Human liver carboxylesterase. Medical search. Frequent questions

Liver carboxylesterase 1 also known as carboxylesterase 1 (CES1, hCE-1 or CES1A1) is an enzyme that in humans is encoded by the CES1 gene. (wikipedia.org)
CES1 is present in most tissues with higher levels in the liver and low levels in the gastrointestinal tract. (wikipedia.org)
However, no thorough assessment of their potential to inhibit the major hepatic hydrolase, carboxylesterase 1 (CES1), exists. (inra.fr)
Based on available pharmacokinetic data, determined Ki values, and a physiologically based inhibition screen mimicking alkaloid exposures in humans, a DDI mediated via CES1 inhibition appears unlikely across a spectrum of doses (i.e., 2-20g per dose). (inra.fr)
In vitro studies suggest CBD may inhibit a number of drug-metabolizing enzymes, including carboxylesterase 1 (CES1). (inra.fr)
The overall structure of mCes2c resembles that of the human CES1 (hCES1). (inrae.fr)
CES1 and carboxylesterase 2 (CES2) are the two major human carboxylesterase isoforms and share 48% sequence homology. (ecologicalsgardens.com)
CES1 is usually expressed in multiple tissues while CES2 is usually detected in a more tissue-specific manner with liver small intestine and kidney being major sites of expression [14]. (ecologicalsgardens.com)

Diazinon caused an inhibition of carboxylesterase (CES) and acetylcholinesterase (AChE) activity in zebrafish larvae, diuron inhibited AChE activity in in vitro testing, and both pesticides significantly affected gene expression and activities of some of the cytochrome P450 (CYP) family enzymes. (springeropen.com)

Carboxylesterase 1 is a member of a large family of carboxylesterases that are responsible for the hydrolysis of ester and amide bonds (1, 2). (rndsystems.com)
N -Nitrosodimethylamine (NDMA) demethylation and p -nitrophenyl acetate (PNA) hydrolysis were used as catalytic markers of CYP2E1 and carboxylesterase enzymes, respectively. (aspetjournals.org)
Incubation of liver microsomes with EC (1 mM) produced slight but significant decreases in NDMA demethylation and PNA hydrolysis activities. (aspetjournals.org)
Here, through combined computational modeling and experimental studies, we demonstrate for the first time that human butyrylcholinesterase (BChE) is actually active against benzoylecgonine, and that a rationally designed BChE mutant can not only more efficiently accelerate cocaine hydrolysis but also significantly hydrolyze benzoylecgonine in vitro and in vivo. (inra.fr)
A non-specific carboxylesterase was purified from human liver that catalyzes the hydrolysis of the methyl ester group of cocaine to form benzoylecgonine. (inra.fr)
Undergoes hydrolysis in liver and tissues to form the active moiety (fluorouracil), inhibiting thymidylate synthetase, which in turn blocks methylation of deoxyuridylic acid to thymidylic acid. (medscape.com)

Cytochrome P450 and carboxylesterase enzymes have been implicated in the metabolism of the carcinogen ethyl carbamate (EC). (aspetjournals.org)
Irinotecan serves as a water-soluble precursor of the lipophilic metabolite SN-38, which is formed from irinotecan primarily by liver carboxylesterase enzymes. (rxmed.com)
The metabolic conversion of irinotecan to SN-38 is mediated by carboxylesterase enzymes primarily in the liver. (rxmed.com)
2,6-Dihydroxybenzoic acid is a secondary metabolite of salicylic acid which has been hydrolyzed by liver enzymes during phase I metabolism. (medchemexpress.com)

human-ABHD12 Homo sapiens (Human) abhydrolase domain-containing protein 12. (inrae.fr)
Saboori and Newcombe [19] previously showed that a carboxylesterase protein which was purified from human monocytes could be inhibited by oxon treatment. (ecologicalsgardens.com)
To better understand their role, Long's team engineered mice that secreted high levels of protein carboxylesterases from their livers without exercise. (musclemembers.com)
In the course of infection, the bacteria invade and colonize tissues of the upper respiratory tract, proliferate and produce exotoxin that inhibits protein synthesis and causes local lesions and systemic degenerative changes in the heart, muscles, peripheral nerves, liver and other vital organs. (up.ac.za)
Full length human recombinant protein of human LIPG produced in HEK293T cell. (thermofisher.com)

Thus, this study broadens our understanding of the mammalian carboxylesterase family and assists in delineating the similarities and differences of the different family members. (inrae.fr)
Bacteria were used as sensitive indicators for DNA damage and mammalian liver extracts for metabolic conversion of carcinogens to their active metabolic forms. (europa.eu)

Two major liver isoforms of aldehyde dehydrogenase, cytosolic and mitochondrial, can be distinguished by their electrophoretic mobilities, kinetic properties, and subcellular localizations. (nih.gov)
2005): Malathion bioactivation in the human liver: The contribution of different cytochrome p450 isoforms. (ankara.edu.tr)

In this study, we have used a murine liver microsomal system to investigate the relative contributions of P450 and carboxylesterase isozymes to hepatic metabolism of EC. (aspetjournals.org)

Oxons are the bioactivated metabolites of organophosphothionate pesticides and are formed mainly in liver following cytochrome P450 monooxygenase-catalyzed desulfuration [18]. (ecologicalsgardens.com)

The SN-38 metabolite is approximately 1 000 times more potent than irinotecan as an inhibitor of topoisomerase I purified from human and rodent tumor cell lines. (rxmed.com)
Converted by the carboxylesterase enzyme to its active metabolite from, SN-38. (medscape.com)

Members of the carboxylesterase 2 (Ces2/CES2) family have been studied intensively with respect to their hydrolytic function on (pro)drugs, whereas their physiological role in lipid and energy metabolism has been realized only within the last few years. (inrae.fr)
Humans have one CES2 gene which is highly expressed in liver, intestine, and kidney. (inrae.fr)
Mouse Ces2c (mCes2c) is suggested as potential ortholog of human CES2. (inrae.fr)
The purpose of this study was to assess characteristics of SJ-815, a novel oncolytic vaccinia virus lacking a functional thymidine kinase-encoding TK gene, and instead, having two human transgenes: the IFNB1 that encodes interferon β1, and the CES2 that encodes carboxylesterase 2, which metabolizes the prodrug, irinotecan, into cytotoxic SN-38. (e-crt.org)
To this end, we designed and engineered SJ-185, a novel oncolytic vaccinia virus, through incorporating two human transgenes, the IFNB1 and CES2 , into the TK gene region of a Western Reserve (WR) strain vaccinia virus backbone. (e-crt.org)

Carboxylesterase 1 is a serine esterase and member of a large multigene carboxylesterase family. (wikipedia.org)
In this report we characterize the inhibitory effects of three oxons derived from commonly used pesticides on esterase activities in human THP-1 monocyte/macrophages. (ecologicalsgardens.com)
Metabolism involves CYP450 activation and detoxification of CPF to CPF-oxon and 3,5,6-trichloro-2-pyridinol (TCP), as well as cholinesterase (acetyl- and butyrylcholinesterase), carboxylesterase (CaE), and A-esterase (PON-1) detoxification of CPF-oxon to TCP. (cdc.gov)

2 The antibodies for the carboxylesterases were raised against rat liver microsomal hydrolase A and hydrolase B. For ease of description, the murine liver microsomal proteins recognized by these antibodies are designated with the same nomenclature. (aspetjournals.org)
SN-38 is approximately 95% bound to human plasma proteins, mainly albumin. (rxmed.com)
The team was also surprised to find that liver cells, and liver cells alone, secrete different members of the carboxylesterase family of proteins after exercise. (musclemembers.com)

however, reaction with PAX and not PMSF or EC resulted in loss of immunoreactivity for hydrolase B. These data correlated with levels of covalent binding of [ ethyl - 14 C]EC to liver microsomes, which were significantly elevated in incubations conducted with PAX or PMSF. (aspetjournals.org)

These results are consistent with the premise that EC is metabolized by CYP2E1 and hydrolase A in liver microsomes of mice. (aspetjournals.org)

E. coli in humans is a commensal inhabitant of the gastrointestinal tract. (cdc.gov)

Two identical matches were found corresponding to carboxylesterase cDNAs from human liver and lung. (inra.fr)

2013), a human cell gene mutation assay in the TK locus (Budinsky et al. (europa.eu)
A human cell gene mutation assay in the HPRT locus is also available, although experimental methodology is limited (Budinsky et al. (europa.eu)
Vinyl acetate was negative in bacterial gene mutation assays using Salmonella typhimurium TA98, TA100, TA1535 and TA1537, with and without rat liver S-9 activation. (europa.eu)
Vinyl acetate was shown to be negative in bacterial gene mutation assays using Salmonella typhimurium TA98, TA100, TA1535 and TA1537, with and without rat liver S-9 activation. (europa.eu)

Keramati V, Jamili S, Ramin M (2010): Effect of diazinon on catalase antioxidant enzyme activity in liver tissue of Rutilus rutilus. (ankara.edu.tr)

Includes patients co-infected with human immunodeficiency virus (HIV). (medicines.org.uk)

Hepatocyte-Specific Expression of Human Carboxylesterase 2 Attenuates Non-alcoholic Steatohepatitis in Mice. (fudan.edu.cn)
Hepatocyte-specific Expression of Human Carboxylesterase 1 Attenuates Diet-induced Steatohepatitis and Hyperlipidemia. (fudan.edu.cn)

The National Institute of Environmental Health Sciences (NIEHS) is expanding and accelerating its contributions to scientific knowledge of human health and the environment, and to the health and well-being of people everywhere. (nih.gov)

Hepatocyte miR-34a is a key regulator of the development and progression of non-alcoholic fatty liver disease. (fudan.edu.cn)
Lipocalin-2 Protects Against Diet-induced Non-alcoholic Fatty Liver Disease by Targeting Hepatocytes. (fudan.edu.cn)
Department of Health and Human Services, Public Health Service, Agency for Toxic Substances and Disease Registry. (cdc.gov)
Influenza A viruses are classified into subtypes on the basis of two surface antigens: hemagglutinin (H) and neuraminidase (N). Three subtypes of hemagglutinin (H1, H2 and H3) and two subtypes of neuraminidase (N1 and N2) are recognized among influenza A viruses that have caused widespread human disease. (canada.ca)
NIEHS research uses state-of-the-art science and technology to investigate the interplay between environmental exposures, human biology, genetics, and common diseases to help prevent disease and improve human health. (nih.gov)

A human apolipoprotein E mimetic peptide reduces atherosclerosis in aged apolipoprotein E null mice. (fudan.edu.cn)
Kettarman AJ, Pond SM, Becker CE (1987): The effect of carboxylesterase and glutathion S-transferase activities on malathion toxicity in mice. (ankara.edu.tr)
In humans, do blood-transported carboxylesterase levels change in response to exercise as they do in mice? (musclemembers.com)

Tumor cytotoxicity of SJ-815 (or mSJ-815, which has the murine IFNB1 transgene for mouse cancers) was evaluated using human and mouse cancer cells. (e-crt.org)

Myhep ought to be simultaneously utilized with ribavirin as a single dose until liver transmission. (mhp.ooo)

3. HEALTH EFFECTS the effects vary with dose and/or duration, and place into perspective the possible significance of these effects to human health. (cdc.gov)

Pharmacokinetics: After i.v. infusion of irinotecan in humans, irinotecan plasma levels decline in a multiexponential manner. (rxmed.com)
Public health officials and others concerned with appropriate actions to take at hazardous waste sites may want information on levels of exposure associated with more subtle effects in humans or animals (LOAELs) or exposure levels below which no adverse effects (NOAELs) have been observed. (cdc.gov)
Estimates of levels posing minimal risk to humans (minimal risk levels or MRLs) may be of interest to health professionals and citizens alike. (cdc.gov)
Estimates of exposure levels posing minimal risk to humans (Minimal Risk Levels or MRLs) have been made for methyl parathion. (cdc.gov)
As these kinds of health effects data become available and methods to assess levels of significant human exposure improve, these MRLs will be revised. (cdc.gov)

They also participate in detoxification of drugs such as cocaine and heroin in serum and liver. (rndsystems.com)
The carboxylesterase obeys simple Michaelis-Menten kinetics with Km values of 116 microM for cocaine and 43 mM for ethanol. (inra.fr)

Homogenates of rat (or human) liver (S9 mix) were added directly to petri plates to evaluate the need for metabolic activation. (europa.eu)

Antitumor effects of SJ-815, with/without irinotecan, were evaluated using a human pancreatic cancer-bearing mouse model and a syngeneic melanoma-bearing mouse model. (e-crt.org)

Researchers have long been intrigued by the possibility that exercise causes various cells in our bodies to produce molecules that benefit human health, says Jonathan Long, an assistant professor of pathology at Stanford University. (musclemembers.com)
Find out about the exciting discoveries being made by NIEHS and NIEHS-supported researchers that are helping to improve health and save lives. (nih.gov)

An MRL is defined as an estimate of daily human exposure to a substance that is likely to be without an appreciable risk of adverse effects (noncarcinogenic) over a specified duration of exposure. (cdc.gov)
Gerdy GF, Rose HA, Starey NH (1987): Effect of lenght of exposure to malathion on xenobiotic biotransformation in male rat liver. (ankara.edu.tr)

The precise contribution of SN-38 to the activity of irinotecan in humans has not been completely defined. (rxmed.com)

General Information: They may be found as members of the normal microflora of humans, where these bacteria find a suitable niche in virtually every anatomic site. (up.ac.za)

In fact, the usual suspects like muscle, bone and liver cells all had only moderate responses by comparison, Long says. (musclemembers.com)

Anatomy2

Diseases6

Chemicals and Drugs7

CES18

Inhibition of carboxylesterase1

Hydrolysis6

Enzymes4

Protein5

Mammalian2

Isoforms2

Isozymes1

Cytochrome P4501

Metabolite2

CES25

Esterase3

Proteins3

Ethyl1

Microsomes1

Gastrointestinal tract1

Lung1

Gene4

Diazinon1

Immunodeficiency virus1

Expression2

Contributions1

Disease5

Mice3

Murine1

Ribavirin1

Significance1

Levels5

Cocaine2

Metabolic1

Mouse1

Researchers2

Exposure2

Activity1

Members1

Responses1