edition, 2003Gregory C, Adam +3 more
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