carboxylesterase

Summary

Summary: 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.

Top Publications

  1. ncbi Identification of the cytosolic carboxylesterase catalyzing the 5'-deoxy-5-fluorocytidine formation from capecitabine in human liver
    Toshiki Tabata
    Drug Metabolism and Toxicology, Division of Pharmaceutical Sciences, Graduate School of Medical Science, Kanazawa University, Kakuma machi, Kanazawa 920 1192, Japan
    Drug Metab Dispos 32:1103-10. 2004
  2. pmc Structure and function of an insect α-carboxylesterase (αEsterase7) associated with insecticide resistance
    Colin J Jackson
    Research School of Chemistry, Australian National University, Canberra, ACT 0200, Australia
    Proc Natl Acad Sci U S A 110:10177-82. 2013
  3. ncbi Age- and sex-related expression and activity of carboxylesterase 1 and 2 in mouse and human liver
    Hao Jie Zhu
    Department of Pharmaceutical and Biomedical Sciences, Medical University of South Carolina, 73 Ashley Avenue, Charleston, SC 29425, USA
    Drug Metab Dispos 37:1819-25. 2009
  4. pmc Correlation between carboxylesterase alleles and insecticide resistance in Culex pipiens complex from China
    Yangyang Liu
    Plant Protection College, Shandong Agricultural University, Tai an, Shandong, 271018 China
    Parasit Vectors 4:236. 2011
  5. pmc A single amino acid substitution converts a carboxylesterase to an organophosphorus hydrolase and confers insecticide resistance on a blowfly
    R D Newcomb
    Commonwealth Scientific and Industrial Research Organisation, Division of Entomology, G P O Box 1700, Canberra, Australian Capital Territory 2601, Australia
    Proc Natl Acad Sci U S A 94:7464-8. 1997
  6. pmc Characterization of a novel thermostable carboxylesterase from Geobacillus kaustophilus HTA426 shows the existence of a new carboxylesterase family
    Silvia Montoro-García
    Department of Biochemistry and Molecular Biology A, Faculty of Biology, University of Murcia, Campus Espinardo, E30011 Murcia, Spain
    J Bacteriol 191:3076-85. 2009
  7. ncbi Testing the evolvability of an insect carboxylesterase for the detoxification of synthetic pyrethroid insecticides
    Chris W Coppin
    CSIRO Ecosystem Sciences, Canberra, ACT 2601, Australia
    Insect Biochem Mol Biol 42:343-52. 2012
  8. ncbi Hydrolysis of organophosphorus insecticides by in vitro modified carboxylesterase E3 from Lucilia cuprina
    R Heidari
    CSIRO Entomology, GPO Box 1700, Canberra, ACT 2601, Australia
    Insect Biochem Mol Biol 34:353-63. 2004
  9. pmc A carboxylesterase, Esterase-6, modulates sensory physiological and behavioral response dynamics to pheromone in Drosophila
    Thomas Chertemps
    Universite Pierre et Marie Curie, UMR, Physiologie de l Insecte, Signalisation et Communication, Paris, France
    BMC Biol 10:56. 2012
  10. pmc Cloning of a novel pyrethroid-hydrolyzing carboxylesterase gene from Sphingobium sp. strain JZ-1 and characterization of the gene product
    Bao zhan Wang
    Key Laboratory of Microbiological Engineering of Agricultural Environment, Ministry of Agriculture, Life Sciences College of Nanjing Agricultural University, Nanjing, Jiangsu 210095, People s Republic of China
    Appl Environ Microbiol 75:5496-500. 2009

Detail Information

Publications249 found, 100 shown here

  1. ncbi Identification of the cytosolic carboxylesterase catalyzing the 5'-deoxy-5-fluorocytidine formation from capecitabine in human liver
    Toshiki Tabata
    Drug Metabolism and Toxicology, Division of Pharmaceutical Sciences, Graduate School of Medical Science, Kanazawa University, Kakuma machi, Kanazawa 920 1192, Japan
    Drug Metab Dispos 32:1103-10. 2004
    Capecitabine, a prodrug of 5-fluorouracil, is first metabolized to 5'-deoxy-5-fluorocytidine (5'-DFCR) by carboxylesterase (CES), which is mainly expressed in microsomes...
  2. pmc Structure and function of an insect α-carboxylesterase (αEsterase7) associated with insecticide resistance
    Colin J Jackson
    Research School of Chemistry, Australian National University, Canberra, ACT 0200, Australia
    Proc Natl Acad Sci U S A 110:10177-82. 2013
    ....
  3. ncbi Age- and sex-related expression and activity of carboxylesterase 1 and 2 in mouse and human liver
    Hao Jie Zhu
    Department of Pharmaceutical and Biomedical Sciences, Medical University of South Carolina, 73 Ashley Avenue, Charleston, SC 29425, USA
    Drug Metab Dispos 37:1819-25. 2009
    b>Carboxylesterase (CES) 1 and CES2 are two major hepatic hydrolases responsible for the metabolism of numerous endogenous and exogenous compounds...
  4. pmc Correlation between carboxylesterase alleles and insecticide resistance in Culex pipiens complex from China
    Yangyang Liu
    Plant Protection College, Shandong Agricultural University, Tai an, Shandong, 271018 China
    Parasit Vectors 4:236. 2011
    ..Six resistant carboxylesterase alleles (Ester) were recorded previously and sometimes co-existed in one field population, representing a ..
  5. pmc A single amino acid substitution converts a carboxylesterase to an organophosphorus hydrolase and confers insecticide resistance on a blowfly
    R D Newcomb
    Commonwealth Scientific and Industrial Research Organisation, Division of Entomology, G P O Box 1700, Canberra, Australian Capital Territory 2601, Australia
    Proc Natl Acad Sci U S A 94:7464-8. 1997
    Resistance to organophosphorus (OP) insecticides is associated with decreased carboxylesterase activity in several insect species...
  6. pmc Characterization of a novel thermostable carboxylesterase from Geobacillus kaustophilus HTA426 shows the existence of a new carboxylesterase family
    Silvia Montoro-García
    Department of Biochemistry and Molecular Biology A, Faculty of Biology, University of Murcia, Campus Espinardo, E30011 Murcia, Spain
    J Bacteriol 191:3076-85. 2009
    ..However, this carboxylesterase showed no more than 17% sequence identity with the closest members in the eight families of microbial ..
  7. ncbi Testing the evolvability of an insect carboxylesterase for the detoxification of synthetic pyrethroid insecticides
    Chris W Coppin
    CSIRO Ecosystem Sciences, Canberra, ACT 2601, Australia
    Insect Biochem Mol Biol 42:343-52. 2012
    ..to test to what extent it is possible to genetically enhance the pyrethroid hydrolytic activity of the E3 carboxylesterase from the blowfly Lucilia cuprina...
  8. ncbi Hydrolysis of organophosphorus insecticides by in vitro modified carboxylesterase E3 from Lucilia cuprina
    R Heidari
    CSIRO Entomology, GPO Box 1700, Canberra, ACT 2601, Australia
    Insect Biochem Mol Biol 34:353-63. 2004
    ..Lucilia cuprina, to organophosphorus (OP) insecticides is due to mutations in LcalphaE7, the gene encoding carboxylesterase E3, that enhance the enzyme's ability to hydrolyse insecticides...
  9. pmc A carboxylesterase, Esterase-6, modulates sensory physiological and behavioral response dynamics to pheromone in Drosophila
    Thomas Chertemps
    Universite Pierre et Marie Curie, UMR, Physiologie de l Insecte, Signalisation et Communication, Paris, France
    BMC Biol 10:56. 2012
    ..Here we verified the role of an extracellular carboxylesterase, esterase-6 (Est-6), in the sensory physiological and behavioral dynamics of Drosophila melanogaster response ..
  10. pmc Cloning of a novel pyrethroid-hydrolyzing carboxylesterase gene from Sphingobium sp. strain JZ-1 and characterization of the gene product
    Bao zhan Wang
    Key Laboratory of Microbiological Engineering of Agricultural Environment, Ministry of Agriculture, Life Sciences College of Nanjing Agricultural University, Nanjing, Jiangsu 210095, People s Republic of China
    Appl Environ Microbiol 75:5496-500. 2009
    A novel esterase gene, pytH, encoding a pyrethroid-hydrolyzing carboxylesterase was cloned from Sphingobium sp. strain JZ-1. The gene contained an open reading frame of 840 bp...
  11. ncbi Fitness trade-off in peach-potato aphids (Myzus persicae) between insecticide resistance and vulnerability to parasitoid attack at several spatial scales
    S P Foster
    Rothamsted Research, Harpenden, Hertfordshire, UK
    Bull Entomol Res 101:659-66. 2011
    ..The findings imply that parasitoids, and possibly other natural enemies, can influence the evolution and dynamics of insecticide resistance through pleiotropic effects of resistance genes on important behavioural traits...
  12. ncbi Induction effects of host plants on insecticide susceptibility and detoxification enzymes of Bemisia tabaci (Hemiptera: Aleyrodidae)
    Wen Xie
    Department of Plant Protection, Institute of Vegetables and Flowers, Chinese Academy of Agricultural Sciences, Beijing 100081, PR China
    Pest Manag Sci 67:87-93. 2011
    ..To illustrate the induced changes by host plant, bioassay and biochemical research on five different host populations were investigated...
  13. ncbi Molecular characterization of the amplified carboxylesterase gene associated with organophosphorus insecticide resistance in the brown planthopper, Nilaparvata lugens
    G J Small
    Cardiff University Centre for Pest Management, Cardiff School of Biosciences, Cardiff University, PO Box 915, Cardiff CF10 3TL, Wales, UK
    Insect Mol Biol 9:647-53. 2000
    ..resistance to organophosphorus insecticides (OPs) in Nilaparvata lugens is associated with elevation of carboxylesterase activity...
  14. pmc Characterization of an antennal carboxylesterase from the pest moth Spodoptera littoralis degrading a host plant odorant
    Nicolas Durand
    UMR A 1272 UPMC INRA Physiologie de l Insecte, Université Pierre et Marie Curie and INRA, Paris and Versailles, France
    PLoS ONE 5:e15026. 2010
    ..These enzymes are only expressed in the male antennae, and secreted into the lumen of the pheromone-sensitive sensilla. CCEs able to hydrolyze other odorants than sex pheromones, such as plant volatiles, have not been identified...
  15. ncbi A diversity of putative carboxylesterases are expressed in the antennae of the noctuid moth Spodoptera littoralis
    N Durand
    UMR A 1272 Université Paris 6 INRA, Physiologie de l Insecte, Signalisation et Communication, Paris, France
    Insect Mol Biol 19:87-97. 2010
    Recent studies have suggested that pheromone-degrading enzymes belonging to the carboxylesterase family could play a role in the dynamics of the olfactory response to acetate sex pheromones in insects...
  16. ncbi Human carboxylesterase 2 is commonly expressed in tumor tissue and is correlated with activation of irinotecan
    Guang Xu
    Department of Medicine, Washington University School of Medicine, and The Siteman Cancer Center, St Louis, Missouri 63110, USA
    Clin Cancer Res 8:2605-11. 2002
    ..Previous studies suggest that human carboxylesterase 2 (CES2) is the key activating isoform...
  17. ncbi Genomics-based approaches to screening carboxylesterase-like genes potentially involved in malathion resistance in oriental migratory locust (Locusta migratoria manilensis)
    Jianzhen Zhang
    Research Institute of Applied Biology, Shanxi University, Taiyuan, Shanxi, China
    Pest Manag Sci 67:183-90. 2011
    Previous studies have indicated that increased carboxylesterase (CarE) activity is a major mechanism of malathion resistance in field populations of the oriental migratory locust, Locusta migratoria manilensis (Meyen), in China...
  18. pmc Molecular cloning of a novel bioH gene from an environmental metagenome encoding a carboxylesterase with exceptional tolerance to organic solvents
    Yuping Shi
    Key Laboratory of Quality and Safety Risk Assessment for Aquatic Products on Storage and Preservation Shanghai, China Ministry of Agriculture, Engineering Centre for Quality Control and Risk Assessment of Aquatic Products, College of Food Science and Technology, Shanghai Ocean University, 999 Hu Cheng Huan Road, 201306, Shanghai, PR China
    BMC Biotechnol 13:13. 2013
    ..The biochemical property of the purified BioHx protein was also investigated...
  19. ncbi Molecular characterization of two carboxylesterase genes of the citrus red mite, Panonychus citri (Acari: Tetranychidae)
    Kun Zhang
    Key Laboratory of Entomology and Pest Control Engineering, College of Plant Protection, Southwest University, Chongqing, P R China
    Arch Insect Biochem Physiol 82:213-26. 2013
    ..To get better insight into the detoxification mechanism of P. citri, two carboxylesterase (CarE) genes, PCE1 and PCE2, were isolated and characterized...
  20. ncbi Structural study of carboxylesterase from hyperthermophilic bacteria Geobacillus stearothermophilus by molecular dynamics simulation
    Sangeeta Kundu
    Bioinformatics Centre, Bose Institute, Kolkata, India
    J Mol Graph Model 28:820-7. 2010
    ..Here, we have performed molecular dynamics simulations of carboxylesterase from hyperthermophilic bacterium Geobacillus stearothermophilus (GsEst) for 10ns each at five different ..
  21. pmc Diabetes and pancreatic exocrine dysfunction due to mutations in the carboxyl ester lipase gene-maturity onset diabetes of the young (CEL-MODY): a protein misfolding disease
    Bente B Johansson
    Department of Clinical Medicine, University of Bergen, N 5020 Bergen, Norway
    J Biol Chem 286:34593-605. 2011
    ..Thus, we propose that CEL-MODY is a protein misfolding disease caused by a negative gain-of-function effect of the mutant proteins in pancreatic tissues...
  22. ncbi Structure and characterization of human carboxylesterase 1A1, 1A2, and 1A3 genes
    Tatsuki Fukami
    Drug Metabolism and Toxicology, Division of Pharmaceutical Sciences, Graduate School of Medical Science, Kanazawa University, Kakuma machi, Kanazawa, Japan
    Pharmacogenet Genomics 18:911-20. 2008
    Human carboxylesterase (CES) 1A1 gene (14 exons) and CES1A3 pseudogene (six exons) are inverted and duplicated genes in a reference sequence (NT_010498)...
  23. pmc Synthesis and secretion of the pancreatic-type carboxyl ester lipase by human endothelial cells
    F Li
    Department of Pathology and Laboratory Medicine, University of Cincinnati College of Medicine, OH 45267 0529, USA
    Biochem J 329:675-9. 1998
    ..Moreover, vascular CEL may interact with cholesterol and oxidized lipoproteins to modulate the progression of atherosclerosis...
  24. pmc Nucleotide polymorphism in the Est6 promoter, which is widespread in derived populations of Drosophila melanogaster, changes the level of Esterase 6 expressed in the male ejaculatory duct
    Wendy A Odgers
    CSIRO Entomology, Canberra, 2601 Australia
    Genetics 162:785-97. 2002
    ..Thus the P1/P7 difference could be a major source of adaptively significant EST6 activity variation through much of the now cosmopolitan range of D. melanogaster...
  25. ncbi Covalent reaction intermediate revealed in crystal structure of the Geobacillus stearothermophilus carboxylesterase Est30
    Ping Liu
    Department of Biology, Molecular Basis of Disease Program, Georgia State University, Atlanta, GA 30303, USA
    J Mol Biol 342:551-61. 2004
    Est30 is a thermophilic carboxylesterase cloned from Geobacillus stearothermophilus that showed optimal hydrolysis of esters with short acyl chains at 70 degrees C...
  26. pmc hMSC-mediated concurrent delivery of endostatin and carboxylesterase to mouse xenografts suppresses glioma initiation and recurrence
    Jinlong Yin
    National Research Laboratory of Animal Cell Biotechnology, School of Agricultural Biotechnology, Seoul National University, Seoul, Republic of Korea
    Mol Ther 19:1161-9. 2011
    ..transducing the gene encoding endostatin (an antiangiogenesis factor), the gene encoding secretable form of carboxylesterase 2 (sCE2, a prodrug-activating enzyme), or a mixture of both genes...
  27. ncbi Carboxylesterase 1 gene polymorphism and methylphenidate response in ADHD
    Zsofia Nemoda
    Institute of Medical Chemistry, Molecular Biology and Pathobiochemistry, Semmelweis University, Budapest, Hungary
    Neuropharmacology 57:731-3. 2009
    ..Genetic analyses of MPH metabolizing carboxylesterase 1 enzyme (CES1) have not been carried out, whereas, meta-analysis of CYP2D6 genetic variants has been already ..
  28. ncbi The relative contributions of carboxylesterase and beta-glucuronidase in the formation of SN-38 in human colorectal tumours
    Peter J Tobin
    Department of Pharmacology, University of Sydney, New South Wales, Australia
    Oncol Rep 10:1977-9. 2003
    ..The production of SN-38 from CPT-11 and SN-38G was measured by HPLC in human colorectal tumour homogenates. Carboxylesterase and beta-glucuronidase activities were found to be lower in tumour tissues compared to matched normal colon ..
  29. ncbi Gene identification and proteomic analysis of the esterases of the cotton bollworm, Helicoverpa armigera
    Mark G Teese
    CSIRO Entomology, GPO Box 1700, Canberra ACT 2601, Australia
    Insect Biochem Mol Biol 40:1-16. 2010
    ..Five of these sequences were matched to zones of activity on native PAGE at relative mobility values previously associated with insecticide resistance in this species...
  30. ncbi Intestinal absorption of dietary cholesteryl ester is decreased but retinyl ester absorption is normal in carboxyl ester lipase knockout mice
    W Weng
    Laboratory of Biochemical Genetics and Metabolism, The Rockefeller University, New York 10021, USA
    Biochemistry 38:4143-9. 1999
    ..Overall, the data indicate that in the mouse, other enzymes besides CEL participate in the hydrolysis of dietary cholesteryl esters, retinyl esters, and triglycerides...
  31. pmc Pancreatic carboxyl ester lipase: a circulating enzyme that modifies normal and oxidized lipoproteins in vitro
    R Shamir
    Department of Biochemistry, Medical College of Pennsylvania and Hahnemann University, Philadelphia, 19129, USA
    J Clin Invest 97:1696-704. 1996
    ..We conclude that CEL has the capability to modify normal human LDL and HDL composition and structure and to reduce the atherogenicity of OxLDL by decreasing its lysoPC content...
  32. pmc Relationship between amount of esterase and gene copy number in insecticide-resistant Myzus persicae (Sulzer)
    L M Field
    IACR Rothamsted, Harpenden, Herts AL5 2JQ, UK
    Biochem J 339:737-42. 1999
    ..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...
  33. ncbi Discovery of a novel carboxylesterase through functional screening of a pre-enriched environmental library
    K Rashamuse
    CSIR Biosciences, Modderfontein, Johannesburg, South Africa
    J Appl Microbiol 106:1532-9. 2009
    ....
  34. ncbi Crystal structure of human carboxylesterase 1 complexed with the Alzheimer's drug tacrine: from binding promiscuity to selective inhibition
    Sompop Bencharit
    Department of Chemistry, School of Dentistry, University of North Carolina, Chapel Hill, 27599, USA
    Chem Biol 10:341-9. 2003
    Human carboxylesterase 1 (hCE1) is a broad-spectrum bioscavenger that plays important roles in narcotic metabolism, clinical prodrug activation, and the processing of fatty acid and cholesterol derivatives. We determined the 2...
  35. ncbi Organophosphates' resistance in the B-biotype of Bemisia tabaci (Hemiptera: Aleyrodidae) is associated with a point mutation in an ace1-type acetylcholinesterase and overexpression of carboxylesterase
    Michal Alon
    Department of Entomology, Faculty of Agriculture, The Hebrew University of Jerusalem, Rehovot, Israel
    Insect Biochem Mol Biol 38:940-9. 2008
    ..tabaci (Hemiptera: Aleyrodidae) proposed the existence of two molecular mechanisms for OPs' resistance: carboxylesterase- (COE) mediated hydrolysis or sequestration and decreased sensitivity of AChE...
  36. ncbi A carboxylesterase from the thermoacidophilic archaeon Sulfolobus solfataricus P1; purification, characterization, and expression
    Young Jun Park
    Department of Biochemistry, College of Natural Sciences, Kangwon National University, Chuncheon 200 701, Republic of Korea
    Biochim Biophys Acta 1760:820-8. 2006
    The carboxylesterase, a 34 kDa monomeric enzyme, was purified from the thermoacidophilic archaeon Sulfolobus solfataricus P1. The optimum temperature and pH were 85 degrees C and 8.0, respectively...
  37. ncbi Transcriptional regulation of human carboxylesterase 1A1 by nuclear factor-erythroid 2 related factor 2 (Nrf2)
    Taiga Maruichi
    Drug Metabolism and Toxicology, Faculty of Pharmaceutical Sciences, Kanazawa University, Kakuma machi, Kanazawa 920 1192, Japan
    Biochem Pharmacol 79:288-95. 2010
    Human carboxylesterase (CES) 1A, which is predominantly expressed in liver and lung, plays an important role in the hydrolysis of endogenous compounds and xenobiotics...
  38. ncbi Esterase activities in the blood, liver and intestine of several preclinical species and humans
    Loren M Berry
    Pharmacokinetics and Drug Metabolism, Amgen, Inc, Cambridge, MA, USA
    Drug Metab Lett 3:70-7. 2009
    Species and tissue differences in the activity of three major classes of esterases, carboxylesterase (CE), butyrylcholinesterase (BChE) and paraoxonase (PON), were studied...
  39. ncbi Carboxylesterase 2 is downregulated in colorectal cancer following progression of the disease
    Xiaobo Tang
    College of Pharmacy, Harbin Medical University, Harbin, China
    Cancer Invest 26:178-81. 2008
    Expression of carboxylesterase 2 in colorectal tumor tissues and serum carboxylesterase 2 levels at different stages of the disease were investigated by Western blotting...
  40. ncbi Carboxylesterase: specificity and spontaneous reactivation of an endogenous scavenger for organophosphorus compounds
    D M Maxwell
    US Army Medical Research Institute of Chemical Defense 3100 Ricketts Point Road, Aberdeen Proving Ground, MD 21010-5400, USA
    J Appl Toxicol 21:S103-7. 2001
    The ability of carboxylesterase (CaE) to act as a bioscavenger to provide protection against organophosphorus (OP) compounds has been demonstrated in several animal models...
  41. ncbi Gestational exposure to chlorpyrifos: dose response profiles for cholinesterase and carboxylesterase activity
    T L Lassiter
    Curriculum in Toxicology, University of North Carolina, Chapel Hill, USA
    Toxicol Sci 52:92-100. 1999
    ..the in vivo dose response profiles of the target enzyme cholinesterase (ChE) and the detoxifying enzymes carboxylesterase (CaE) in the fetal and maternal compartments of pregnant rats dosed with chlorpyrifos [(O,O'-diethyl O-3,5,6-..
  42. ncbi [Hydrolysis by carboxylesterase and disposition of prodrug with ester moiety]
    Teruko Imai
    Graduate School of Pharmaceutical Sciences, Kumamoto University, Japan
    Yakugaku Zasshi 127:611-9. 2007
    ..These findings indicate that identification of substrate specificity of CES isozymes and development of an in vitro experimental method are essential to support rational design of prodrug...
  43. ncbi Genomic structure and transcriptional regulation of the rat, mouse, and human carboxylesterase genes
    Masakiyo Hosokawa
    Faculty of Pharmaceutical Sciences, Chiba Institute of Sciences, Choshi, 288 0025, Japan
    Drug Metab Rev 39:1-15. 2007
    ....
  44. ncbi Allosteric kinetics of human carboxylesterase 1: species differences and interindividual variability
    Shiori Takahashi
    Drug Metabolism and Toxicology, Division of Pharmaceutical Sciences, Graduate School of Medical Science, Kanazawa University, Kanazawa 920 1192, Japan
    J Pharm Sci 97:5434-45. 2008
    Esterified drugs such as imidapril, derapril, and oxybutynin hydrolyzed by carboxylesterase 1 (CES1) are extensively used in clinical practice...
  45. ncbi Stereoselective characteristics and mechanisms of epidermal carboxylesterase metabolism observed in HaCaT keratinocytes
    Quan Gang Zhu
    Department of Pharmacy, Changhai Hospital, Second Military Medical University, 174 Chang Hai Road, Shanghai 200433, PR China
    Biol Pharm Bull 30:532-6. 2007
    There is increasing evidence that epidermal carboxylesterase may be involved in the stereoselective hydrolysis of prodrugs in percutaneous absorption...
  46. ncbi Pancreatic lipomatosis is a structural marker in nondiabetic children with mutations in carboxyl-ester lipase
    Helge Raeder
    Section for Pediatrics, Department of Clinical Medicine, University of Bergen, N 5020 Bergen, Norway
    Diabetes 56:444-9. 2007
    ..Our findings suggest that lipomatosis of the pancreas reflects early events involved in the pathogenesis of diabetes and exocrine pancreatic dysfunction syndrome...
  47. ncbi Expression and characterization of a human carboxylesterase 2 splice variant
    Marissa A Schiel
    Department of Biochemistry and Molecular Biology, Indiana University School of Medicine, Indianapolis, Indiana, USA
    J Pharmacol Exp Ther 323:94-101. 2007
    ..carbonyloxycamptothecin or Irinotecan] is a carbamate prodrug that is activated in vivo by carboxylesterase (CES)-2 to SN-38 (7-ethyl-10-hydroxycamptothecin), a potent topoisomerase I inhibitor...
  48. ncbi Carboxylesterase activity, cDNA sequence, and gene expression in malathion susceptible and resistant strains of the cotton aphid, Aphis gossypii
    Yiou Pan
    Department of Entomology, China Agricultural University, No 2 Yuanmingyuan West Road, Haidian District, Beijing, China
    Comp Biochem Physiol B Biochem Mol Biol 152:266-70. 2009
    Levels of insecticide resistance, carboxylesterase activity, carboxylesterase expression, and the cDNA sequence of carboxylesterase gene were investigated in malathion resistant and susceptible strains of cotton aphids, Aphis gossypii (..
  49. ncbi Decontamination of vegetables sprayed with organophosphate pesticides by organophosphorus hydrolase and carboxylesterase (B1)
    Y Z Zheng
    State Key Laboratory of Integrated Management of Pest Insects and Rodents, Institute of Zoology, Chinese Academy of Sciences, Beijing 100080, China
    Appl Biochem Biotechnol 136:233-41. 2007
    ..Additionally, the products of pesticide hydrolysis generated by treatment with the enzyme extract were determined to be virtually nontoxic...
  50. ncbi Plasma cholinesterase and carboxylesterase activities and nuclear and mitochondrial lipid composition of human placenta associated with maternal exposure to pesticides
    Berta Vera
    Instituto Multidisciplinario de Investigación y Desarrollo de la Patagonia Norte, CONICET Universidad Nacional del Comahue, Neuquen, Argentina
    Reprod Toxicol 34:402-7. 2012
    ..These changes in lipid profiles suggest repair by hyperplasia of the cytotrophoblast. Decreased CE activity may have clinical and toxicological implications and thus entail potential risks to damage fetal growth and development...
  51. ncbi Structure and stability of a thermostable carboxylesterase from the thermoacidophilic archaeon Sulfolobus tokodaii
    Clement Angkawidjaja
    Department of Material and Life Science, Graduate School of Engineering, Osaka University, Japan
    FEBS J 279:3071-84. 2012
    ..We prepared and crystallized a carboxylesterase of the HSL family from Sulfolobus tokodaii (Sto-Est), and determined its structures in the presence and ..
  52. ncbi Structure, biochemical characterization and analysis of the pleomorphism of carboxylesterase Cest-2923 from Lactobacillus plantarum WCFS1
    Rocío Benavente
    Department of Crystallography and Structural Biology, Institute of Physical Chemistry Rocasolano, CSIC, Madrid, Spain
    FEBS J 280:6658-71. 2013
    ..In the present study, we clarified the crystal structure of the carboxylesterase Cest-2923 from the lactic acid bacterium Lactobacillus plantarum WCFS1 refined to 2...
  53. ncbi Identification of a carboxylesterase-producing Rhodococcus soil isolate
    Serena Falcocchio
    Department of Microbiology, Faculty of Biology, University of Barcelona, Spain
    Can J Microbiol 51:753-8. 2005
    ....
  54. ncbi Molecular cloning and characterization of a novel putative carboxylesterase, present in human intestine and liver
    H Schwer
    Institute for Clinical Chemistry and Laboratory Medicine, University of Regensburg, Germany
    Biochem Biophys Res Commun 233:117-20. 1997
    A full-length cDNA coding for a putative intestinal carboxylesterase (iCE) was isolated from a human small intestine cDNA library...
  55. ncbi Human carboxylesterase-2 hydrolyzes the prodrug of gemcitabine (LY2334737) and confers prodrug sensitivity to cancer cells
    Susan E Pratt
    Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, Indiana 46285, USA
    Clin Cancer Res 19:1159-68. 2013
    ..LY2334737 cytotoxicity was tested in the NCI-60 panel; mining of microarray expression data identified carboxylesterase (CES) as a top hydrolase candidate...
  56. ncbi Molecular characterization of an ecdysteroid inducible carboxylesterase with GQSCG motif in the corn borer, Sesamia nonagrioides
    Dimitrios Kontogiannatos
    Department of Agricultural Biotechnology, Agricultural University of Athens, Iera Odos 75, Athens 11855, Greece
    J Insect Physiol 57:1000-9. 2011
    We obtained a full-length cDNA encoding a carboxylesterase in Sesamia nonagrioides. The complete cDNA sequence is comprised of 1838 bp with an open reading frame encoding 576 amino acid residues with predicted molecular mass of 64.24 kDa...
  57. pmc Photochemotherapeutic agent 8-methoxypsoralen induces cytochrome P450 3A4 and carboxylesterase HCE2: evidence on an involvement of the pregnane X receptor
    Jian Yang
    Department of Biomedical and Pharmaceutical Sciences, University of Rhode Island, Kingston, Rhode Island 02881, USA
    Toxicol Sci 95:13-22. 2007
    ..In this study, we report that 8-MOP is a potent inducer of cytochrome P450 3A4 (CYP3A4) and carboxylesterase 2 (HCE2), two major human enzymes that catalyze oxidative and hydrolytic reactions, respectively...
  58. ncbi Screening for and isolation and identification of malathion-degrading bacteria: cloning and sequencing a gene that potentially encodes the malathion-degrading enzyme, carboxylestrase in soil bacteria
    Sayed K Goda
    Shafallah Medical Genetic Centre, Doha, Qatar
    Biodegradation 21:903-13. 2010
    ..the degradation of malathion to malathion monocarboxylic and dicarboxylic acids, which formed as a result of carboxylesterase activity...
  59. ncbi Molecular cloning, purification and biochemical characterization of a novel pyrethroid-hydrolyzing carboxylesterase gene from Ochrobactrum anthropi YZ-1
    Yi Zhai
    Laboratory of Biology, Graduate School, Chinese Academy of Agriculture Science, Beijing 100081, China
    J Hazard Mater 221:206-12. 2012
    ..The pytZ contained an open reading frame of 606bp encoding a pyrethroid-hydrolyzing carboxylesterase. Deduced amino acid sequence showed moderate identities (39-59%) with most homologous carboxylesterase, ..
  60. ncbi In vitro evaluation of inhibitory effects of antidiabetic and antihyperlipidemic drugs on human carboxylesterase activities
    Tatsuki Fukami
    Drug Metabolism and Toxicology, Faculty of Pharmaceutical Sciences, Kanazawa University, Kakuma machi, Kanazawa 920 1192, Japan
    Drug Metab Dispos 38:2173-8. 2010
    Human carboxylesterase (CES) 1A is responsible for the biotransformation of angiotensin-converting enzyme (ACE) inhibitors such as imidapril and temocapril...
  61. ncbi Therapeutic targeting of melanoma cells using neural stem cells expressing carboxylesterase, a CPT-11 activating enzyme
    Margarita Gutova
    Division of Hematology and Hematopoietic Cell Transplantation, City of Hope National Medical Center and Beckman Research Institute, Duarte, CA 91010 3000, USA
    Curr Stem Cell Res Ther 5:273-6. 2010
    ..HB1.F3.CD cells were transduced by adenovirus encoding rabbit carboxylesterase (rCE), which converts CPT-11 into SN-38, a potent topoisomerase 1 inhibitor...
  62. ncbi Dexamethasone-mediated transcriptional regulation of rat carboxylesterase 2 gene
    Takeshi Hori
    Laboratory of Drug Metabolism and Biopharmaceutics, Faculty of Pharmaceutical Sciences, Chiba Institute of Science, Choshi, Japan
    Xenobiotica 42:614-23. 2012
    Rat carboxylesterase 2 (rCES2), which was previously identified as a methylprednisolone 21-hemisuccinate hydrolase, is highly inducible by dexamethasone in the liver...
  63. ncbi Hypoxia-targeted over-expression of carboxylesterase as a means of increasing tumour sensitivity to irinotecan (CPT-11)
    Torkjel Matzow
    Paterson Institute for Cancer Research, Christie Hospital NHS Trust, and School of Pharmacy and Pharmaceutical Sciences, University of Manchester, UK
    J Gene Med 9:244-52. 2007
    The induced expression of carboxylesterase (CE) enzymes, which convert the prodrug irinotecan (CPT-11) into its active cytotoxic metabolite SN-38, constitutes a promising strategy for cancer gene therapy...
  64. pmc Liver prenylated methylated protein methyl esterase is the same enzyme as Sus scrofa carboxylesterase
    Onovughode T Oboh
    College of Pharmacy and Pharmaceutical Sciences, Florida A and M University, Tallahassee, FL 32307, USA
    J Biochem Mol Toxicol 22:51-62. 2008
    ..A Mascot database search revealed these as portions of the Sus scrofa carboxylesterase, a 62-kDa serine hydrolase with the C-terminal HAEL endoplasmic reticulum-retention signal...
  65. ncbi Cloning and characterization of a carboxylesterase from Bacillus coagulans 81-11
    Stephens M Mnisi
    CSIR Bio Chemtek, P O Box 395, Pretoria 0001, South Africa
    Curr Microbiol 50:196-201. 2005
    ..Maximum activity was found at pH 8 and 50 degrees C, although the enzyme displayed stability at temperatures up to 60 degrees C...
  66. pmc Plasma carboxyl ester lipase activity modulates apolipoprotein B-containing lipoprotein metabolism in a transgenic mouse model
    Ling Li
    Laboratory of Lipoprotein Research, Cardiovascular Institute, Department of Medicine, Mount Sinai School of Medicine, New York, NY 10029, USA
    Metabolism 57:1361-8. 2008
    ..In summary, our results demonstrate that plasma CEL modulates apo B-Lp metabolism in vivo, resulting in reduced VLDL clearance and elevated plasma cholesterol levels...
  67. ncbi Expression and characterization of carboxylesterase E4 gene from peach-potato aphid (Myzus persicae) for degradation of carbaryl and malathion
    Wen Sheng Lan
    State Key Laboratory of Integrated Management of Pest Insects and Rodents, Institute of Zoology Chinese Academy of Sciences, 100080, Beijing, P R China
    Biotechnol Lett 27:1141-6. 2005
    An abridged carboxylesterase E4 (CbE E4) gene was cloned from the peach-potato aphid, Myzus persicae, by reverse transcription-PCR and subcloned into the expression vector pET28b. The abridged CbE E4 gene was successfully expressed in E...
  68. pmc Secreted and tumour targeted human carboxylesterase for activation of irinotecan
    D Oosterhoff
    Division of Gene Therapy, Department of Medical Oncology, Vrije Universiteit Medical Center, PO Box 7057, 1007 MB, Amsterdam, The Netherlands
    Br J Cancer 87:659-64. 2002
    ..CPT-11 can be considered as a prodrug, since it needs to be activated into the toxic drug SN-38 by the enzyme carboxylesterase. An approach to achieve tumour specific activation of CPT-11 is to transduce the cDNA encoding ..
  69. ncbi Association of MACE-based insecticide resistance in Myzus persicae with reproductive rate, response to alarm pheromone and vulnerability to attack by Aphidius colemani
    Stephen P Foster
    Division of Plant and Invertebrate Ecology, Rothamsted Research, Harpenden, Herts, AL5 2JQ, UK
    Pest Manag Sci 59:1169-78. 2003
    ..rates than non-MACE forms expressing moderate (R1) levels of another resistance mechanism based on elevated carboxylesterase. However, MACE forms were more responsive to alarm pheromone than their non-MACE counterparts...
  70. ncbi Sensitization of human tumor cells to CPT-11 via adenoviral-mediated delivery of a rabbit liver carboxylesterase
    M Wierdl
    Department of Molecular Pharmacology, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, USA
    Cancer Res 61:5078-82. 2001
    ..These data suggest that the described reagents may be suitable for use in vivo in a viral-directed enzyme prodrug therapy approach using CPT-11...
  71. ncbi A single nucleotide polymorphism in the carboxylesterase gene is associated with the responsiveness to imidapril medication and the promoter activity
    Eiichi Geshi
    Third Department of Internal Medicine, Showa University School of Medicine Tokyo, Japan
    Hypertens Res 28:719-25. 2005
    ..We investigated whether a single nucleotide polymorphism at position -816 of the carboxylesterase 1 (CES1) gene, which activates imidapril in the liver, is involved in the responsiveness to imidapril ..
  72. ncbi Prolonged toxic effects after cocaine challenge in butyrylcholinesterase/plasma carboxylesterase double knockout mice: a model for butyrylcholinesterase-deficient humans
    Ellen G Duysen
    University of Nebraska Medical Center, Eppley Institute, 985950 Nebraska Medical Center, Omaha, NE 68198 5950, USA
    Drug Metab Dispos 39:1321-3. 2011
    ..A reduction in endogenous levels of BChE may result in increased metabolism by hepatic carboxylesterase to produce norcocaine, a toxic product...
  73. ncbi Cloning of the esterase-5 locus from Drosophila pseudoobscura and comparison with its homologue in D. melanogaster
    J P Brady
    Department of Biology, Indiana University
    Mol Biol Evol 7:525-46. 1990
    ..The patterns of nucleotide substitutions and amino acid replacements between Est-5B and Est-6 are consistent with the hypothesis that mutation and genetic drift are responsible for the differences between these two genes...
  74. ncbi Purification and characterization of a carboxylesterase involved in malathion-specific resistance from Tribolium castaneum (Coleoptera: Tenebrionidae)
    Eric Haubruge
    Department of Pure and Applied Zoology, Gembloux Agricultural University, B 5030 Gembloux, Belgium
    Insect Biochem Mol Biol 32:1181-90. 2002
    Specific resistance to malathion in a strain of Tribolium castaneum is due to a 44-fold increase in malathion carboxylesterase (MCE) activity relative to a susceptible strain, whereas non-specific esterase levels are slightly lower...
  75. ncbi Recombinant porcine intestinal carboxylesterase: cloning from the pig liver esterase gene by site-directed mutagenesis, functional expression and characterization
    Anna Musidlowska-Persson
    Institute of Chemistry and Biochemistry, Department of Technical Chemistry and Biotechnology, Greifswald University, Soldmannstrasse 16, D 17487 Greifswald, Germany
    Protein Eng 16:1139-45. 2003
    ..The gene encoding rPLE shares 97% identity with the published nucleotide sequence of porcine intestinal carboxylesterase (PICE)...
  76. ncbi Carboxylesterase expression in human dental pulp cells: role in regulation of BisGMA-induced prostanoid production and cytotoxicity
    M C Chang
    Biomedical Science Team, Chang Gung University of Science and Technology, Taoyuan, Taiwan
    Acta Biomater 8:1380-7. 2012
    ..This study found that human dental pulp cells expressed mainly carboxylesterase-2 (CES2) and smaller amounts of CES1A1 and CES3 isoforms...
  77. pmc Novel metagenome-derived carboxylesterase that hydrolyzes β-lactam antibiotics
    Jeong Ho Jeon
    Marine Biotechnology Research Center, Korea Ocean Research and Development Institute, Ansan, South Korea
    Appl Environ Microbiol 77:7830-6. 2011
    ..Here, we describe the first example of a novel carboxylesterase derived from a metagenome that is able to cleave the amide bond of various β-lactam substrates and the ester ..
  78. ncbi Overexpression of carboxylesterase-2 results in enhanced efficacy of topoisomerase I inhibitor, irinotecan (CPT-11), for multiple myeloma
    Hiroki Yano
    Department of Medical Oncology and Immunology, Nagoya City University Graduate School of Medical Sciences, Nagoya, Aichi, Japan
    Cancer Sci 99:2309-14. 2008
    ..This efficacy was partly explained by the high expression level of human carboxylesterase-2 (hCE-2) in MM cells...
  79. ncbi Evolution in the amidohydrolase superfamily: substrate-assisted gain of function in the E183K mutant of a phosphotriesterase-like metal-carboxylesterase
    Luigi Mandrich
    Institute of Protein Biochemistry, National Research Council, Via Pietro Castellino 111, 80131, Naples, Italy
    Biochemistry 48:5602-12. 2009
    ..The promiscuous carboxylesterase and phosphodiesterase activities detected in pPTE and PLLs in turn paved the way for the prediction of the ..
  80. ncbi Transcriptional activation of the carboxylesterase 2 gene by the p53 pathway
    Woonyoung Choi
    Department of Pathology, The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, USA
    Cancer Biol Ther 5:1450-6. 2006
    ..form of p53 (p53T18D/S20D) into colon carcinoma cell lines identified transcriptional activation of the carboxylesterase 2 (CES-2) gene, which is involved in drug metabolism...
  81. ncbi Effect of flavonoids from various Mediterranean plants on enzymatic activity of intestinal carboxylesterase
    P Stocker
    Institut Méditerranéen de Recherche en Nutrition, Faculté des Sciences de St Jérôme, Universite d Aix Marseille, 13397 Marseille Cedex 20, France
    Biochimie 86:919-25. 2004
    ..garganica, were found to inhibit the enzymatic activities of both rat intestine and purified porcine liver carboxylesterase in a concentration-dependent manner...
  82. ncbi Genetic variation in carboxylesterase genes and susceptibility to isoniazid-induced hepatotoxicity
    S Yamada
    Cancer Genetics, Canada s Michael Smith Genome Sciences Centre, British Columbia Cancer Agency, Vancouver, Canada
    Pharmacogenomics J 10:524-36. 2010
    ..Replication of this possible association in a larger sample set and functional studies will be necessary to determine if this CES1 variant has a role in INH-induced hepatotoxicity...
  83. ncbi Human carboxylesterase 1A2 expressed from carboxylesterase 1A1 and 1A2 genes is a potent predictor of CPT-11 cytotoxicity in vitro
    Keiji Tanimoto
    Department of Translational Cancer Research, Research Institute for Radiation Biology and Medicine, Hiroshima University, Hiroshima, Japan
    Pharmacogenet Genomics 17:1-10. 2007
    ..Among the CESs, CES1 and CES2 probably play a major role in the metabolism, but the functional significance and molecular basis of CES1 on CPT-11 response remain unclear...
  84. ncbi Determination and analysis of single nucleotide polymorphisms and haplotype structure of the human carboxylesterase 2 gene
    Michael H Wu
    Department of Medicine, University of Chicago, Chicago, Illinois, USA
    Pharmacogenetics 14:595-605. 2004
    ..There are two known carboxylesterases expressed in human liver, small intestine and other tissues, carboxylesterase 1 (CES1) and carboxylesterase 2 (CES2)...
  85. pmc Mammalian carboxylesterase 3: comparative genomics and proteomics
    Roger S Holmes
    Department of Genetics, Southwest Foundation for Biomedical Research, San Antonio, TX 78227, USA
    Genetica 138:695-708. 2010
    ..Phylogenetic analyses demonstrated the relationships and potential evolutionary origins of the mammalian CES3 family of genes which were related to but distinct from other mammalian CES gene families...
  86. ncbi Cloning and characterization of a bacterial cell-bound type B carboxylesterase from Bacillus sp. BP-7
    N Prim
    Department of Microbiology, Faculty of Biology, University of Barcelona, Av Diagonal 645, 08028 Barcelona, Spain
    Curr Microbiol 42:237-40. 2001
    ..1. The enzyme showed homology to members of the bacterial subclass of type B carboxylesterases, a set of proteins potentially useful for biotechnological applications...
  87. pmc The in vitro metabolism of irinotecan (CPT-11) by carboxylesterase and beta-glucuronidase in human colorectal tumours
    Peter Tobin
    Department of Pharmacology, University of Sydney, and Department of Anatomical Pathology, Royal Prince Alfred Hospital, New South Wales, Australia
    Br J Clin Pharmacol 62:122-9. 2006
    ..SN-38 is metabolized to its inactive glucuronide, SN-38 glucuronide. The aim of this study was to determine, the reactivation of SN-38 from SN-38 glucuronide by beta-glucuronidase may represent a significant pathway of SN-38 formation...
  88. ncbi An improved human carboxylesterase for enzyme/prodrug therapy with CPT-11
    M Wierdl
    Department of Molecular Pharmacology, St Jude Children s Research Hospital, Memphis, TN 38105, USA
    Cancer Gene Ther 15:183-92. 2008
    ..We propose that this enzyme should likely be less immunogenic than rCE and would be suitable for the in vivo application of CE/CPT-11 enzyme/prodrug therapy...
  89. ncbi Degradation of fumonisin B1 by the consecutive action of two bacterial enzymes
    Stefan Heinl
    Department of Biotechnology, University of Natural Resources and Applied Life Sciences, Muthgasse 18, 1190 Vienna, Austria
    J Biotechnol 145:120-9. 2010
    ..The recombinant carboxylesterase was shown to catalyze the deesterification of fumonisin B(1) to hydrolyzed fumonisin B(1)...
  90. pmc Divergent and conserved features in the spatial expression of the Drosophila pseudoobscura esterase-5B gene and the esterase-6 gene of Drosophila melanogaster
    N A Tamarina
    Division of Vascular Surgery, Department of Surgery, Northwestern University Medical School, 251 East Chicago Avenue, Suite 626, Chicago, IL 60611, USA
    Proc Natl Acad Sci U S A 94:7735-41. 1997
    ..The results suggest that the conservation of the expression pattern in genes that evolved from a common ancestor may not be accompanied by preservation of the corresponding cis-regulatory elements...
  91. ncbi Identification of a novel member of the carboxylesterase family that hydrolyzes triacylglycerol: a potential role in adipocyte lipolysis
    Hiroaki Okazaki
    Division of Endocrinology and Metabolism, Department of Medicine, Jichi Medical University, 3311 1 Yakushiji, Shimotsuke, Tochigi 329 0498, Japan
    Diabetes 55:2091-7. 2006
    ..Thus, TGH-2 may make a contribution to adipocyte lipolysis during period of increased energy demand...
  92. pmc Recommended nomenclature for five mammalian carboxylesterase gene families: human, mouse, and rat genes and proteins
    Roger S Holmes
    Department of Genetics, Southwest Foundation for Biomedical Research, San Antonio, TX 78227 5301, USA
    Mamm Genome 21:427-41. 2010
    Mammalian carboxylesterase (CES or Ces) genes encode enzymes that participate in xenobiotic, drug, and lipid metabolism in the body and are members of at least five gene families...
  93. ncbi Irinotecan pathway genotype analysis to predict pharmacokinetics
    Ron H J Mathijssen
    Department of Medical Oncology, Erasmus MC Daniel den Hoed Cancer Center, 3075 EA Rotterdam, The Netherlands
    Clin Cancer Res 9:3246-53. 2003
    ..The purpose was to explore the relationships between irinotecan disposition and allelic variants of genes coding for adenosine triphosphate binding cassette transporters and enzymes of putative relevance for irinotecan...
  94. ncbi Mouse liver and kidney carboxylesterase (M-LK) rapidly hydrolyzes antitumor prodrug irinotecan and the N-terminal three quarter sequence determines substrate selectivity
    Mingxing Xie
    Department of Biomedical Sciences, University of Rhode Island, Kingston, Rhode Island 02881, USA
    Drug Metab Dispos 31:21-7. 2003
    ..This report describes a novel mouse liver and kidney carboxylesterase (M-LK) that is highly active toward this prodrug...
  95. ncbi Carboxylesterase isoform 2 mRNA expression in peripheral blood mononuclear cells is a predictive marker of the irinotecan to SN38 activation step in colorectal cancer patients
    Erika Cecchin
    Experimental and Clinical Pharmacology, Centro di Riferimento Oncologico, National Cancer Institute, Aviano, Italy
    Clin Cancer Res 11:6901-7. 2005
    Irinotecan (CPT11) is a prodrug activated in humans mainly by carboxylesterase 2 (CES2) generating the SN38 metabolite responsible for the drug efficacy and toxicity...
  96. ncbi Comparing the organophosphorus and carbamate insecticide resistance mutations in cholin- and carboxyl-esterases
    John G Oakeshott
    CSIRO Entomology, GPO Box 1700, Canberra, ACT 2601, Australia
    Chem Biol Interact 157:269-75. 2005
    ..It appears that the constraints of the genetic code and eukaryote genetic systems have severely limited the evolutionary response of insects to the widespread use of the insecticides over the last 60 years...
  97. ncbi Purification and cloning of a broad substrate specificity human liver carboxylesterase that catalyzes the hydrolysis of cocaine and heroin
    E V Pindel
    Department of Biochemistry, Indiana University School of Medicine, Indianapolis, Indiana 46202 5122, USA
    J Biol Chem 272:14769-75. 1997
    A human liver carboxylesterase (hCE-2) that catalyzes the hydrolysis of the benzoyl group of cocaine and the acetyl groups of 4-methylumbelliferyl acetate, heroin, and 6-monoacetylmorphine was purified from human liver...
  98. ncbi Carboxylesterase 3 (EC 3.1.1.1) is a major adipocyte lipase
    Krishnakant G Soni
    Division of Medical Genetics, Ste Justine Hospital, Montreal, Quebec H3T 1C5, Canada
    J Biol Chem 279:40683-9. 2004
    ..SDS-PAGE, followed by tandem mass spectrometric analysis of excised Coomassie Blue-stained peptides, revealed carboxylesterase 3 (triacylglycerol hydrolase (TGH); EC 3.1.1.1). TGH is also the principle lipase of WAT fat cake extracts...
  99. ncbi Butyrylcholinesterase, paraoxonase, and albumin esterase, but not carboxylesterase, are present in human plasma
    Bin Li
    University of Nebraska Medical Center, Eppley Institute, Omaha, NE 68198 6805, USA
    Biochem Pharmacol 70:1673-84. 2005
    ..Misconception #1 is that human plasma contains carboxylesterase. We demonstrate that human plasma contains no carboxylesterase (EC 3.1.1...
  100. ncbi An epididymal form of cauxin, a carboxylesterase-like enzyme, is present and active in mammalian male reproductive fluids
    Heath Ecroyd
    Gamètes Males et Fertilité, UMR 6175 INRA CNRS Universite de Tours Haras Nationaux, Station de Physiologie de la Reproduction et des Comportements, Institut National de la Recherche Agronomique, INRA Nouzilly, 37380 Monnaie, France
    Biol Reprod 74:439-47. 2006
    ..complex isolated from ram cauda epididymal fluid revealed a protein that showed homology to a carboxylesterase-like protein previously identified in cat urine (cauxin)...
  101. ncbi Brain tumor oncolysis with replication-conditional herpes simplex virus type 1 expressing the prodrug-activating genes, CYP2B1 and secreted human intestinal carboxylesterase, in combination with cyclophosphamide and irinotecan
    Edyta Tyminski
    Molecular Neuro oncology Laboratories, Neurosurgery Service and Biostatistics Center, Massachusetts General Hospital, Charlestown, Massachusetts, USA
    Cancer Res 65:6850-7. 2005
    ..5 genes and an insertion of the two prodrug activating genes, CYP2B1 and secreted human intestinal carboxylesterase. Each of these can convert the inactive prodrugs, cyclophosphamide and irinotecan (CPT-11), into their active ..

Research Grants61

  1. Carboxylesterase-activated Doxazolidine-prodrug for Hepatocellular Carcinoma
    Tad H Koch; Fiscal Year: 2012
    ..is proposed to evaluate in vivo a newly designed, targeted, prodrug therapy for cancers that overexpress the carboxylesterase, CES2, with focus on HCC...
  2. Inhibition of Carboxylesterase Metabolism by Ethanol
    Robert B Parker; Fiscal Year: 2011
    ..In distinct contrast, little information is available on whether drug interactions are important for carboxylesterase substrate drugs...
  3. Identification of Novel Genes/Pathways That Regulate Lipid and Glucose Metabolism
    Yanqiao Zhang; Fiscal Year: 2013
    ..b>Carboxylesterase 1 (CES1) is highly and principally expressed in the liver...
  4. Genetic Variants of Human Carboxylesterase 1 Influence the Activation and Antivir
    John S Markowitz; Fiscal Year: 2012
    DESCRIPTION (provided by applicant): Human carboxylesterase 1 (hCES1) is the most abundant hepatic hydrolase and is encoded by two CES1 genes, i.e. CES1A1 and CES1A2...
  5. Development of a CES 2-Activated Doxazolidine Prodrug for Pancreatic Cancer
    Tad H Koch; Fiscal Year: 2010
    ..is proposed to evaluate in vivo a newly designed, targeted, prodrug therapy for cancers that overexpress the carboxylesterase, CES2, with focus on pancreatic cancer...
  6. CGI-58 Regulation of Triglyceride Metabolism and Inflammation
    JENNA BETTERS; Fiscal Year: 2010
    ....
  7. Development of vector-specific, resistance-breaking insecticides to reduce malari
    Paul R Carlier; Fiscal Year: 2013
    ..bivalent carbamates for resilience to target-site mutation;4)identify strategies to mitigate against carboxylesterase-mediated detoxification;and 5)make a preliminary assessment of mammalian toxicity of the most promising ..
  8. Organ-specific Ugt1 profiling in detoxifying the anticancer drug CPT-11
    Shujuan Chen; Fiscal Year: 2013
    ..CPT-11 is a prodrug that is hydrolyzed by carboxylesterase to the active topoisomerase 1 inhibitor, SN-38...
  9. Selective Inhibitors to Improve CPT-11 Therapy
    Philip M Potter; Fiscal Year: 2013
    ..to arise, in part, from direct activation of CPT-11, that is secreted in the bile, by a human intestinal carboxylesterase (CE) that is highly expressed in the small intestine...
  10. Relationship of Blood Esterases, Pesticide Exposure and Cardiovascular Disease
    Janice Chambers; Fiscal Year: 2009
    ..for many years because of their involvement in the detoxication of many pesticides are paraoxonase (PON1) and carboxylesterase (CaE)...
  11. Improving CPT-11 Efficacy Using Structural and Chemical Biology
    Matthew R Redinbo; Fiscal Year: 2013
    ..CPT-11 is a prodrug that is hydrolyzed in vivo to its active metabolite, SN-38, by carboxylesterase enzymes (CEs)...
  12. Neural Stem Cell Mediated CE-CPT11 Therapy for Neuroblastoma
    Karen S Aboody; Fiscal Year: 2013
    ..The goal of this U-01 proposal is to identify the optimal dose and schedule of carboxylesterase (CE)-secreting neural stem cells (NSCs) in combination with CPT-11 (Irinotecan) for a tumor selective, more ..
  13. Novel Protein-Based Therapeutics for Nerve Agent Detoxification
    MATTHEW REDINBO; Fiscal Year: 2010
    ..Human carboxylesterase 1 (hCE1), a promiscuous drug metabolism enzyme, offers promise as a broad- spectrum protein-based therapeutic ..
  14. Therapeutics against chemical threat induced respiratory toxicity
    MADHUSOODANA NAMBIAR; Fiscal Year: 2009
    ..bypasses the detoxification of chemical threat agents in the airway of rodents, which have high levels of carboxylesterase and mucus. Thus, the chemical agents reach alveoli and mimics an exposure similar to human...
  15. BIOCHEMICAL TOXICOLOGY OF CARBOXYESTERASES
    Andrew Parkinson; Fiscal Year: 1992
    ..Therefore, the experiments outlined in this proposal will contribute significantly to our basic understanding of carboxyesterases as a family of enzymes involved in the detoxication of foreign compounds...
  16. EVALUATION OF LIPOXYGENASE-DERIVED PRODUCTS AS MEDIATORS
    Charles Serhan; Fiscal Year: 1990
    ..In addition, they will provide a basis for both the design and evaluation of pharmacologic interventions in specific disorders...
  17. Epididymis-specific proteins for male contraception
    FRANK FRENCH; Fiscal Year: 2004
    ..Aim 1 Define expression of the human proteins corresponding to monkey Clones ESC46I-ribonuclease A and ESC615-carboxylesterase B, Specific Aim 2 Determine the functions of the human ESC461 protein Specific Aim 3 Determine the functions ..
  18. Retinyl Ester Binding Proteins and the Visual Cycle
    Robert Rando; Fiscal Year: 2007
    ..unreadable] [unreadable]..
  19. IGA FC RECEPTORS
    JULIA PHILLIPS QUAGLIATA; Fiscal Year: 1993
    ..5) To establish whether the receptor plays a physiological role in the function of the cells...
  20. HYDROLYSIS OF VITAMIN A ESTERS IN LIVER
    EARL HARRISON; Fiscal Year: 2007
    ..distribution of carboxylesterases between stellate cells & hepatocytes and to test the hypotheses that carboxylesterase ES-2 is localized exclusively in hepatocytes and that carboxylesterase ES-10 is localized in hepatocytes and ..
  21. Prodrug enzyme therapy of pancreatic cancer mediated by oncolytic HSV vector
    Michael Lanuti; Fiscal Year: 2010
    ..enzymes, yeast cytosine deaminase and uracil phosphoribosyltransferase fusion protein (yCD-UPRT) and rabbit carboxylesterase (rCE), by an oncolytic HSV vector and subsequent treatment with two prodrugs, 5-fluorocytosine (5-FC) and ..
  22. AMINOKETONE INHIBITORS OF THE DOPAMINE TRANSPORTER
    JOHN REINHARD; Fiscal Year: 2005
    ..esters of 1555U88 will not directly inhibit the dopamine transporter but, following hydrolysis by intestinal carboxylesterase, will yield the active drug...
  23. Molecular Toxicology of Carboxylesterases
    Bingfang Yan; Fiscal Year: 2006
    ..to selectively block or alter either pathway and the role of each receptor will be established in regulating carboxylesterase expression...
  24. PROTEIN KINASE C BASED ANTILEUKEMIC THERAPY
    Richard Stone; Fiscal Year: 1999
    ....
  25. MONOCYTE AND ENDOTHELIAL INTERACTIONS IN VEIN GRAFTS
    GAYLE ADCOCK; Fiscal Year: 1993
    ..These studies may help to define whether the interaction between monocytes and endothelial cells is a protective mechanism evoked in vein grafts following implantation...
  26. Phase II randomized trial of CPT-11 and Mitomycin C
    MIGUEL VILLALONA; Fiscal Year: 2003
    ..As a potential proof-of-concept in humans of the importance of NQ01 mutations, topoisomerase I and carboxylesterase gene expression, as predictors of chemoresistance to MMC and CPT-11, we will obtain tumor tissue and PBMC ..
  27. HUMAN CARBOXYLESTERASES FOR TARGETED CPT-11 ACTIVATION
    Peter Senter; Fiscal Year: 2000
    ..This will be accomplished in a two-step approach to cancer chemotherapy, in which a monoclonal antibody-carboxylesterase conjugate is allowed to bind to cell- surface antigens prior to the administration of CPT-11...
  28. Improving the activation of CPT-11 by hCE-2
    DANIEL MONTICELLO; Fiscal Year: 2002
    ..a clinically approved cancer pro-drug, which is converted to the active form SN-38 by the major human liver carboxylesterase hCE-2...
  29. Polymeric delivery of enzymes and prodrugs for cancer
    Hamid Ghandehari; Fiscal Year: 2002
    ..2) To synthesize and characterize a series of polyethylene glycol - rabbit carboxylesterase (PEG -CE) conjugates...
  30. Mixture Modeling: Pesticide Drug Interactions
    Charles Timchalk; Fiscal Year: 2009
    ..It is fully anticipated that this approach will facilitate the understanding of a variety of complex chemical interactions as it relates to the occupational health implications of working with insecticides. ..
  31. Development of Selective Nanoporous Sorbents for Radionuclide Decorporation
    Charles Timchalk; Fiscal Year: 2008
    ..abstract_text> ..
  32. INNOVATIVE BIOMONITORING FOR LEAD IN SALIVA
    Charles Timchalk; Fiscal Year: 2006
    ..It is reasonable to speculate that once this model system has been adequately validated it can readily be employed to screen sensitive populations (e.g. children) that are at greatest risk from chronic Pb exposure. ..
  33. SELECTIVE THERAPY OF TUMORS THAT OVEREXPRESS C MYC
    PHILIP POTTER; Fiscal Year: 2006
    ..Expression of a rabbit liver carboxylesterase (rCE) that can efficiently activate CPT-11 confers sensitivity to the drug both to cells in culture and when ..
  34. Novel Therapeutic Approaches for Narcotic Overdose
    PHILIP POTTER; Fiscal Year: 2009
    ..With cocaine, the methyl group is removed by human carboxylesterase 1 (hCE1) to produce benzyl ecgonine, the major inactive metabolite of the drug...
  35. CPT11 activation by carboxylesterases in colon cancer
    WILLIAM BOSRON; Fiscal Year: 2003
    ..The overall goal is to produce a CPT-11 (Irinotecan) carboxylesterase assay that could be used to predict treatment outcome and/or toxicity for patients on CPT-11 therapy for ..
  36. Retinoid Metabolism in Hepatitic Stellate Cells
    WILLIAM BOSRON; Fiscal Year: 2005
    ..Inhibitors of retinyl ester hydrolysis in stellate cells may be an effective therapeutic strategy for arresting stellate cell activation early in hepatic fibrosis. ..
  37. Effect of ethanol on retinoid metabolism and signaling in zebrafish embryos
    WILLIAM BOSRON; Fiscal Year: 2007
    ..We will assess the feasibility of performing targeted proteomics studies with tissues from other populations that express different SNPs in alcohol metabolizing enzymes. [unreadable] [unreadable] [unreadable]..
  38. Methylphenidate-Ethanol Interactions in ADHD and Co-abuse
    KENNERLY SEXTON PATRICK; Fiscal Year: 2010
    ..For instance, ETOH induced elevation of plasma MPH may predispose a patient to cardiovascular accidents in the absence of informed treatment interventions. ..
  39. Methylphenidate-Ethanol Interaction in ADHD and Coabuse
    Kennerly Patrick; Fiscal Year: 2003
    ..g., dextroamphetamine vs. MPH; dI-MPH vs. d-MPH; immediate-release MPH vs. extended-release MPH; or adjustment of MPH. ..
  40. Effects of Statins on AD beyond Cholesterol and Amyloid
    Ling Li; Fiscal Year: 2006
    ..abstract_text> ..
  41. Role of NPC1L1 in regulating energy metabolism, nutrient utilization & weight gai
    Philip N Howles; Fiscal Year: 2010
    ....
  42. Polytene chromosomes of Culex pipiens mosquito complex
    Anthony Cornel; Fiscal Year: 2004
    ..p. pipiens, Cx. p. quinquefasciatus and Cx. p. molestus and 2) Determine chromosomal homologies between Cx. p. pipiens, Cx. p. quinquefasciatus and Cx. p. molestus. ..
  43. Structure and Mechanism of Human Topoisomerase I
    MATTHEW REDINBO; Fiscal Year: 2004
    ....
  44. GABAERGIC INSECTICIDE TOXICOLOGY
    JOHN CASIDA; Fiscal Year: 2002
    ....
  45. Trihalomethane Pharmacokinetics and Pharmacodynamics
    MATTHEW ROSS; Fiscal Year: 2003
    ..It is also essential to determine if the same metabolic pathways are operative in rodents and humans and if metabolic flux through the different pathways is similar. ..
  46. Cyanohydrin based fluorescent substrates of sEH (RMI)
    Christophe Morisseau; Fiscal Year: 2004
    ..This will be done by screening the combinatorial libraries from the "NIH Roadmap", libraries contracted from commercial vendors, and more defined libraries generated in house. ..
  47. Carboxyl Ester Lipase Affects Hepatic HDL Metabolism
    PHILIP HOWLES; Fiscal Year: 2009
    ....
  48. Neural Progenitor Cells as Cancer Therapy Vectors
    Karen Aboody; Fiscal Year: 2009
    ..show that NPCs transduced with replication-defective adenovirus encoding the CPT-11-activating enzyme rabbit carboxylesterase (rCE) express up to 1000-fold higher levels of CE activity than do human normal or tumor cells...
  49. The Effect of a Mixture of Pesticides on the Rat Cardiac Proteome
    John Crow; Fiscal Year: 2007
    ..Our long-term objective is to better understand the extent to which commonly used pesticides and other environmental chemicals influence heart disease and its treatment. [unreadable] [unreadable] [unreadable]..
  50. Selfish gene and genetic control of vector-borne diseases
    ZACH ADELMAN; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  51. Forward and Reverse Genetics in Mosquitoes Using an RNA Virus
    ZACH ADELMAN; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  52. SELECTIVE THERAPY OF NEUROBLASTOMA
    MARY DANKS; Fiscal Year: 2007
    ..Overall, these studies should provide alternative treatment modalities for high-risk neuroblastoma. ..
  53. Glutathione-s-transferase mediated pyrethroid resistance in Culex pipiens s.l.
    Anthony Cornel; Fiscal Year: 2007
    ..These studies will also lead to understanding the mechanism of metabolic resistance to aid in development of novel, next generation insecticides and synergists that may augment pyrethroids. [unreadable] [unreadable] [unreadable]..
  54. Vitamin D regulation of ECM in model of heart failure
    Robert Simpson; Fiscal Year: 2007
    ..Moreover, it will determine if decreased vitamin D metabolite levels correlate with changes in heart collagen and MMP in an established model of heart failure. ..
  55. Cell Signaling, PXR Phosphorylation & Drug Disposition
    Jeffrey Staudinger; Fiscal Year: 2009
    ..These studies will provide additional insight into the regulation of drug disposition and drug-drug interaction. ..
  56. CHOLINERGIC INSECTICIDE TOXICOLOGY
    JOHN CASIDA; Fiscal Year: 2006
    ....
  57. VITAMIN D PLANT ANTIOXIDANT SILIBININ IN LEUKEMIA TRANSLATIONAL STUDY
    George P Studzinski; Fiscal Year: 2010
    ..Thus, myeloid leukemia can be considered an orphan disease, and merits support from public sources for the development of novel therapy. ..
  58. Organophosphorus Pesticide Toxicology
    JOHN CASIDA; Fiscal Year: 2006
    ..Knowledge gained on OP pesticide toxicology is also applicable to OP nerve gases as chemical warfare and terrorism agents. ..
  59. Structure and Function of the Human Pregnane X Receptor
    MATTHEW REDINBO; Fiscal Year: 2006
    ..5. Elucidate structures of hPXR in complexes with large drugs like rifampicin and taxol. 6. Examine structures of mouse and rabbit PXR to determine why different species respond to distinct xenobiotics. ..
  60. Antioxidant Defense System and Leydig Cell Aging
    Haolin Chen; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..