Carboxylesterase is a serine-dependent esterase with wide substrate specificity. The enzyme is involved in the detoxification of XENOBIOTICS and the activation of ester and of amide PRODRUGS.
Enzymes which catalyze the hydrolysis of carboxylic acid esters with the formation of an alcohol and a carboxylic acid anion.
An organophosphate cholinesterase inhibitor that is used as a pesticide.
A compound that, on administration, must undergo chemical conversion by metabolic processes before becoming the pharmacologically active drug for which it is a prodrug.
The process of cleaving a chemical compound by the addition of a molecule of water.
An enzyme inhibitor that inactivates IRC-50 arvin, subtilisin, and the fatty acid synthetase complex.
A di-isopropyl-fluorophosphate which is an irreversible cholinesterase inhibitor used to investigate the NERVOUS SYSTEM.
An alkaloid isolated from the stem wood of the Chinese tree, Camptotheca acuminata. This compound selectively inhibits the nuclear enzyme DNA TOPOISOMERASES, TYPE I. Several semisynthetic analogs of camptothecin have demonstrated antitumor activity.
Enzyme catalyzing reversibly the hydrolysis of palmitoyl-CoA or other long-chain acyl coenzyme A compounds to yield CoA and palmitate or other acyl esters. The enzyme is involved in the esterification of fatty acids to form triglycerides. EC 3.1.2.2.
A wide spectrum aliphatic organophosphate insecticide widely used for both domestic and commercial agricultural purposes.
Cyclic amide of caproic acid used in manufacture of synthetic fibers of the polyamide type. Can cause local irritation.
Closed vesicles of fragmented endoplasmic reticulum created when liver cells or tissue are disrupted by homogenization. They may be smooth or rough.
An organothiophosphorus cholinesterase inhibitor that is used as an insecticide and as a acaricide.
The active insecticidal constituent of CHRYSANTHEMUM CINERARIIFOLIUM flowers. Pyrethrin I is the pyretholone ester of chrysanthemummonocarboxylic acid and pyrethrin II is the pyretholone ester of chrysanthemumdicarboxylic acid monomethyl ester.
7-Hydroxycoumarins. Substances present in many plants, especially umbelliferae. Umbelliferones are used in sunscreen preparations and may be mutagenic. Their derivatives are used in liver therapy, as reagents, plant growth factors, sunscreens, insecticides, parasiticides, choleretics, spasmolytics, etc.
Agents obtained from higher plants that have demonstrable cytostatic or antineoplastic activity.
Chemicals that are used to cause the disturbance, disease, or death of humans during WARFARE.
The development by insects of resistance to insecticides.
An organophosphorus compound that inhibits cholinesterase. It causes seizures and has been used as a chemical warfare agent.
Carbon-containing phosphoric acid derivatives. Included under this heading are compounds that have CARBON atoms bound to one or more OXYGEN atoms of the P(=O)(O)3 structure. Note that several specific classes of endogenous phosphorus-containing compounds such as NUCLEOTIDES; PHOSPHOLIPIDS; and PHOSPHOPROTEINS are listed elsewhere.
Naphthalene derivatives containing the -CH2CCO2H radical at the 1-position, the 2-position, or both. Compounds are used as plant growth regulators to delay sprouting, exert weed control, thin fruit, etc.
An aspect of cholinesterase (EC 3.1.1.8).
An enzyme that catalyzes reversibly the hydrolysis of acetyl-CoA to yield CoA and acetate. The enzyme is involved in the oxidation of fatty acids. EC 3.1.2.1.
An organothiophosphate cholinesterase inhibitor that is used as an insecticide and as an acaricide.
A characteristic feature of enzyme activity in relation to the kind of substrate on which the enzyme or catalytic molecule reacts.
A genus of GRAM-POSITIVE ENDOSPORE-FORMING RODS, in the family Alicyclobacillaceae, containing a unique lipid in their membranes.
Antineoplastic agent that is also used as a veterinary anesthetic. It has also been used as an intermediate in organic synthesis. Urethane is suspected to be a carcinogen.
An enzyme that catalyzes the hydrolysis of glycerol monoesters of long-chain fatty acids EC 3.1.1.23.
Drugs that inhibit cholinesterases. The neurotransmitter ACETYLCHOLINE is rapidly hydrolyzed, and thereby inactivated, by cholinesterases. When cholinesterases are inhibited, the action of endogenously released acetylcholine at cholinergic synapses is potentiated. Cholinesterase inhibitors are widely used clinically for their potentiation of cholinergic inputs to the gastrointestinal tract and urinary bladder, the eye, and skeletal muscles; they are also used for their effects on the heart and the central nervous system.
A large lobed glandular organ in the abdomen of vertebrates that is responsible for detoxification, metabolism, synthesis and storage of various substances.
Salts and esters of CHOLIC ACID.
The chemical alteration of an exogenous substance by or in a biological system. The alteration may inactivate the compound or it may result in the production of an active metabolite of an inactive parent compound. The alterations may be divided into METABOLIC DETOXICATION, PHASE I and METABOLIC DETOXICATION, PHASE II.
Pesticides designed to control insects that are harmful to man. The insects may be directly harmful, as those acting as disease vectors, or indirectly harmful, as destroyers of crops, food products, or textile fabrics.
Hydroxylated benzoic acid derivatives that contain mercury. Some of these are used as sulfhydryl reagents in biochemical studies.
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
One of the long-acting synthetic ANTIDIARRHEALS; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally.
A species of gram-negative, obligately aerobic rods. Motility occurs by peritrichous flagella. (From Bergey's Manual of Determinative Bacteriology, 9th ed)
An enzyme that catalyzes the hydrolysis of ACETYLCHOLINE to CHOLINE and acetate. In the CNS, this enzyme plays a role in the function of peripheral neuromuscular junctions. EC 3.1.1.7.
The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.
Organic compounds that contain phosphorus as an integral part of the molecule. Included under this heading is broad array of synthetic compounds that are used as PESTICIDES and DRUGS.
Specialized non-fenestrated tightly-joined ENDOTHELIAL CELLS with TIGHT JUNCTIONS that form a transport barrier for certain substances between the cerebral capillaries and the BRAIN tissue.
Fatty acid esters of cholesterol which constitute about two-thirds of the cholesterol in the plasma. The accumulation of cholesterol esters in the arterial intima is a characteristic feature of atherosclerosis.
Luciferases from BACTERIA such as PHOTOBACTERIUM; VIBRIO; and PHOTORHABDUS.
Lists of words, usually in alphabetical order, giving information about form, pronunciation, etymology, grammar, and meaning.
Membrane-like channels of cytoplasm connecting adjacent plant cells. Plasmodesmata connect through pores in the CELL WALL and associate with the CYTOSKELETON machinery. They are essential for intercellular transport and communication.
Conjugated protein-carbohydrate compounds including mucins, mucoid, and amyloid glycoproteins.
Proteins prepared by recombinant DNA technology.
The chemical or biochemical addition of carbohydrate or glycosyl groups to other chemicals, especially peptides or proteins. Glycosyl transferases are used in this biochemical reaction.

Localization of a candidate surfactant convertase to type II cells, macrophages, and surfactant subfractions. (1/410)

Pulmonary surfactant exists in the alveolus in several distinct subtypes that differ in their morphology, composition, and surface activity. Experiments by others have implicated a serine hydrolase in the production of the inactive small vesicular subtype of surfactant (N. J. Gross and R. M. Schultz. Biochim. Biophys. Acta 1044: 222-230, 1990). Our laboratory recently identified this enzyme in the rat as the serine carboxylesterase ES-2 [F. Barr, H. Clark, and S. Hawgood. Am. J. Physiol. 274 (Lung Cell. Mol. Physiol. 18): L404-L410, 1998]. In the present study, we determined the cellular sites of expression of ES-2 in rat lung using a digoxygenin-labeled ES-2 riboprobe. ES-2 mRNA was localized to type II cells and alveolar macrophages but not to Clara cells. Using a specific ES-2 antibody, we determined the protein distribution of ES-2 in the lung by immunohistochemistry, and it was found to be consistent with the sites of mRNA expression. Most of the ES-2 in rat bronchoalveolar lavage is in the surfactant-depleted supernatant, but ES-2 was also consistently localized to the small vesicular surfactant subfraction presumed to form as a consequence of conversion activity. These results are consistent with a role for endogenous lung ES-2 in surfactant metabolism.  (+info)

Comparison of activation of CPT-11 by rabbit and human carboxylesterases for use in enzyme/prodrug therapy. (2/410)

Several recent studies have examined the possibility of producing tumor-specific cytotoxicity with various enzyme/ prodrug combinations. The enzymes are targeted to tumor cells either with antibodies (ADEPT, antibody directed enzyme prodrug therapy) or with viruses (VDEPT). The goal of the present study was to identify an appropriate enzyme for use in activating the prodrug 7-ethyl-10-[4-(1-piper-idino)-1-piperidino]carbonyloxycamptothe cin (CPT-11). In this study, we compared the efficiency of CPT-11 metabolism by rabbit and human carboxylesterases in in vitro and in situ assays. Although the rabbit and human enzymes are very similar (81% identical; 86% homologous) and the active site amino acids are 100% identical, the rabbit enzyme was 100-1000-fold more efficient at converting CPT-11 to SN-38 in vitro and was 12-55-fold more efficient in sensitizing transfected cells to CPT-11. In vivo, Rh30 rhabdomyosarcoma cells expressing the rabbit carboxylesterase and grown as xenografts in immune-deprived mice were also more sensitive to CPT-11 than were control xenografts or xenografts expressing the human enzyme. Each of the three types of xenografts regressed when the mice were treated with CPT-11 given i.v. at 2.5 mg of CPT-11/kg/daily for 5 days/week for 2 weeks [(dx5)2] (one cycle of therapy), repeated every 21 days for a total of three cycles. However, following cessation of treatment, recurrent tumors were detected in seven of seven mice bearing control Rh30 xenografts and in two of seven mice bearing Rh30 xenografts that expressed the human enzyme. No tumors recurred in mice bearing xenografts that expressed the rabbit carboxylesterase. We conclude that rabbit carboxylesterase/CPT-11 may be a useful enzyme/prodrug combination.  (+info)

Relationship between amount of esterase and gene copy number in insecticide-resistant Myzus persicae (Sulzer). (3/410)

Overproduction of the insecticide-degrading esterases, E4 and FE4, in peach-potato aphids, Myzus persicae (Sulzer), depends on both gene amplification and transcriptional control, the latter being associated with changes in DNA methylation. The structure and function of the aphid esterase genes have been studied but the determination of their copy number has proved difficult, a common problem with gene amplification. We have now used a combination of pulsed-field gel electrophoresis and quantitative competitive PCR to determine relative esterase gene copy numbers in aphid clones with different levels of insecticide resistance (R1, R2 and R3). There are approx. 4-fold increases between susceptible, R1, R2 and R3 aphids, reaching a maximum of approx. 80 times more genes in R3; this gives proportionate increases in esterase protein relative to susceptible aphids. Thus there is no overexpression of the amplified genes, in contrast with what was thought previously. For E4 genes, the loss of 5-methylcytosine is correlated with a loss of expression, greatly decreasing the amount of enzyme relative to the copy number.  (+info)

Establishment of an activated macrophage cell line, A-THP-1, and its properties. (4/410)

A new macrophage cell line with activated character and unique morphology was isolated by selecting adherent cells from the human monocytic cell line THP-1. The original THP-1 cells had been cultured for more than 9 years using 25 cm2 flasks, when cells with a different morphology appeared, adhering to the bottoms of the culture flasks. These were selected by discarding floating nonadherent cells at every subculture. Enrichment of adherent THP-1 cells with long processes proceeded during the cultivation. These adherent THP-1 showed remarkable phenotypic changes, not only morphologically, but also functionally. Namely, increased phagocytic activity, HLA-DR expression and MLR stimulator activity were remarkable. This adherent cell line was designated as activated-THP-1 (A-THP-1), since it demonstrated characteristics of activated macrophages continuously without exogenous stimulation. A cloned A-THP-1 cell line (A-THP-1 C1) also showed the same features and contained about 10% multinucleated giant cells probably caused by cell fusion. This A-THP-1 cell line, the first activated macrophage cell line to be established, provides a good model for understanding of activation mechanisms of macrophages and multinucleation. In this paper, morphological, immunological, and biological characters of this cell line are described.  (+info)

Targeting proteins to the lumen of endoplasmic reticulum using N-terminal domains of 11beta-hydroxysteroid dehydrogenase and the 50-kDa esterase. (5/410)

Previous studies identified two intrinsic endoplasmic reticulum (ER) proteins, 11beta-hydroxysteroid dehydrogenase, isozyme 1 (11beta-HSD) and the 50-kDa esterase (E3), sharing some amino acid sequence motifs in their N-terminal transmembrane (TM) domains. Both are type II membrane proteins with the C terminus projecting into the lumen of the ER. This finding implied that the N-terminal TM domains of 11beta-HSD and E3 may constitute a lumenal targeting signal (LTS). To investigate this hypothesis we created chimeric fusions using the putative targeting sequences and the reporter gene, Aequorea victoria green fluorescent protein. Transfected COS cells expressing LTS-green fluorescent protein chimeras were examined by fluorescent microscopy and electron microscopic immunogold labeling. The orientation of expressed chimeras was established by immunocytofluorescent staining of selectively permeabilized COS cells. In addition, protease protection assays of membranes in the presence and absence of detergents was used to confirm lumenal or the cytosolic orientation of the constructed chimeras. To investigate the general applicability of the proposed LTS, we fused the N terminus of E3 to the N terminus of the NADH-cytochrome b5 reductase lacking the myristoyl group and N-terminal 30-residue membrane anchor. The orientation of the cytochrome b5 reductase was reversed, from cytosolic to lumenal projection of the active domain. These observations establish that an amino acid sequence consisting of short basic or neutral residues at the N terminus, followed by a specific array of hydrophobic residues terminating with acidic residues, is sufficient for lumenal targeting of single-pass proteins that are structurally and functionally unrelated.  (+info)

Inactivation and loss of antigenicity of esterase by sugars and a steroid. (6/410)

Glycation, the non-enzymic reaction of sugars with proteins, has an important role in the complications of diabetes. It has been studied mostly in structural proteins but more recently has been shown to inactivate enzymes. Previous evidence from our laboratory indicated that glycation-induced inactivation and loss of antigenicity of catalase and superoxide dismutase are simultaneous. Esterase, which decreases activity in the lens in senile cataract and diabetes, was measured by a spectrophotometric assay using p-nitrophenyl acetate as the substrate. Here we investigated the inactivation of carboxylesterase (EC 3.1.1.1) by sugars of different glycating power and prednisolone-21-hemisuccinate while simultaneously monitoring the loss of antigenicity. Antigenicity was assessed by immunoprecipitation and by dot-blotting the glycated and non-glycated fractions of enzymes separated by affinity chromatography. Ribose and fructose inactivated more rapidly than glucose and glucose 6-phosphate. The esterase was progressively inactivated by prednisolone-21-hemisuccinate at a lower concentration. Activity and antigenicity were lost simultaneously. The glycated enzyme had entirely lost its antigenicity. These results further support the idea that inactivation of enzyme and loss of antigenicity are simultaneous.  (+info)

A non-AUG-defined alternative open reading frame of the intestinal carboxyl esterase mRNA generates an epitope recognized by renal cell carcinoma-reactive tumor-infiltrating lymphocytes in situ. (7/410)

A number of Ags recognized by tumor-reactive T cells have been characterized, including nonmutated gene products and a variety of epitopes shown to arise from either mutated or alternatively processed transcripts. Here, we report that the screening of a cDNA library with an HLA-B7-restricted renal cell carcinoma-reactive T cell clone derived from tumor-infiltrating lymphocytes (TILs) that were clonally amplified in vivo (as assessed by TCRBV complementarity determining region-3 length distribution analysis) resulted in the isolation of a nonamer encoded by an alternative open reading frame (ORF) (a +1 frameshift) of the intestinal carboxyl esterase gene. This peptide binds HLA-B*0702-presenting molecules as assessed in an immunofluorescence-based peptide binding assay using transfected T2 cells. Constitutive expression of this alternative ORF protein was observed in all transformed HLA-B7+ renal cell lines that were recognized in cytotoxicity assays by the TILs. The intestinal carboxyl esterase gene is transcribed in renal cell carcinoma tumors as well as in normal liver, intestinal, or renal tissues. Mutation of the natural ATG translation initiation site did not alter recognition, indicating that frameshifting (i.e., slippage of the ribosome forward) and recoding are not involved. In addition, a point mutation of the three AUG codons that may be used as alternative translation initiation sites in the +1 ORF did not abolish recognition, whereas mutation of an upstream ACG codon did, indicating that the latter codon initiates the translation of the alternative ORF. These results further extend the types of Ags that can be recognized by tumor-reactive TILs in situ (i.e., leading to clonal T cell expansion).  (+info)

Microsomal long-chain acyl-CoA thioesterase (carboxylesterase ES-4) is regulated by thyroxine. (8/410)

Long chain acyl-CoA thioesterase activity is mainly located in microsomes after subcellular fractionation of liver from untreated rats. The physiological function and regulation of expression of this activity is not known. In the present study we have investigated the effect of thyroxine on expression of carboxylesterase ES-4, the major acyl-CoA thioesterase of liver microsomes. Thyroidectomy of rats decreased the palmitoyl-CoA thioesterase activity to about 25% of normal activity. This decrease was accompanied by similar decreases at the protein and mRNA levels (31% and 57%, respectively, of controls). Treatment with thyroxine completely reversed the effect of thyroidectomy and resulted in elevated levels in both thyroidectomized and control rats. For reasons of comparison we also studied the possibility that ES-10 and ES-2, two other members of the same gene family, are affected by thyroxine. ES-10 was not changed at the protein or mRNA level by any of the treatments, while ES-2 expression in liver was decreased by thyroxine treatment. The data shows that changes in activity and expression of ES-4 correlate to thyroxine status in the rat suggesting a physiological regulatory role by this hormone. Since thyroxine regulates the expression of lipogenic enzymes, these results are consistent with a function for this microsomal acyl-CoA thioesterase in fatty acid synthesis and/or secretion, rather than in oxidative degradation of fatty acids.  (+info)

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TY - JOUR. T1 - Hydrolysis of capecitabine to 5′-deoxy-5-fluorocytidine by human carboxylesterases and inhibition by loperamide. AU - Quinney, S. K.. AU - Sanghani, S. P.. AU - Davis, W. I.. AU - Hurley, T. D.. AU - Sun, Z.. AU - Murry, D. J.. AU - Bosron, William F.. PY - 2005/6/1. Y1 - 2005/6/1. N2 - Capecitabine is an oral prodrug of 5-fluorouracil that is indicated for the treatment of breast and colorectal cancers. A three-step in vivo-targeted activation process requiring carboxylesterases, cytidine deaminase, and thymidine phosphorylase converts capecitabine to 5-fluorouracil. Carboxylesterases hydrolyze capecitabines carbamate side chain to form 5′-deoxy-5-fluorocytidine (5′-DFCR). This study examines the steady-state kinetics of recombinant human carboxylesterase isozymes carboxylesterase (CES) 1A1, CES2, and CES3 for hydrolysis of capecitabine with a liquid chromatography/mass spectroscopy assay. Additionally, a spectrophotometric screening assay was utilized to identify drugs ...
Carboxyl Ester Lipase/CEL Antibodies available through Novus Biologicals. Browse our Carboxyl Ester Lipase/CEL Antibody catalog backed by our Guarantee+.
In enzymology, a carboxylesterase or carboxylic-ester hydrolase (EC 3.1.1.1) is an enzyme that catalyzes a chemical reaction of the form a carboxylic ester + H2O ⇌ {\displaystyle \rightleftharpoons } an alcohol + a carboxylate Thus, the two substrates of this enzyme are carboxylic ester and H2O, whereas its two products are alcohol and carboxylate. Most enzymes from this group are serine hydrolases belonging to the superfamily of proteins with alpha/beta hydrolase fold. Some exceptions include an esterase with beta-lactamase like structure (PDB: 1ci8​). Carboxylesterases are widely distributed in nature, and are common in mammalian liver. Many participate in phase I metabolism of xenobiotics such as toxins or drugs; the resulting carboxylates are then conjugated by other enzymes to increase solubility and eventually excreted. The carboxylesterase family of evolutionarily related proteins (those with clear sequence homology to each other) includes a number of proteins with different substrate ...
Irinotecan is a relatively new anticancer agent of interest for both its clinical activity and its complex clinical pharmacology. It is a prodrug, requiring activation by carboxylesterases to SN-38, an inhibitor of topoisomerase I. Recent studies suggest that human carboxylesterase-2 is the primary carboxylesterase involved in the hydrolysis at pharmacological concentrations (1) . Irinotecan is also oxidized by CYP3A43 to the inactive metabolite 7-ethyl-10-[4-N-(5-aminopentanoic acid)-1-piperidino]carbonyloxycamptothecin as well as to 7-ethyl-10-[4-(piperidino)-1-amino]carbonyloxycamptothecin, which can undergo hydrolysis to SN-38 (2, 3, 4) . SN-38 undergoes glucuronidation by UGT1A1 (5) and is possibly oxidized by CYP3A4 as well (6) . Mass balance studies have demonstrated that 64% of the total dose is excreted in the feces, confirming the important role of biliary excretion (7) . Studies suggest that canalicular multispecific organic anion transporter is the major transporter of irinotecan and ...
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 = 8.7 x 10(-18)) and brothers (n = 12 Pairs, P = 0.048). CES1 expression was higher in subcutaneous compared with omental adipose tissue in lean (P = 0.027) and obese Subjects (P = 0.00036), and reduced during diet-induced weight loss (it = 24, weeks 8, 16, and 18 compared to baseline, P , 0.0001 for all time points). CES1 expression was higher in isolated adipocytes compared with intact adipose tissue (P = 0.0018) and higher in large compared with small adipocytes (P = 4.1 x 10(-6)). Basal and Stimulated lipolysis was not different in individuals with high, intermediate, and low expression of CES1. Thus, CES1 expression was linked to body fat and adipocyte fat content but not to lipolytic activity. (C) 2009 Elsevier Inc. All ...
Human carboxylesterase 2 (hCE-2) is a member of the serine esterase superfamily and is responsible for hydrolysis of a wide variety of xenobiotic and endogenous esters. hCE-2 also activates an anticancer drug, irinotecan (7-ethyl-10-[4-(1-piperidino)-1-piperidino]-carbonyloxycamptothecin, CPT-11), into its active metabolite, 7-ethyl-10-hydroxycamptothecin (SN-38). In this study, a comprehensive haplotype analysis of the CES2 gene, which encodes hCE-2, in a Japanese population was conducted. Using 21 single nucleotide polymorphisms (SNPs), including 4 nonsynonymous SNPs, 100C,T (Arg34Trp, *2), 424G,A (Val142Met, *3), 1A,T (Met1Leu, *5), and 617G,A (Arg206His, *6), and a SNP at the splice acceptor site of intron 8 (IVS8-2A,G, *4), 20 haplotypes were identified in 262 Japanese subjects. In 176 Japanese cancer patients who received irinotecan, associations of CES2 haplotypes and changes in a pharmacokinetic parameter, (SN-38 + SN-38G)/CPT-11 area under the plasma concentration curve (AUC) ratio, ...
The use of a prodrug, a conjugate of an active drug with a lipophilic substituent, is a good way of increasing the cutaneous absorption of a drug. However, the activity of dermal hydrolases has rarely been investigated in humans, or experimental animals. In the present study, we focused on the identification of rat dermal esterases and the hydrolysis of a prodrug during permeation across rat skin. We found that carboxylesterase (CES), especially the rat CES1 isozyme, Hydrolase A, is expressed in rat skin and that the hydrolysis of p-nitrophenyl acyl derivatives and caproyl-propranolol (PL) was 20-fold lower in the 9000g supernatant fraction of skin homogenate than in liver microsomes. A permeation study of caproyl-PL was performed in rat full-thickness and stripped skin using a flow-through diffusion cell. Caproyl-PL was easily partitioned into the stratum corneum and retained, not only in the stratum corneum, but also in viable epidermis and dermis. Caproyl-PL could barely be detected in the receptor
Recombinant Carboxylesterase 5A (CES5A) Protein (His tag). Species: Mouse (Murine). Source: Human Cells. Order product ABIN2008060.
Measurement of Carboxylesterase (CES) Activities (Masakiyo Hosokawa, Chiba University, Chiba, Japan and Tetsuo Satoh, Biomedical Research Institute, Chiba, Japan)
This gene encodes a member of the carboxylesterase large family. The family members are responsible for the hydrolysis or transesterification of various xenobiotics, such as cocaine and heroin, and endogenous substrates with ester, thioester, or amide bonds. They may participate in fatty acyl and cholesterol ester metabolism, and may play a role in the blood-brain barrier system. The protein encoded by this gene is the major intestinal enzyme and functions in intestine drug clearance. Alternatively spliced transcript variants have been found for this gene.[provided by RefSeq, Oct 2010 ...
CES2 Antibody (monoclonal) (M02), Mouse monoclonal antibody raised against a partial recombinant CES2. validated in WB, IHC, E (AT1499a), Abgent
A near-infrared fluorescent probe (DDAB) for highly selective and sensitive detection of carboxylesterase 2 (CE2) has been designed, synthesized, and systematically studied both in vitro and in vivo. Upon addition of CE2, the ester bond of DDAB could be rapidly cleaved and then release a near-infrared (NIR) fluorophore DDAO, which brings a remarkable yellow-to-blue color change and strong NIR fluo ...
The holy grail of pharmacology is the ability to specifically target the cell type responsible for a disease. Given that many drugs act intracellularly on targets that are active in most cells in the body, targeting specificity could be used to reduce unwanted side effects and toxicities. Needham et al. have investigated the development of a chemical platform that enhances the potency and delivery of small-molecule drugs to intracellular targets. Attaching a small esterase-sensitive chemical motif (ESM) that is selectively hydrolyzed by an intracellular carboxylesterase human carboxylesterase-1 (hCE1) allows small-molecule inhibitors to be released as charged, pharmacologically active drugs specifically in monocytes and macrophages. An ESM-linked histone deacetylase (HDAC) inhibitor showed impressive anticytokine and antiarthritic activity in hCE1 knock-in mice. The activity of the HDAC ESM (CHR4487) was demonstrated in human whole blood with anticytokine activity observed at concentrations ...
Landowski, Christopher P. et al Nucleoside Ester Prodrug Substrate Specificity of Liver Carboxylesterase. Journal of Pharmacology and Experimental Therapeutics 316.2 (2006): 572-580. Web. 29 Mar. 2020. ...
Where did the nylon-eating ability come from? Carboxylesterases are enzymes with broad substrate specificities; they can carry out a variety of reactions. Their binding pocket is large and can accommodate a lot of different substrates. They are promiscuous enzymes, in other words. Furthermore, the carboxylesterase reaction hydrolyzes a chemical bond similar to the one hydrolyzed by nylonase.. […]. From Kato et al. (1991):. Our studies demonstrated that among the 47 amino acids altered between the EII and EII proteins, a single amino acid substitution at position 181 was essential for the activity of 6-aminohexanoate-dimer hydrolase [nylonase] and substitution at position 266 enhanced the effect.. So. This is not the story of a highly improbable frame-shift producing a new functional enzyme. This is the story of a pre-existing enzyme with a low level of promiscuous nylonase activity, which improved its activity toward nylon by first one, then another selectable mutation. In other words ...
CES1 Human produced in Sf9 Insect cells is a single, glycosylated polypeptide chain containing 559 amino acids and having a molecular mass of 61.7kDa.
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As is the case for lipases and serine proteases, the catalytic apparatus of esterases involves three residues (catalytic triad): a serine, a glutamate or aspartate and a histidine. The sequence around the active site serine is well conserved and can be used as a signature pattern. As a second signature pattern, we selected a conserved region located in the N-terminal section and which contains a cysteine involved in a disulfide bond. Note: Human esterase-D, also a type-B carboxylesterase, does not seem to be evolutionary related. Expert(s) to contact by email: Sussman J ...
SWISS-MODEL Repository entry for A0A0D3QS99 (NOT1_XENLA), Palmitoleoyl-protein carboxylesterase notum1. Xenopus laevis (African clawed frog)
Complete information for ESD gene (Protein Coding), Esterase D, including: function, proteins, disorders, pathways, orthologs, and expression. GeneCards - The Human Gene Compendium
The PDB archive contains information about experimentally-determined structures of proteins, nucleic acids, and complex assemblies. As a member of the wwPDB, the RCSB PDB curates and annotates PDB data according to agreed upon standards. The RCSB PDB also provides a variety of tools and resources. Users can perform simple and advanced searches based on annotations relating to sequence, structure and function. These molecules are visualized, downloaded, and analyzed by users who range from students to specialized scientists.
Human CES7 full-length ORF (BAB71094.1, 1 a.a. - 525 a.a.) recombinant protein with GST-tag at N-terminal. (H00221223-P01) - Products - Abnova
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Looking for online definition of carboxylesterase 2 in the Medical Dictionary? carboxylesterase 2 explanation free. What is carboxylesterase 2? Meaning of carboxylesterase 2 medical term. What does carboxylesterase 2 mean?
Any risk of strain JPL-2, with the capacity of degrading fenoxaprop-P-ethyl (FE), was isolated from the soil of the wheat line of business and defined as JPL-2, FE -hydrolyzing carboxylesterase gene Introduction Fenoxaprop-ethylethyl-2-(4-((6-chloro-2-benzoxazolyl)oxy) phenoxy) propanoate) (FE) is normally a representative of aryloxyphenoxy propanoate (AOPP) herbicides. their matching acid type (Nie sp. B2 could degrade clodinafop propargyl (CF) to clodinafop acidity and 4-(4-Chloro-2-fluoro-phenoxy)-phenol (Singh, 2013). In summary, step one in the degradation of AOPP herbicides, which is normally distributed among these strains, may be the break down of the carboxylic acidity ester bond with a carboxylesterase. Far Thus, just two genes encoding this enzyme have already been cloned: from QDZ-1 and from sp. T1. Nevertheless, the features of FeH possess yet to become investigated. In this study: JPL-2, an aryloxyphenoxy propanoate (AOPP) herbicide-degrading strain of was cloned and expressed; and ...
Carboxylesterases hydrolyze numerous endogenous and foreign compounds with diverse structures. Humans and rodents express multiple forms of carboxylesterases, which share a high degree of sequence identity (∼70%). Alignment analyses locate in carboxylesterases several functional subsites such the catalytic triad as seen in acetylcholinesterase. The aim of this study was to determine among human and rodent carboxylesterases the immunorelatedness, overlapping substrate specificity, differential sensitivity to serine enzyme inhibitors, tissue distribution, and tumor-related expression. Six antibodies against whole carboxylesterases or synthetic peptides were tested for their reactivity toward 11 human or rodent recombinant carboxylesterases. The antibodies against whole proteins generally exhibited a broader cross-reactivity than the anti-peptide antibodies. All carboxylesterases hydrolyzed para-nitrophenylacetate and para-nitrophenylbutyrate. However, the relative activity varied markedly from ...
cell wall, extracellular region, acylglycerol lipase activity, carboxylic ester hydrolase activity, short-chain carboxylesterase activity, medium-chain fatty acid catabolic process, monoacylglycerol catabolic process, short-chain fatty acid catabolic process
https://doi.org/10.18632/oncotarget.23619 Dominique Lombardo, Françoise Silvy, Isabelle Crenon, Emmanuelle Martinez, Aurélie Collignon, Evelyne Beraud, Eric Mas
Five mouse anti-human butyrylcholinesterase (BChE) monoclonal antibodies bind tightly to native human BChE with nanomolar dissociation constants. Pairing analysis in the Octet system identified the monoclonal antibodies that bind to overlapping and independent epitopes on human BChE. The nucleotide and amino acid sequences of 4 monoclonal antibodies are deposited in GenBank. Our goal was to determine which of the 5 monoclonal antibodies recognize BChE in the plasma of animals. Binding of monoclonal antibodies 11D8, B2 18-5, B2 12-1, mAb2 and 3E8 to BChE in animal plasma was measured using antibody immobilized on Pansorbin cells and on Dynabeads Protein G. A third method visualized binding by the shift of BChE activity bands on nondenaturing gels stained for BChE activity. Gels were counterstained for carboxylesterase activity. The three methods agreed that B2 18-5 and mAb2 have broad species specificity, but the other monoclonal antibodies interacted only with human BChE, the exception being ...
Port Phillip Bay, Australia, is a large semi-closed bay with over four million people living in its catchment basin. The Bay receives waters from the Yarra River which drains the city of Melbourne, as well as receiving the discharges of sewage treatment plants and petrochemical and agricultural chemicals. A 1999 study demonstrated that fish inhabiting Port Phillip Bay showed signs of effects related to pollutant exposure despite pollution management practices having been implemented for over a decade. To assess the current health status of the fish inhabiting the Bay, a follow up survey was conducted in 2015. A suite of biomarkers of exposure and effects were measured to determine the health status of Port Phillip Bay sand flathead (Platycephalus bassensis), namely ethoxyresorufin-O-deethylase (EROD) activity, polycyclic aromatic hydrocarbons (PAH) biliary metabolites, carboxylesterase activity (CbE) and DNA damage (8-oxo-dG). The reduction in EROD activity in the present study suggests a ...
Cocaethylene (ethylbenzoylecgonine) is the ethyl ester of benzoylecgonine. It is structurally similar to cocaine, which is the methyl ester of benzoylecgonine. Cocaethylene is formed by the liver when cocaine and ethanol coexist in the blood. Cocaethylene is the byproduct of concurrent consumption of alcohol and cocaine as metabolized by the liver. Normally, metabolism of cocaine produces two primarily biologically inactive metabolites-benzoylecgonine and ecgonine methyl ester. The hepatic enzyme carboxylesterase is an important part of cocaines metabolism because it acts as a catalyst for the hydrolysis of cocaine in the liver, which produces these inactive metabolites. If ethanol is present during the metabolism of cocaine, a portion of the cocaine undergoes transesterification with ethanol, rather than undergoing hydrolysis with water, which results in the production of cocaethylene. cocaine + H2O → benzoylecgonine + methanol (with liver carboxylesterase 1) benzoylecgonine + ethanol → ...
Transcription and expression regulation of some individual cel genes (cel5A, cel5I, cel5D and cel44O) of Clostridium cellulolyticum were investigated. Unlike the cip-cel operon, these genes are transcribed as monocistronic units of transcription, except cel5D. The location of the transcription initiation sites was determined using RT-PCR and the mRNA 5′-end extremities were detected using primer extension experiments. Similarly to the cip-cel operon, cel5A and cel5I expressions are regulated by a carbon catabolite repression mechanism, whereas cel44O and cel5D expressions do not seem to be submitted to this regulation. The role of the putative transcriptional regulator GlyR2 in the regulation of cel5D expression was investigated. The recombinant protein GlyR2 was produced and was shown to bind in vitro to the cel5D and glyR2 promoter regions, suggesting that besides regulating its own expression, GlyR2 may regulate cel5D expression. To test this hypothesis in vivo, an insertional glyR2 mutant ...
A new ratiometric fluorescent probe derived from 2-(2-hydroxy-3-methoxyphenyl) benzothiazole (HMBT) has been developed for selective monitoring of human carboxylesterase 1 (hCE1). The probe is designed by introducing benzoyl moiety to HMBT. The prepared latent spectroscopic probe 1 displays satisfying stability under physiological pH conditions with very low background signal. Both the reaction phynotyping and chemical inhibition assays demonstrated that hCE1 mediated the specific cleavage of the carboxylic ester bond of probe 1 in human biological samples. The release of HMBT leads to a remarkable red-shifted emission in fluorescence spectrum (120 nm large emission shift). Furthermore, human cell-based assays show that probe 1 is cell membrane permeable, and it can be used for bioassay and cellular imaging of hCE1 activity in HepG2 cells. These findings lead to the development of a simple and sensitive fluorescent method for measurement of hCE1 activity in vitro or in living cells, in the ...
Background The main toxicity of irinotecan in advanced colorectal cancer (CRC) is delayed diarrhoea. Intestinal SN-38, released by deconjugation of the parent glucuronide excreted into the bile or produced in situ by intestinal carboxylesterase, is toxic to the intestinal epithelium. The canalicular transport of irinotecan and SN-38G is mediated by ABCC2 (MRP2) and ABCB1 (MDR1) which are both inhibited by ciclosporin. We tested whether irinotecan and ciclosporin was non-inferior for anti-cancer efficacy and superior for toxicity compared with single-agent irinotecan. Methods Six hundred and seventy-two patients with advanced, measurable CRC following prior fluoropyrimidine- containing chemotherapy were randomised to either irinotecan 3-weekly 350 mg/m 2 (or 300 mg/m 2 if age | 70 or performance status (PS) = 2) or 3-weekly irinotecan at 140 mg/m 2 (120 mg/m 2 if age | 70 or PS = 2) with ciclosporin 3 mg/kg t.d.s. for three days by mouth starting on the morning before irinotecan. The primary end
A scarce number of tests with terrestrial organisms are available for the category members of the Short Chain Alcohol Esters. As the category members of the Short Chain Alcohol Esters (SCAE) are readily biodegradable, ready degradation into metabolites is postulated. Fatty acids have been shown to have a low potential for bioaccumulation when considering biotransformation and the omnipresent activity of the enzyme carboxylesterase. Fatty acids and alcohols are the main metabolites of fatty acid esters. These components occur in soils naturally and are part of physiological pathways and can be used as energy source. The enzyme carboxylesterase is omnipresent in the environment. Bioaccumulation in organisms birds feed on are not expected. Furthermore, low toxicity to rats (repeated dose oral, NOAEL(90d) = 6000 mg/kg bw/d) was found. As a result, a low potential for secondary poisoning of birds is expected. Further testing should not be conducted due to animal welfare. ...
Non-P-glycoprotein-mediated multidrug-resistant C-A120 cells that overexpressed multidrug resistance protein (MRP) were 10.8- and 29.6-fold more resistant to 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (CPT-11) and SN-38, respectively, than parental KB-3-1 cells. To see whether MRP is involved in CPT-11 and SN-38 resistance,MRP cDNA was transfected into KB-3-1 cells. The transfectant, KB/MRP, which overexpressed MRP, was resistant to both CPT-11 and SN-38. 2-[4-Diphenylmethyl)-1-piperazinyl]ethyl-5-(trans-4,6-dimethyl-1,3,2-dioxaphosphorinan-2-yl)-2,6-dimethyl-4-(3-nitrophenyl)-3-pyridinecarboxylate P-oxide (PAK-104P) and MK571, which reversed drug resistance in MRP overexpressing multidrug-resistant cells, significantly increased the sensitivity of C-A120 and KB/MRP cells, but not of KB-3-1 cells, to CPT-11 and SN-38. The accumulation of both CPT-11 and SN-38 in C-A120 and KB/MRP cells was lower than that in KB-3-1 cells. The treatment with 10 μM PAK-104P increased the ...
Irinotecan (CPT-11) is now widely used as the first-line chemotherapy for mCRC. There were 4 key enzymes for CPT-11 metabolizing, CYP3A4, UDP-glucuronosyltransferase, carboxylesterase(CES), and ATP-binding cassette (ABC) transporters. Genetic variations of those enzymes may cause the heterogeneity in safety and efficacy of CPT-11. The aim of this study is to figure out the correlation between the genetic polymorphism and the drug response ...
4133 Individualized, tailored drug therapy is an important direction for development of cancer treatment. Currently, irinotecan (CPT-11) has been widely used in a variety of human cancers. Occasionally, occurrence of unexpected severe toxicities (Gr. 4 neutropenia, Gr. 4 diarrhea, sepsis) of irinotecan may hinder its clinical use. Irinotecan is activated by carboxylesterase to SN-38 with its antitumor activity, and which has been associated with the severe diarrheal episodes as a result of the direct enteric injury. SN-38 undergoes glucuronide conjugation and inactivation by UDP-glucuronosyl transferase 1A1 (UGT1A1) isoform to form the inactive SN-38 glucuronide (SN-38G). Among the UGT1A1 polymorphism, the UGT1A1*28 genotype, with (TA)7TAA change of UGT1A1 gene promoter, had probable important implications to predict and monitor clinical toxicity induced by irinotecan. We tried to analyze the polymorphisms in UGT1A1*28 genotype as predictors of severe toxic events occurring after irinotecan ...
Carboxylesterase is a serine-dependent esterase with wide substrate specificity. The enzyme is involved in the detoxification of XENOBIOTICS and the activation of ester and of amide PRODRUGS. . ...
Le Registre public des espèces en péril est une source complète dinformation publique sur des espèces en péril au Canada et la Loi sur les espèces en péril (LEP).
ISBN 9789898066343 - Get FREE shipping offers and dollar off coupons with our price comparison for Os Ces Nunca Mentem sobre o Amor Reflexes acerca do mundo emocional dos ces - ISBN 9789898066343, 9898066342.
Samsung's latest Creative Lab projects are shaping up to be some of their most innovative ideas yet. The projects, which will be shown off at CES next week, include the S-Ray portable directional speaker, the GoBreath lung damage recovery device…
Learn more about Parto por cesárea at Grand Strand Medical Center DefiniciónRazones para realizar el procedimientoPosibles complicaciones¿Qué...
CES 2017 took place from Jan 3-8th in Las Vegas. This years show was crazy big with interesting technology that has some unique potential.
Iriarte Corredora, Venta y arriendo de propiedades, administración de propiedades en arriendo, tasaciones de bienes raíces y terrenos.
Iriarte Corredora, Venta y arriendo de propiedades, administración de propiedades en arriendo, tasaciones de bienes raíces y terrenos.
Selim, Samy; Hagagy, Nashwa (2016-03-01). "Genome sequence of carboxylesterase, carboxylase and xylose isomerase producing ... and carboxylesterase. Other genes coding for biosynthesis of peptides and secondary metabolites were also detected. ...
Carboxylesterase, an enzyme that catalyzes the reaction between a carboxylic ester and water Caspian Engineers Society Center ...
Dermed dannes metabolitten ritalinsyre.[24] Hydrolysen er katalyseret af enzymet carboxylesterase 1 (CES1), der primært findes ... "Methylphenidate is stereoselectively hydrolyzed by human carboxylesterase CES1A1". J Pharmacol Exp Ther. 310 (2): 469-76. PMID ...
Ohara, Kazuhiro; Unno, Hideaki; Oshima, Yasuhiro «Structural Insights into the Low pH Adaptation of a Unique Carboxylesterase ...
The metabolites are excreted in the urine.[5] DEP is metabolized by carboxyl esterase, which is synthesized in the human liver ...
carboxylesterase activity. · cholinesterase activity. · cholinesterase activity. · protein binding. · collagen binding. · ...
carboxylesterase 2 (intestine, liver). intestinal carboxylesterase; liver carboxylesterase-2. methylumbelliferyl-acetate ... Carboxylesterase-2-Selective Two-Photon Ratiometric Probe Reveals Decreased Carboxylesterase-2 Activity in Breast Cancer Cells. ... Title: Carboxylesterase-2-Selective Two-Photon Ratiometric Probe Reveals Decreased Carboxylesterase-2 Activity in Breast Cancer ... CES2 carboxylesterase 2 [Homo sapiens] CES2 carboxylesterase 2 [Homo sapiens]. Gene ID:8824 ...
Liver carboxylesterase 1 isoform a, CES1, ACAT, CE-1, CEH, CES2, hCE-1, HMSE, HMSE1, PCE-1, REH, SES1, TGH, Acyl-coenzyme A: ...
Measurement of Carboxylesterase (CES) Activities (Masakiyo Hosokawa, Chiba University, Chiba, Japan and Tetsuo Satoh, ... Measurement of Carboxylesterase (CES) Activities (Masakiyo Hosokawa, Chiba University, Chiba, Japan and Tetsuo Satoh, ... cDNA cloning, characterization and stable expression of novel human brain carboxylesterase. F.E.B.S. Lett. 458:17‐22. ... Differences in the induction of carboxylesterase isozymes in rat liver microsomes by perfluorinated fatty acids. Xenobiotica. ...
We found that carboxylesterase (CES), especially the rat CES1 isozyme, Hydrolase A, is expressed in rat skin and that the ... Keywords: prodrug; skin permeation; hydrolysis; carboxylesterase prodrug; skin permeation; hydrolysis; carboxylesterase ►▼ ... Involvement of Carboxylesterase in Hydrolysis of Propranolol Prodrug during Permeation across Rat Skin. Teruko Imai * , Yuko ... We found that carboxylesterase (CES), especially the rat CES1 isozyme, Hydrolase A, is expressed in rat skin and that the ...
Recombinant Carboxylesterase 5A (CES5A) Protein (His tag). Species: Mouse (Murine). Source: Human Cells. Order product ... Carboxylesterase 5A (CES5A) (Extracellular Domain), (AA 1-556) (Active) protein (... Carboxylesterase 5A (CES5A) (Extracellular ... Carboxylesterase 5A (CES5A) (Extracellular Domain), (AA 1-556) (Active) protein (His tag) Read product details ... Carboxylesterase 5A (CES5A) (Extracellular Domain), (AA 1-556) (Active) protein (His tag) Read product details ...
Silencing carboxylesterase 1 in human THP-1 macrophages perturbs genes regulated by PPARγ/RXR and RAR/RXR: down-regulation of ... Silencing carboxylesterase 1 in human THP-1 macrophages perturbs genes regulated by PPARγ/RXR and RAR/RXR: down-regulation of ... Silencing carboxylesterase 1 in human THP-1 macrophages perturbs genes regulated by PPARγ/RXR and RAR/RXR: down-regulation of ... Silencing carboxylesterase 1 in human THP-1 macrophages perturbs genes regulated by PPARγ/RXR and RAR/RXR: down-regulation of ...
Recombinant Protein and Liver carboxylesterase Antibody at MyBioSource. Custom ELISA Kit, Recombinant Protein and Antibody are ... Liver carboxylesterase. Liver carboxylesterase ELISA Kit. Liver carboxylesterase Recombinant. Liver carboxylesterase Antibody. ... Liver carboxylesterase 1. Liver carboxylesterase 1 ELISA Kit. Liver carboxylesterase 1 Recombinant. Liver carboxylesterase 1 ... Liver carboxylesterase 2. Liver carboxylesterase 2 ELISA Kit. Liver carboxylesterase 2 Recombinant. Liver carboxylesterase 2 ...
carboxylesterase; esters; flavonoids; humans; hydrolysis; xenobiotics. Abstract:. ... Human carboxylesterase 1 (hCE1) is a key ... You searched for: Author Hou, Jie Remove constraint Author: Hou, Jie Subject carboxylesterase Remove constraint Subject: ... 1. Rational Design of a Long-Wavelength Fluorescent Probe for Highly Selective Sensing of Carboxylesterase 1 in Living Systems ... 6. A highly selective marker reaction for measuring the activity of human carboxylesterase 1 in complex biological samples ...
Carboxylesterase 1 (CES1) has recently been suggested to play a role in lipolysis. Our aim was to Study the regulation of CES1 ... 2009) Regulation of carboxylesterase 1 (CES1) in human adipose tissue. Biochemical and Biophysical Research Communications, Vol ...
Palmitoleoyl-protein carboxylesterase notum1. Xenopus laevis (African clawed frog) ... Palmitoleoyl-protein carboxylesterase notum1 UniProtKBInterProInteractive Modelling. 488 aa; Sequence (Fasta) ...
liver carboxylesterase 1. Names. acyl coenzyme A:cholesterol acyltransferase. brain carboxylesterase hBr1. carboxylesterase 1 ( ... carboxylesterase 2 (liver). cholesteryl ester hydrolase. cocaine carboxylesterase. egasyn. human monocyte/macrophage serine ... CES1 carboxylesterase 1 [Homo sapiens] CES1 carboxylesterase 1 [Homo sapiens]. Gene ID:1066 ... Title: Age-Dependent Human Hepatic Carboxylesterase 1 (CES1) and Carboxylesterase 2 (CES2) Postnatal Ontogeny. ...
Proteins matched: CARBOXYLESTERASE_B_1 (PS00122) This signature appears in the following proteins: Showing 1 to 20 of 27967 ... Carboxylesterase patB. Aspergillus clavatus (strain ATCC 1007 / CBS 513.65 / DSM 816 / NCTC 3887 / NRRL 1). Loading... ...
Compare carboxylesterase 1G ELISA Kits from leading suppliers on Biocompare. View specifications, prices, citations, reviews, ... carboxylesterase 1G ELISA Kits. The ELISA (enzyme-linked immunosorbent assay) is a widely used application for detecting and ... Your search returned 5 carboxylesterase 1G ELISA ELISA Kit across 4 suppliers. ...
Quax, W. J., & Broekhuizen, C. P. (1994). Development of a new Bacillus carboxyl esterase for use in the resolution of chiral ... 2008). Application of carboxylesterase activity in environmental monitoring and toxicity identification protocol (TIEs). ... Redinbo, M. R., Bencharit, S., & Potter, P. M. (2003). Human carboxylesterase 1: From drug metabolism to drug discovery. ... 1997). Purification and cloning of a broad substrate specificity human liver carboxylesterase that catalyzes the hydrolysis of ...
Maxwell D.M., Brecht K., Saxena A., Feaster S., Doctor B.P. (1998) Comparison of Cholinesterases and Carboxylesterase as ... and carboxylesterase (CaE), to provide protection against OP compounds has been demonstrated in rodents as well as nonhuman ...
Carboxylesterase that acts as a key negative regulator of the Wnt signaling pathway by specifically mediating ...
PS00122 CARBOXYLESTERASE_B_1, 1 hit. PS00941 CARBOXYLESTERASE_B_2, 1 hit. ... PS00122 CARBOXYLESTERASE_B_1, 1 hit. PS00941 CARBOXYLESTERASE_B_2, 1 hit. ... Carboxylesterase 1FAdd BLAST. 544. Amino acid modifications. Feature key. Position(s). DescriptionActions. Graphical view. ... Carboxylesterase 1FImported. ,p>Manually validated information which has been imported from another database.,/p> ,p>,a href="/ ...
Browse our carboxylesterase 4A product catalog backed by our Guarantee+. ... Diseases related to carboxylesterase 4A. Discover more about diseases related to carboxylesterase 4A.. Confusion. ... Bioinformatics Tool for carboxylesterase 4A. Discover related pathways, diseases and genes to carboxylesterase 4A. Need help? ... carboxylesterase 4A products available through Novus Biologicals. ...
Browse our Carboxylesterase 1/CES1 Protein catalog backed by our Guarantee+. ... Carboxylesterase 1/CES1 Proteins. We offer Carboxylesterase 1/CES1 Peptides and Carboxylesterase 1/CES1 Proteins for use in ... Our Carboxylesterase 1/CES1 Peptides and Carboxylesterase 1/CES1 Proteins can be used in a variety of model species: Mouse. Use ... Each Carboxylesterase 1/CES1 Peptide and Carboxylesterase 1/CES1 Protein is fully covered by our Guarantee+, to give you ...
carboxylesterase 2E Ces5 carboxylesterase 5 Nomenclature updated to reflect human and mouse nomenclature. 1299863. APPROVED. ... carboxylesterase 5 Loc192257 phenobarbital-inducible carboxylesterase (liver) Symbol and Name updated. 1299863. APPROVED. ... carboxylesterase 5; carboxylic ester hydrolase; Ces5; Loc192257; phenobarbital-inducible carboxylesterase (liver); pyrethroid ... phenobarbital-inducible carboxylesterase (liver) Symbol and Name status set to provisional. 70820. PROVISIONAL. ...
carboxylesterase 2 , carboxylesterase 3 (brain) , esterase 31 , liver carboxylesterase 31 homolog , carboxylesterase 3 ... Carboxylesterase 3 (CES3) Antigen-Profil Beschreibung des Gens This gene encodes a member of the carboxylesterase large family ... anti-Carboxylesterase 3 (CES3) Antikörper. Bezeichnung:. anti-Carboxylesterase 3 Antikörper (CES3). Auf www.antikoerper-online. ... Weitere Antikörper gegen Carboxylesterase 3 Interaktionspartner. Human Carboxylesterase 3 (CES3) Interaktionspartner * This ...
Phospholipase/CarboxylesteraseImported. ,p>Information which has been imported from another database using automatic procedures ... ehrcj-q3yss3 LYsophospholipase_carboxylesterase. Protocols and materials databases. Structural Biology Knowledgebase. Search... ... tr,Q3YSS3,Q3YSS3_EHRCJ Phospholipase/Carboxylesterase OS=Ehrlichia canis (strain Jake) OX=269484 GN=Ecaj_0181 PE=4 SV=1 ...
Here, we present the silica encapsulation of human drug metabolism enzyme carboxylesterase 1 (hCE1) in the presence of a range ... Immobilization of active human carboxylesterase 1 in biomimetic silica nanoparticles. Authors. *. Jonathan S. Edwards,. *Dept. ...
What is carboxylesterase 2? Meaning of carboxylesterase 2 medical term. What does carboxylesterase 2 mean? ... Looking for online definition of carboxylesterase 2 in the Medical Dictionary? carboxylesterase 2 explanation free. ... redirected from carboxylesterase 2) CES1. A gene on chromosome 16q22.2 that encodes a member of the carboxylesterase family, ... Carboxylesterase 2 , definition of carboxylesterase 2 by Medical dictionary https://medical-dictionary.thefreedictionary.com/ ...
Compare and order Carboxylesterase 3 ELISA Kits. View citations, images, detection ranges, sensitivity, prices and more. ... carboxylesterase 2 , carboxylesterase 3 (brain) , esterase 31 , liver carboxylesterase 31 homolog , carboxylesterase 3 ... This gene encodes a member of the carboxylesterase large family. The family members are responsible for the hydrolysis or ...
Nucleoside Ester Prodrug Substrate Specificity of Liver Carboxylesterase. Christopher P. Landowski, Philip L. Lorenzi, Xueqin ... Nucleoside Ester Prodrug Substrate Specificity of Liver Carboxylesterase. Christopher P. Landowski, Philip L. Lorenzi, Xueqin ... Nucleoside Ester Prodrug Substrate Specificity of Liver Carboxylesterase. Christopher P. Landowski, Philip L. Lorenzi, Xueqin ... Nucleoside Ester Prodrug Substrate Specificity of Liver Carboxylesterase Message Subject (Your Name) has forwarded a page to ...
... investigate the herb-drug interaction of Clopidogrel and XST by modulation of the pharmacodynamics and liver Carboxylesterase ... Y. Suzaki, N. Uemura, M. Takada et al., "The effect of carboxylesterase 1 (CES1) polymorphisms on the pharmacokinetics of ... T. Kabeya, W. Matsumura, T. Iwao, M. Hosokawa, and T. Matsunaga, "Functional analysis of carboxylesterase in human induced ... T. Maruichi, T. Fukami, M. Nakajima, and T. Yokoi, "Transcriptional regulation of human carboxylesterase 1A1 by nuclear factor- ...
carboxylesterase 2F. Synonyms: 2310038E17Rik. Gene nomenclature, locus information, and GO, OMIM, and PMID associations are ...
... synthesized and applied for the highly selective and sensitive fluorescence sensing of carboxylesterase in live cells, sera and ... Upon addition of carboxylesterase, the latent probe could be easily hydrolyzed to liberate the fluorophore hydroxy hemicyanine ... A red lysosome-targeted fluorescent probe for carboxylesterase detection and bioimaging H. Zhou, J. Tang, J. Zhang, B. Chen, J ... The newly developed probe was successfully used to monitor and image carboxylesterase activity in complex biological samples ...
Carboxylesterase Assays. General carboxylesterase activity was determined spectrophotometrically using the carboxylesterase ... carboxylesterase activity remaining) and compound 4 selectively inhibited rCE (2% carboxylesterase activity remaining) compared ... Schematic Figure Showing Carboxylesterase-Catalyzed Metabolism of o-NPA and CPT-11. o-NPA is a general esterase substrate (Fig ... Inhibition of carboxylesterase-mediated catalysis of CPT-11. A, enzymes were incubated with 5 μmol/L CPT-11 with 0.5, 5.0, or ...
The kit uses the proprietary substrate for the quantification of Carboxylesterase (CE)... ... plate-based fluorometric assay for measuring Carboxylesterase activity in biological samples. ... BioVisions Carboxylesterase Activity Assay Kit is a simple, rapid, ... Human Carboxylesterase 1 (E.C. 3.1.1.1, CES1, hCE1, CES1b or CES1A1) is a α,β-serine hydrolase expressed in most tissues with ...
Characterization of CPT-11 Hydrolysis by Human Liver Carboxylesterase Isoforms hCE-1 and hCE-2. Rod Humerickhouse, Karen ... We characterized the hydrolysis of CPT-11 by two recently identified human carboxylesterase (hCE) enzymes, hCE-1 and hCE-2. Km ... Kojima A., Hackett N. R., Ohwada A., Crystal R. G. In vivo human carboxylesterase cDNA gene transfer to activate the prodrug ... Zhang J., Burnell J. C., Dumaual N., Bosron W. F. Binding and hydrolysis of meperidine by human liver carboxylesterase hCE-1. J ...
Several mouse carboxylesterase (CES) isozymes have been identified, but information about their roles in drug metabolism is ... Identification of di-(2-ethylhexyl) phthalate-induced carboxylesterase 1 in C57BL/6 mouse liver microsomes: purification, cDNA ...
Methods: The distribution of the carboxylesterase-1 (CES1) mRNA in human eye was analyzed by RT-PCR. Expression levels of CES1 ... The aim of this study was to examine whether human carboxylesterase 1 (CES1) has retinyl ester hydrolyzing activity and is ... Human carboxylesterase 1 is expressed in retinal pigment epithelium and hydrolyzes retinyl ester ... Human carboxylesterase 1 is expressed in retinal pigment epithelium and hydrolyzes retinyl ester ...
  • Human carboxylesterase 2 (CES2A), one of the most abundant hydrolases distributed in human small intestine and colon, play key roles in the hydrolysis of a wide range of prodrugs and other esters. (usda.gov)
  • 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. (usda.gov)
  • This study examines the steady-state kinetics of recombinant human carboxylesterase isozymes carboxylesterase (CES) 1A1, CES2, and CES3 for hydrolysis of capecitabine with a liquid chromatography/mass spectroscopy assay. (elsevier.com)
  • Herein, a practical and highly specific fluorescent probe for carboxylesterase 1 (CES1) was rationally designed using meso-carboxyl-BODIPY as the basic fluorophore based on the substrate preference and catalytic properties of CES1. (usda.gov)
  • Carboxylesterase 2 as a Determinant of Response to Irinotecan and Neoadjuvant FOLFIRINOX Therapy in Pancreatic Ductal Adenocarcinoma. (nih.gov)
  • Tissue-infiltrating plasma cells are an important source of carboxylesterase 2 contributing to the therapeutic efficacy of prodrugs. (nih.gov)
  • Functional analysis of carboxylesterase in human induced pluripotent stem cell-derived enterocytes. (nih.gov)
  • This study aimed to investigate the inhibitory effects of ethanol extract from WMR against human carboxylesterase 2 (hCE2), as well as to identity and character natural hCE2 inhibitors in this herbal. (usda.gov)
  • Several mouse carboxylesterase (CES) isozymes have been identified, but information about their roles in drug metabolism is limited. (sigmaaldrich.com)
  • These results are the first experimental evidence confirming the capability of bacterial carboxylesterase to hydrolyse cocaine into its main metabolites, therefore opening up the possibility to use these enzymes in numerous biotechnological applications in addition to a cocaine biosensor. (springer.com)
  • CPT-11) is a prodrug activated by carboxylesterase enzymes. (aacrjournals.org)
  • Romano, Diego 2018-01-01 00:00:00 AbbreviationsBCEBacillus coagulans carboxylesterase 1CDcircular dichroismEtOAcethyl acetatehMGLhuman monoacylglycerol lipaseIPG1,2‐O‐isopropylideneglycerolpNPAp‐nitrophenyl acetateIntroductionCarboxylester hydrolases (EC 3.1.1.1) are enzymes that catalyze the cleavage or formation of carboxyl ester bonds, being often classified as esterases and lipases, based on experimental data and theoretical hypotheses. (deepdyve.com)
  • Materials and methods Hepatic enzymes that metabolize 123 I-iomazenil were identified by thin-layer chromatography in mouse liver homogenates with bis(4-nitrophenyl) phosphate (BNPP) inhibitor for carboxylesterase enzymes and nicotinamide adenine dinucleotide phosphate (NADPH) generator for cytochrome P450 enzymes. (ovid.com)
  • Carboxylesterase inhibitors may play a role in improved efficacy of compounds inactivated by this class of enzymes and/or reduce the toxicity of agents that are activated by these enzymes. (cyprotex.com)
  • Cyprotex's carboxylesterase inhibition assay identifies if your compound is an inhibitor of the carboxylesterase (CE) isoform, hCE1, using hCE1-b and hCE1-c recombinant enzymes. (cyprotex.com)
  • This revealed 193 subsystems including several enzymes encoding genes for carboxylase, cellulase and xylanase enzymes, xylose isomerase, and carboxylesterase. (wikipedia.org)
  • Mouse blood contains four esterases that detoxify organophosphorus compounds: carboxylesterase, butyrylcholinesterase, acetylcholinesterase, and paraoxonase-In contrast human blood contains the latter three enzymes but not carboxylesterase. (geoscience.net)
  • Zusätzlich bieten wir Ihnen Carboxylesterase 3 Proteine (6) und Carboxylesterase 3 Kits (3) und viele weitere Produktgruppen zu diesem Protein an. (antikoerper-online.de)
  • The purified BioHx protein displayed carboxylesterase activity, and it was most active on p -nitrophenyl esters of fatty acids substrate with a short acyl chain (C4). (biomedcentral.com)
  • This gene encodes a member of the carboxylesterase large family. (nih.gov)
  • A gene on chromosome 16q22.2 that encodes a member of the carboxylesterase family, which hydrolyse or transesterify xenobiotics (e.g., cocaine and heroin) and endogenous substrates with ester, thioester or amide bonds. (thefreedictionary.com)
  • Mutations of this gene cause carboxylesterase 1 deficiency. (nih.gov)
  • Effects of Genetic Variants on Carboxylesterase 1 Gene Expression, and Clopidogrel Pharmacokinetics and Antiplatelet Effects. (nih.gov)
  • Rasmussen, HB , Madsen, MB , Hansen, PR & INDICES Consortium 2017, ' Nomenclature for alleles of the human carboxylesterase 1 gene ' Pharmacogenetics and Genomics , vol. 27, no. 2, pp. 78-80. (regionh.dk)
  • The present study was to investigate the herb-drug interaction of Clopidogrel and XST by modulation of the pharmacodynamics and liver Carboxylesterase 1A(CES1A) metabolism. (hindawi.com)
  • During clopidogrel metabolism [ 11 , 12 ], carboxylesterase 1A (CES1A) begins by hydrolyzing approximately 85-90% of the prodrug to an inactive carboxylic acid metabolite [ 13 ]. (hindawi.com)
  • Results From the in-vitro metabolism of 123 I-iomazenil using BNPP, the enzyme converting 123 I-iomazenil to 123 I-R-COOH was identified as carboxylesterase, and that converting 123 I-iomazenil to M2 was identified as cytochrome P450 in experiments with and without an NADPH generator. (ovid.com)
  • Carboxylesterase (CE) inhibition is a non-CYP mediated metabolism assay within our portfolio of in vitro ADME screening services. (cyprotex.com)
  • Metabolism of pethidine to pethidinic acid is carried out mainly by the carboxylesterase enzyme hCE-1 in the liver, and since the activity of this enzyme can vary between individuals, the rate and extent of pethidinic acid production can vary. (wikipedia.org)
  • 1 Hatfield MJ and Potter PM (2011) Carboxylesterase inhibitors. (cyprotex.com)
  • This study aimed to investigate the inhibitory effects of ethanol extract from WMR against human carboxylesterase 2 (hCE2), as well as to identity and character natural hCE2 inhibitors in this herbal. (usda.gov)
  • We demonstrate that human plasma contains no carboxylesterase (EC 3.1.1.1), in contrast to mouse, rat, rabbit, horse, cat, and tiger that have high amounts of plasma carboxylesterase. (nebraska.edu)
  • Our goal was to determine the effect of plasma carboxylesterase deficiency on response to sublethal doses of 1 organophosphorus toxicants and one carbamate pesticide. (geoscience.net)
  • Homozygous plasma carboxylesterase deficient ES1-/- mice and wild-type littermates were observed for toxic signs and changes in body temperature after treatment with a single sublethal dose of toxicant. (geoscience.net)
  • Inhibition of plasma acetylcholinesterase, butyrylcholinesterase, and plasma carboxylesterase was measured. (geoscience.net)
  • Also known as Liver carboxylesterase 4 (Carboxyesterase ES-4) (Kidney microsomal carboxylesterase) (Microsomal palmitoyl-CoA hydrolase). (mybiosource.com)
  • Native polyacrylamide gel electrophoresis showed carboxylesterase (CES) to be the most abundant hydrolase in the liver and small intestine of humans, monkeys, dogs, rabbits and rats. (semanticscholar.org)
  • A synthetic peptide derived from the C terminus of human Liver Carboxylesterase 1. (abcam.cn)
  • Purification and characterization of a human liver cocaine carboxylesterase that catalyzes the production of benzoylecgonine and the formation of cocaethylene from alcohol and cocaine. (proteopedia.org)
  • Identification of di-(2-ethylhexyl) phthalate-induced carboxylesterase 1 in C57BL/6 mouse liver microsomes: purification, cDNA cloning, and baculovirus-mediated expression. (sigmaaldrich.com)
  • It was concluded that carboxylesterase in mouse plasma protects from high toxicity agents, but the amount of carboxylesterase in plasma is too low to protect from low toxicity compounds that require high doses to inhibit acetylcholinesterase. (geoscience.net)
  • Conclusion 123 I-iomazenil whole-body imaging has good possibility of direct measurement of hepatic carboxylesterase activity as accumulation of 123 I-R-COOH in the gall bladder through bile and in the bladder through urine. (ovid.com)
  • Role of geraniol against lead acetate-mediated hepatic damage and their interaction with liver carboxylesterase activity in rats. (ktu.edu.tr)
  • Carboxylesterase 1c (CES1c) is responsible for linker-drug instability and poor pharmacokinetics (PK) of several antibody-drug conjugates (ADCs) in mouse, but not in monkey or human. (aacrjournals.org)
  • In this study, a new red lysosome-targeted fluorescence off-on probe has been rationally designed, synthesized and applied for the highly selective and sensitive fluorescence sensing of carboxylesterase in live cells, sera and tissues. (rsc.org)
  • We have cloned, overexpressed, purified, and crystallized a carboxylesterase from the kiwifruit species Actinidia eriantha (AeCXE1). (edu.au)
  • Carboxylesterase-2-Selective Two-Photon Ratiometric Probe Reveals Decreased Carboxylesterase-2 Activity in Breast Cancer Cells. (nih.gov)
  • The newly developed probe was successfully used to monitor and image carboxylesterase activity in complex biological samples such as serum, live cells and tissues. (rsc.org)
  • Inhibition of this carboxylesterase probably presents a major source for altered therapeutic activity of these medicines if co-administered with orlistat. (uri.edu)
  • Physiologically based pharmacokinetic modeling of impaired carboxylesterase-1 activity: effects on oseltamivir disposition. (cdc.gov)