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Regulation of carboxylesterase 1 (CES1) in human adipose tissue [PDF]

open access: yesBiochemical and Biophysical Research Communications, 2009
Carboxylesterase 1 (CES1) has recently been suggested to play a role in lipolysis. Our aim was to study the regulation of CES1 expression in human adipose tissue. In the SOS Sib Pair Study, CES1 expression was higher in obese compared with lean sisters (n=78 pairs, P=8.7x10(-18)) and brothers (n=12 pairs, P=0.048).
Margareta Jernås   +2 more
exaly   +4 more sources
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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.
Zi-Miao Weng, Jie Hou, Dan-Dan Wang
exaly   +3 more sources

Carboxylesterase 1 Polymorphism Impairs Oseltamivir Bioactivation in Humans

Clinical Pharmacology & Therapeutics, 2012
Bioactivation 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
openaire   +3 more sources

Major implications of single nucleotide polymorphisms in human carboxylesterase 1 on substrate bioavailability

Biotechnology and Genetic Engineering Reviews, 2022
The number of studies and reviews conducted for the Carboxylesterase gene is limited in comparison with other enzymes. Carboxylesterase (CES) gene or human carboxylesterases (hCES) is a multigene protein belonging to the α/β-hydrolase family. Over the last decade, two major carboxylesterases (CES1 and CES2), located at 16q13-q22.1 on human chromosome ...
Goutham Yerrakula   +7 more
openaire   +2 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   +2 more
openaire   +2 more sources

Molecular mechanism of chromogenic substrate hydrolysis in the active site of human carboxylesterase-1

Biomeditsinskaya Khimiya, 2021
Human carboxylesterases are involved in the protective processes of detoxification during the hydrolytic metabolism of xenobiotics. Knowledge of the molecular mechanisms of substrates hydrolysis in the enzymes active site is necessary for the rational drug design.
A M, Kulakova   +2 more
openaire   +2 more sources

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
openaire   +2 more sources

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