Results 161 to 170 of about 10,733 (194)

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
openaire   +2 more sources

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
openaire   +2 more sources

Allosteric kinetics of human carboxylesterase 1: Species differences and interindividual variability

Journal of Pharmaceutical Sciences, 2008
Esterified drugs such as imidapril, derapril, and oxybutynin hydrolyzed by carboxylesterase 1 (CES1) are extensively used in clinical practice. The kinetics using the CES1 substrates have not fully clarified, especially concerning species and tissue differences.
Shiori, Takahashi, Miki, Katoh, Takashi, Saitoh, Miki, Nakajima, Tsuyoshi, Yokoi   +4 more
openaire   +2 more sources

The Biotransformation of Prasugrel, a New Thienopyridine Prodrug, by the Human Carboxylesterases 1 and 2

Drug Metabolism and Disposition, 2008
2-Acetoxy-5-(alpha-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine (prasugrel) is a novel thienopyridine prodrug with demonstrated inhibition of platelet aggregation and activation. The biotransformation of prasugrel to its active metabolite, 2-[1-[2-cyclopropyl-1-(2-fluorophenyl)-2-oxoethyl]-4-mercapto-3-piperidinylidene ...
Eric T, Williams, Karen O, Jones, G Douglas, Ponsler, Shane M, Lowery, Everett J, Perkins, Steven A, Wrighton, Kenneth J, Ruterbories, Miho, Kazui, Nagy A, Farid   +8 more
openaire   +2 more sources

A magnetic SERS immunosensor for highly sensitive and selective detection of human carboxylesterase 1 in human serum samples

Analytica Chimica Acta, 2020
Hepatocellular carcinoma (HCC) is a common and lethal cancer. New serum markers for detecting HCC are urgently needed. Human carboxylesterase 1 (hCE1) is an important member of the serine hydrolase superfamily and is closely related to the occurrence of HCC. It can be used as a good serum marker for early diagnosis of HCC.
Jun Feng, Yajuan Xu, Wenyi Huang, Hongxing Kong, Yanqing Li, Hao Cheng, Lijun Li   +6 more
openaire   +2 more sources

[Progress in the structure and function of human carboxylesterase 1].

Sheng wu gong cheng xue bao = Chinese journal of biotechnology, 2014
Human 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, Yinsha, Yi, Pengrong, Cao, Caiyun, Liu, Lei, Wang, Yuan, Lü   +5 more
openaire   +1 more source

Investigation of the chiral recognition ability of human carboxylesterase 1 using indomethacin esters

Chirality, 2019
AbstractHuman carboxylesterase 1 (hCES1) is an enzyme that plays an important role in hydrolysis of pharmaceuticals in the human liver. In this study, elucidation of the chiral recognition ability of hCES1 was attempted using indomethacin esters in which various chiral alcohols were introduced. Indomethacin was condensed with various chiral alcohols to
Masato Takahashi, Daisuke Takani, Masami Haba, Masakiyo Hosokawa   +3 more
openaire   +2 more sources

Discovery of natural pentacyclic triterpenoids as potent and selective inhibitors against human carboxylesterase 1

Fitoterapia, 2019
Human carboxylesterase 1 (CES1), primarily expressed in the liver and adipocytes, is responsible for the hydrolysis of endogenous esters (such as cholesteryl esters and triacylglycerols) and the metabolism of xenobiotic esters (such as clopidogrel and oseltamivir), thus participates in physiological and pathological processes.
Pei-Fang, Song, Ya-Di, Zhu, Hong-Ying, Ma, Yi-Nan, Wang, Dan-Dan, Wang, Li-Wei, Zou, Guang-Bo, Ge, Ling, Yang   +7 more
openaire   +2 more sources

Chemical synthesis of an indomethacin ester prodrug and its metabolic activation by human carboxylesterase 1

Bioorganic & Medicinal Chemistry Letters, 2018
It is necessary to consider the affinity of prodrugs for metabolic enzymes for efficient activation of the prodrugs in the body. Although many prodrugs have been synthesized with consideration of these chemical properties, there has been little study on the design of a structure with consideration of biological properties such as substrate recognition ...
Masato Takahashi, Tomohiro Ogawa, Hiroshi Kashiwagi, Fumiya Fukushima, Misaki Yoshitsugu, Masami Haba, Masakiyo Hosokawa   +6 more
openaire   +2 more sources

Age- and Sex-Related Expression and Activity of Carboxylesterase 1 and 2 in Mouse and Human Liver

Drug Metabolism and Disposition, 2009
Carboxylesterase (CES) 1 and CES2 are two major hepatic hydrolases responsible for the metabolism of numerous endogenous and exogenous compounds. In this study, age- and sex-dependent expression and activity of CES1 and CES2 were investigated using both animal models and individual human liver s9 samples.
Hao-Jie, Zhu, David I, Appel, Yan, Jiang, John S, Markowitz   +3 more
openaire   +2 more sources