Genomes and Genes
Summary: Artifactual vesicles formed from the endoplasmic reticulum when cells are disrupted. They are isolated by differential centrifugation and are composed of three structural features: rough vesicles, smooth vesicles, and ribosomes. Numerous enzyme activities are associated with the microsomal fraction. (Glick, Glossary of Biochemistry and Molecular Biology, 1990; from Rieger et al., Glossary of Genetics: Classical and Molecular, 5th ed)
Publications290 found, 100 shown here
- Phospholipid:diacylglycerol acyltransferase: an enzyme that catalyzes the acyl-CoA-independent formation of triacylglycerol in yeast and plantsA Dahlqvist
Scandinavian Biotechnology Research ScanBi AB, Herman Ehles Väg 2 S 26831 Svalôv, Sweden
Proc Natl Acad Sci U S A 97:6487-92. 2000..We further found that PDAT activity also is present in yeast microsomes. The substrate specificity of this PDAT depends on the head group of the acyl donor, the acyl group transferred, ..
- Protein disulfide isomerase acts as a redox-dependent chaperone to unfold cholera toxinB Tsai
Howard Hughes Medical Institute and Department of Cell Biology, Harvard Medical School, 240 Longwood Avenue, Boston, MA 02115, USA
Cell 104:937-48. 2001....
- Structure of human estrone sulfatase suggests functional roles of membrane associationFrancisco G Hernandez-Guzman
Department of Structural Biology, Hauptman Woodward Medical Research Institute, Buffalo, New York 14203, USA
J Biol Chem 278:22989-97. 2003..This simple architecture could be a prototype utilized by the ER membrane in dictating the form and the function of ER-resident enzymes...
- Microsomal prostaglandin E synthase-1: the inducible synthase for prostaglandin E2Annaleise V Sampey
University of Michigan, Ann Arbor, MI, USA
Arthritis Res Ther 7:114-7. 2005..The focus of this article is to review some recent advances in our understanding of mechanisms specific to the regulation of inducible mPGES-1 in inflammatory arthritis...
- Evidence suggesting that the two forms of heme oxygenase are products of different genesI Cruse
Department of Biophysics, University of Rochester School of Medicine, New York 14642
J Biol Chem 263:3348-53. 1988Recently, we have reported on the presence of two forms of heme oxygenase in rat liver and testis microsomes, referred to as HO-1 and HO-2 (M. D. Maines, G. M. Trakshel, and R. K. Kutty (1986) J. Biol. Chem. 261, 411-419; G. M...
- Licofelone suppresses prostaglandin E2 formation by interference with the inducible microsomal prostaglandin E2 synthase-1Andreas Koeberle
Pharmaceutical Institute, University of Tuebingen, Auf der Morgenstelle 8, D 72076 Tuebingen, Germany
J Pharmacol Exp Ther 326:975-82. 2008..efficiently blocked the conversion of PGH(2) to PGE(2) mediated by mPGES-1 (IC(50) = 6 microM) derived from microsomes of interleukin-1beta-treated A549 cells, being about equipotent to 3-[1-(4-chlorobenzyl)-3-t-butyl-thio-5-..
- Structure of microsomal cytochrome P450 2B4 complexed with the antifungal drug bifonazole: insight into P450 conformational plasticity and membrane interactionYonghong Zhao
Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, TX 77555, USA
J Biol Chem 281:5973-81. 2006..The results allow us to model the membrane-associated state of P450 and provide insight into how lipophilic substrates access the buried active site...
- Expression in yeast and tobacco of plant cDNAs encoding acyl CoA:diacylglycerol acyltransferaseP Bouvier-Nave
Institut de Biologie Moleculaire des Plantes, Strasbourg, France
Eur J Biochem 267:85-96. 2000..Incorporation was 2-3 times higher in microsomes from yeast transformed with these plant cDNAs than in yeast transformed with the void vector, clearly showing ..
- Carrageenan-induced paw edema in rat elicits a predominant prostaglandin E2 (PGE2) response in the central nervous system associated with the induction of microsomal PGE2 synthase-1Jocelyne Guay
Department of Biochemistry and Molecular Biology, Merck Frosst Centre for Therapeutic Research, Kirkland, Quebec H9H 3L1, Canada
J Biol Chem 279:24866-72. 2004..The data also indicate that the up-regulation of mPGES-1 contributes to COX-2-mediated PGE(2) production in the CNS during peripheral inflammation...
- The role of the microsomal triglygeride transfer protein in abetalipoproteinemiaN Berriot-Varoqueaux
U327 Institut National de la Santé et de la Recherche Médicale, Faculte de Medecine Xavier Bichat, Université de Paris 7 Denis Diderot, 75870 Paris, France
Annu Rev Nutr 20:663-97. 2000..Unless treated, abetalipoproteinemic subjects develop gastrointestinal, neurological, ophthalmological, and hematological abnormalities...
- Microsomal prostaglandin E synthase (mPGES)-1, mPGES-2 and cytosolic PGES expression in human gastritis and gastric ulcer tissueKatya Gudis
Third Department of Internal Medicine, Nippon Medical School, Sendagi, Bunkyo ku, Tokyo, Japan
Lab Invest 85:225-36. 2005....
- Identification of the binding site on cytochrome P450 2B4 for cytochrome b5 and cytochrome P450 reductaseA Bridges
Department of Anesthesia, Veterans Affairs Medical Center, San Francisco, California 94121, USA
J Biol Chem 273:17036-49. 1998..These studies indicate that the binding sites for cytochrome b5 and cytochrome P450 reductase are, as predicted, located on the proximal surface of cytochrome P450 2B4 and are partially overlapping but not identical...
- Halloween genes encode P450 enzymes that mediate steroid hormone biosynthesis in Drosophila melanogasterLawrence I Gilbert
The University of North Carolina at Chapel Hill, CB 3280, Coker Hall, Chapel Hill, NC 27599 3280, USA
Mol Cell Endocrinol 215:1-10. 2004..Shade is present in several tissues as expected while disembodied and shadow are restricted to the ring gland. The paradigm used should allow us to define the enzymes mediating the entire ecdysteroid biosynthetic pathway...
- Evidence that unsaturated fatty acids are potent inhibitors of renal UDP-glucuronosyltransferases (UGT): kinetic studies using human kidney cortical microsomes and recombinant UGT1A9 and UGT2B7Paraskevi Tsoutsikos
Department of Clinical Pharmacology, Flinders University and Flinders Medical Centre, Bedford Park, 5042, Adelaide, Australia
Biochem Pharmacol 67:191-9. 2004..of FA (C2:0-C20:5) on 4-methylumbelliferone (4-MU) glucuronidation was investigated using human kidney cortical microsomes (HKCM) and recombinant UGT1A9 and UGT2B7 as the enzyme sources...
- Effect of iron and ascorbate on cyclosporine-induced oxidative damage of kidney mitochondria and microsomesS H Lee
Department of Pharmacology, College of Medicine, Chung Ang University, Seoul, 156 756, South Korea
Pharmacol Res 43:161-71. 2001The stimulatory effect of iron and ascorbate on the damaging action of cyclosporine in kidney mitochondria, microsomes and epithelial cells was examined...
- Hydrolysis of a series of parabens by skin microsomes and cytosol from human and minipigs and in whole skin in short-term cultureChristopher Jewell
Toxicology Unit, School of Clinical and Laboratory Sciences, Devonshire Building, Newcastle University, Newcastle upon Tyne, NE2 4EA, UK
Toxicol Appl Pharmacol 225:221-8. 2007..These results demonstrate that the minipig is a suitable model for man for assessing dermal absorption and hydrolysis of parabens, although the carboxylesterase profile in skin differs between human and minipig...
- Protective effect of N-acetyl-serotonin on the nonenzymatic lipid peroxidation in rat testicular microsomes and mitochondriaMariana B Gavazza
Catedra de Bioquimica, Facultad de Ciencias Veterinarias, Universidad Nacional de La Plata, B1900 AVW La Plata, Argentina
J Pineal Res 37:153-60. 2004..on the ascorbate-Fe(++) induced lipid peroxidation of polyunsaturated fatty acids (PUFAs) located in testis microsomes and mitochondria...
- Molecular code for transmembrane-helix recognition by the Sec61 transloconTara Hessa
Center for Biomembrane Research, Department of Biochemistry and Biophysics, Stockholm University, SE 106 91 Stockholm, Sweden
Nature 450:1026-30. 2007..Here, using in vitro translation of a model protein in the presence of dog pancreas rough microsomes to analyse a large number of systematically designed hydrophobic segments, we present a quantitative analysis of ..
- Structure-dependent inhibition of human and rat 11beta-hydroxysteroid dehydrogenase 2 activities by phthalatesBinghai Zhao
School of Public Health, Jilin University, Changchun, Jilin 130118, PR China
Chem Biol Interact 183:79-84. 2010..MEHP was a competitive inhibitor of 11beta-HSD2 enzymatic activity. We conclude that phthalates of a certain size act as competitive inhibitors...
- Subcellular and submitochondrial localization of phospholipid-synthesizing enzymes in Saccharomyces cerevisiaeK Kuchler
J Bacteriol 165:901-10. 1986..The other five enzymes tested in this study were common both to the outer mitochondrial membrane and to microsomes. The transmembrane orientation of the mitochondrial enzymes was investigated by protease digestion of intact ..
- Isolation and identification of intestinal CYP3A inhibitors from cranberry (Vaccinium macrocarpon) using human intestinal microsomesEunkyung Kim
Herbal Medicinal Products Division, Korea Food and Drug Administration, Seoul, Republic of Korea
Planta Med 77:265-70. 2011..Ericaceae)], midazolam, and human intestinal microsomes (HIM). Three triterpenes (maslinic acid, corosolic acid, and ursolic acid) were isolated...
- Aldosterone glucuronidation by human liver and kidney microsomes and recombinant UDP-glucuronosyltransferases: inhibition by NSAIDsKathleen M Knights
Department of Clinical Pharmacology, Flinders University, School of Medicine, Bedford Park, Adelaide 5042, Australia
Br J Clin Pharmacol 68:402-12. 2009To characterize: i) the kinetics of aldosterone (ALDO) 18beta-glucuronidation using human liver and human kidney microsomes and identify the human UGT enzyme(s) responsible for ALDO 18beta-glucuronidation and ii) the inhibition of ALDO ..
- Quantitative contribution of CYP2D6 and CYP3A to oxycodone metabolism in human liver and intestinal microsomesBojan Lalovic
Department of Pharmacy, University of Washington, Box 357630, Seattle, WA 98105, USA
Drug Metab Dispos 32:447-54. 2004..Multienzyme, Michaelis-Menten kinetics were observed for both oxidative reactions in microsomes prepared from five human livers...
- Identification of a ribosome receptor in the rough endoplasmic reticulumA J Savitz
Department of Biological Chemistry, UCLA School of Medicine 90024
Nature 346:540-4. 1990..Isolation of this domain has led to the identification, purification and characterization of the intact ribosome receptor, as well as its functional reconstitution into lipid vesicles...
- Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic targetRichard W Friesen
Department of Medicinal Chemistry, Merck Frosst Centre for Therapeutic Research, 16711 Trans Canada Highway, Kirkland, Quebec H9H 3L1, Canada
J Med Chem 51:4059-67. 2008
- Identification and characterization of alkenyl hydrolase (lysoplasmalogenase) in microsomes and identification of a plasmalogen-active phospholipase A2 in cytosol of small intestinal epitheliumM S Jurkowitz
Department of Medical Biochemistry, College of Medicine, Room 471, Hamilton Hall, 1645 Neil Avenue, The Ohio State University, Columbus, OH 43210, USA
Biochim Biophys Acta 1437:142-56. 1999..and physical properties of the lysoplasmalogenase were very similar to those of the enzyme in liver and brain microsomes. In developmental studies the specific activities of the small intestinal and liver enzymes increased markedly, ..
- Shotgun proteomics of Aspergillus niger microsomes upon D-xylose inductionJosé Miguel P Ferreira de Oliveira
Fungal Systems Biology, Laboratory of Systems and Synthetic Biology, Wageningen University, Dreijenplein 10, NL 6708 HB Wageningen, Netherlands
Appl Environ Microbiol 76:4421-9. 2010..niger, and the most prominent change found in this study was the recruitment of the 20S proteasomal subunits to the secretory organelles...
- BiP-dependent export of cholera toxin from endoplasmic reticulum-derived microsomesAlexandra Winkeler
Institut fur Zellbiologie, Rheinische Friedrich Wilhelms Universitat Bonn, Ulrich Haberland Str 61a, 53121 Bonn, Germany
FEBS Lett 554:439-42. 2003..an ER-luminal ATPase, was one of the required proteins the export of CT was analyzed using ER-derived CT-loaded microsomes. The resubstitution of extracted export-incompetent microsomes with purified BiP was sufficient to restore the ..
- Membrane topology of the 12- and the 25-kDa subunits of the mammalian signal peptidase complexK U Kalies
Max Delbruck Center for Molecular Medicine, Robert Rössle Stra sse 10, 13125 Berlin Buch, Germany
J Biol Chem 271:3925-9. 1996..sequence of the remaining 12-kDa subunit (SPC12) as well as the membrane topologies of SPC12 and SPC25 in rough microsomes. Both polypeptides span the membrane twice with their N and C termini facing the cytosol and contain only very ..
- Non-steroidal anti-inflammatory drugs interact with testosterone glucuronidationTaina Sten
Division of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Helsinki, FI 00014 Helsinki, Finland
Steroids 74:971-7. 2009..of two NSAIDs, diclofenac and ibuprofen, on testosterone and epitestosterone glucuronidation in human liver microsomes. In parallel, we have studied the inhibitory effect of these NSAIDs on recombinant UGT2B17 and UGT2B15, as well ..
- Uncoupling retro-translocation and degradation in the ER-associated degradation of a soluble proteinRobert J Lee
Department of Biological Sciences, University of Pittsburgh, Pittsburgh, PA 15260, USA
EMBO J 23:2206-15. 2004..assay was used to investigate the contributions of specific factors in the yeast cytosol and in ER-derived microsomes during the ERAD of a model, soluble polypeptide...
- The protein translocation channel binds proteasomes to the endoplasmic reticulum membraneKai Uwe Kalies
Institute of Biology, University of Lubeck, Lubeck, Germany
EMBO J 24:2284-93. 2005..Collectively, our data suggest that the Sec61 channel is a principal proteasome receptor in the ER membrane...
- Mammalian microsomal cytochrome P450 monooxygenase: structural adaptations for membrane binding and functional diversityP A Williams
Department of Molecular Biology MB 8, Scripps Research Institute, La Jolla, California 92037, USA
Mol Cell 5:121-31. 2000..This structure offers a template for modeling other mammalian P450s and should aid drug discovery and the prediction of drug-drug interactions...
- Characterization of electrogenic bromosulfophthalein transport in carnation petal microsomes and its inhibition by antibodies against bilitranslocaseSabina Passamonti
Dipartimento di Biochimica Biofisica e Chimica delle Macromolecole, Universita di Trieste, Italy
FEBS J 272:3282-96. 2005..In conclusion, carnation petals express a homologue of rat liver bilitranslocase, with a putative function in the membrane transport of secondary metabolites...
- Regulation of prostaglandin E synthases: effects of siRNA-mediated inhibition of microsomal prostaglandin E synthase-1Tove Båge
Department of Pediatric Dentistry, Institute of Odontology, Karolinska Institutet, Huddinge, Sweden
Biochim Biophys Acta 1773:1589-98. 2007..Moreover, mPGES-1 siRNA did not affect PGE2 levels, whereas PGF(2alpha) increased, suggesting a compensatory pathway of PGE2 synthesis when mPGES-1 is knocked down...
- Expression and regulation of microsomal prostaglandin E synthase-1 in human osteoarthritic cartilage and chondrocytesXinfang Li
Osteoarthritis Research Unit, Centre Hospitalier de l Universite de Montreal, Hopital Notre Dame, Montreal, Quebec, Canada
J Rheumatol 32:887-95. 2005..We analyzed expression of mPGES-1 in human normal and osteoarthritic (OA) cartilage and determined the effect of different inflammatory agonists on the expression of mPGES-1 in OA chondrocytes...
- Glucuronidation activity of the UGT2B17 enzyme toward xenobioticsDavid Turgeon
Oncology and Molecular Endocrinology Research Center, Centre de Recherche de l Université Laval, Laval University, Quebec City, Quebec, Canada
Drug Metab Dispos 31:670-6. 2003..Taken together, these data suggest a role of UGT2B17 for the hepatic detoxification...
- Hyperplastic gastric tumors induced by activated macrophages in COX-2/mPGES-1 transgenic miceHiroko Oshima
Department of Pharmacology, Graduate School of Medicine, Kyoto University, Kyoto, Japan
EMBO J 23:1669-78. 2004..Furthermore, Helicobacter infection upregulated epithelial PGE2 production, suggesting that the COX-2/mPGES-1 pathway contributes to the Helicobacter-associated gastric tumorigenesis...
- Microsomal epoxide hydrolase polymorphism and susceptibility to ovarian cancerS W Baxter
VBCRC Cancer Genetics Laboratory, Peter MacCallum Cancer Institute, Locked Bag No 1 A Beckett Street, Melbourne, Victoria, 8006, Australia
Cancer Lett 177:75-81. 2002..Furthermore previous disease association studies of exon 3 alleles which utilized the PCR-RFLP assay may be compromised by the existence of a codon 119 G>A polymorphism which may be common in Caucasian populations...
- Interaction of murine BiP/GRP78 with the DnaJ homologue MTJ1M Chevalier
Department of Medicinal Chemistry and Pharmacognosy, University of Illinois, Chicago, Illinois 60607 7173, USA
J Biol Chem 275:19620-7. 2000..Full-length DnaJ does not stimulate BiP over the range of concentrations investigated. These results indicate that the J domain of MTJ1 is sufficient for its interaction with BiP/GRP78 and cannot be substituted by E. coli DnaJ...
- Microsomal prostaglandin E synthase-1 and 5-lipoxygenase: potential drug targets in cancerO Radmark
Department of Medical Biochemistry and Biophysics, Division of Physiological Chemistry II, Karolinska Institutet, Stockholm, Sweden
J Intern Med 268:5-14. 2010..Several compounds that target COX-2 or MPGES-1 also inhibit 5-lipoxygenase. This may be advantageous for treatment of some forms of cancer...
- Functional identification of two nonredundant Arabidopsis alpha(1,2)fucosyltransferases specific to arabinogalactan proteinsYingying Wu
Department of Environmental and Plant Biology, Ohio University, Athens, Ohio 45701, USA
J Biol Chem 285:13638-45. 2010..AtFUT4 and AtFUT6 are the first enzymes to be characterized for AGP glycosylation and further our understanding of cell wall biosynthesis...
- The involvement of phospholipid:diacylglycerol acyltransferases in triacylglycerol productionA Banas
Scandinavian Biotechnology Research AB, SE 268 31 Svalöv, Sweden
Biochem Soc Trans 28:703-5. 2000..Further, we show that significant PDAT activity is also present in vegetative tissues of Arabidopsis thaliana...
- Purification of microsomal signal peptidase as a complexE A Evans
Proc Natl Acad Sci U S A 83:581-5. 1986We report here the purification to near homogeneity of signal peptidase from canine pancreatic microsomes. Purification was monitored using an improved post-translational assay...
- Effects of AF3442 [N-(9-ethyl-9H-carbazol-3-yl)-2-(trifluoromethyl)benzamide], a novel inhibitor of human microsomal prostaglandin E synthase-1, on prostanoid biosynthesis in human monocytes in vitroAnnalisa Bruno
Department of Medicine and Center of Excellence on Aging, School of Medicine, G d Annunzio University and G d Annunzio University Foundation, Ce S I, Chieti 66100, Italy
Biochem Pharmacol 79:974-81. 2010..Pharmacological inhibition of mPGES-1 did not translate into redirection of PGH(2) metabolism towards other terminal PG synthases in monocytes. The functional relevance of this observation deserves to be investigated in vivo...
- Suppression of Rft1 expression does not impair the transbilayer movement of Man5GlcNAc2-P-P-dolichol in sealed microsomes from yeastJeffrey S Rush
Department of Molecular and Cellular Biochemistry, University of Kentucky College of Medicine, Lexington, Kentucky 40536, USA
J Biol Chem 284:19835-42. 2009..When sealed microsomes from wild type cells and cells depleted of Rft1 were incubated with GDP-[(3)H]mannose or UDP-[(3)H]GlcNAc in the ..
- Distinction of microsomal prostaglandin E synthase-1 (mPGES-1) inhibition from cyclooxygenase-2 inhibition in cells using a novel, selective mPGES-1 inhibitorGabriel Mbalaviele
Pfizer Inc, Chesterfield, MO 63017, USA
Biochem Pharmacol 79:1445-54. 2010..This profile of mPGES-1 inhibition, distinct from COX-2 inhibition in cells, validates mPGES-1 as an attractive target for therapeutic intervention...
- Quantitative profiling of differentiation-induced microsomal proteins using isotope-coded affinity tags and mass spectrometryD K Han
University of Connecticut Health Center, 263 Farmington Ave, Farmington, CT 06030-0002, USA
Nat Biotechnol 19:946-51. 2001..The method and the new software tools to support it are well suited to the large-scale, quantitative analysis of membrane proteins and other classes of proteins that have been refractory to standard proteomics technology...
- FKBP binding characteristics of cardiac microsomes from diverse vertebratesL H Jeyakumar
Department of Biological Sciences, Vanderbilt University, Nashville, Tennessee 37235, USA
Biochem Biophys Res Commun 281:979-86. 2001..In this study, cardiac microsomes were isolated from diverse vertebrates: human, rabbit, rat, mice, dog, chicken, frog, and fish and were analyzed ..
- Neurosteroid metabolism. 7 alpha-Hydroxylation of dehydroepiandrosterone and pregnenolone by rat brain microsomesY Akwa
, Lab Hormones, Bicetre, France
Biochem J 288:959-64. 1992Two 'neurosteroids', dehydroepiandrosterone (DHEA) and pregnenolone (PREG), are converted by rat brain microsomes into polar metabolites, identified as the respective 7 alpha-hydroxylated (7 alpha-OH) derivatives by the 'twin ion' ..
- Coexpression of microsomal-type prostaglandin E synthase with cyclooxygenase-2 in brain endothelial cells of rats during endotoxin-induced feverK Yamagata
Department of Neuropharmacology, Tokyo Metropolitan Institute for Neuroscience, Fuchu 183 8526, Japan
J Neurosci 21:2669-77. 2001..These results demonstrate that brain endothelial cells play an essential role in the PGE(2) production during fever by expressing COX-2 and mPGES...
- Biosynthesis of triacylglycerols containing ricinoleate in castor microsomes using 1-acyl-2-oleoyl-sn-glycero-3-phosphocholine as the substrate of oleoyl-12-hydroxylaseJ T Lin
USDA, ARS, Western Regional Research Center, Albany, California 94710, USA
Lipids 33:59-69. 1998..Thus, the productions of these triacylglycerols in this relatively short incubation (30 min), as well as the availability of 2-oleoyl-PC in vivo, reflect the in vivo drive to produce triricinolein in castor bean...
- In vitro glucuronidation of 2,2-bis(bromomethyl)-1,3-propanediol by microsomes and hepatocytes from rats and humansGolriz Rad
Department of Clinical Pharmacology, College of Medicine, The University of Arizona, P O Box 245050, Tucson, AZ 85724 5050, USA
Drug Metab Dispos 38:957-62. 2010..In addition, the glucuronidation activities of human intestinal microsomes and specific human hepatic UDP-glucuronosyltransferase (UGT) enzymes for BMP were determined...
- Lipid peroxidation and generations of oxygen radicals induced by cephaloridine in renal cortical microsomes of ratsY Suzuki
Department of Toxicology and Clinical Pharmacology, Faculty of Pharmaceutical Sciences, Higashi Nippon Gakuen University, Hokkaido, Japan
Jpn J Pharmacol 52:233-43. 1990To investigate whether oxygen radicals would be generated by cephaloridine (CER) in the renal cortical microsomes obtained from rats and whether the microsomal lipid peroxidation would be promoted by CER, the microsomes were incubated ..
- Cell-free synthesis of functional and endotoxin-free antibody Fab fragments by translocation into microsomesHelmut Merk
RiNA Netzwerk RNA Technologien GmbH, Berlin, Germany
Biotechniques 53:153-60. 2012..Moreover, the system is compatible with PCR-generated linear templates enabling automated generation of antibody fragments in a high-throughput manner, and facilitating its application for screening and validation purposes...
- UDP-glucuronosyltransferase 1A1 is the principal enzyme responsible for etoposide glucuronidation in human liver and intestinal microsomes: structural characterization of phenolic and alcoholic glucuronides of etoposide and estimation of enzyme kineticsZhiming Wen
School of Pharmacy, CB 7360, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599 7360, USA
Drug Metab Dispos 35:371-80. 2007..one phenolic (EPG) and two alcoholic glucuronides (EAG1 and EAG2), were biosynthesized in vitro with human liver microsomes (HLMs), and identified by liquid chromatography-electrospray ionization-mass spectrometry and confirmed by beta-..
- A unified model for predicting human hepatic, metabolic clearance from in vitro intrinsic clearance data in hepatocytes and microsomesRobert J Riley
Department of Physical and Metabolic Science, AstraZeneca R and D Charnwood, Loughborough, Leicestershire, LE11 5RH, UK
Drug Metab Dispos 33:1304-11. 2005..vivo intrinsic clearance (CL(int, in vivo)) and hepatic clearance (CL(h)) from in vitro data in hepatocytes and microsomes by applying the unbound fraction in blood (fu(b)) and in vitro incubations (fu(inc))...
- Metabolism of cyadox by the intestinal mucosa microsomes and gut flora of swine, and identification of metabolites by high-performance liquid chromatography combined with ion trap/time-of-flight mass spectrometryNing Xu
MAO Key Laboratory of Food Safety Evaluation National Reference Laboratory of Veterinary Drug Residues HZAU, Huazhong Agricultural University, Wuhan, Hubei 430070, PR China
Rapid Commun Mass Spectrom 25:2333-44. 2011..To reveal biotransformation of CYX in swine intestine, CYX was incubated with swine intestinal microsomes and mucosa in the presence of an NADPH-generating system and swine ileal flora and colonic flora, respectively...
- Identification of an inhibitor of hsc70-mediated protein translocation and ATP hydrolysisS W Fewell
Department of Biological Sciences, University of Pittsburgh, Pittsburgh, Pennsylvania 15260, USA
J Biol Chem 276:910-4. 2001..Biochemical studies demonstrate that R/1 most likely exerts these effects by altering the oligomeric state of hsc70...
- Morphine metabolism in human skin microsomesS Heilmann
Institut fur Pharmazie, Freie Universitat Berlin, Berlin, Germany
Skin Pharmacol Physiol 25:319-22. 2012..We use skin microsomes to elucidate the impact of skin metabolism on the activity of topically applied morphine...
- Dual subcellular localization of the 3 beta-hydroxysteroid dehydrogenase isomerase: characterization of the mitochondrial enzyme in the bovine adrenal cortexN Cherradi
Unité INSERM 244, DBMS BRCE, Centre d Etudes Nucléaires, Grenoble, France
J Steroid Biochem Mol Biol 46:773-9. 1993..It is considered to be mainly localized in microsomes; however, 3 beta-HSD/I activity has also been described to be associated with mitochondrial preparations...
- Regulation of prostaglandin E2 biosynthesis by inducible membrane-associated prostaglandin E2 synthase that acts in concert with cyclooxygenase-2M Murakami
Department of Health Chemistry, School of Pharmaceutical Sciences, Showa University, 1 5 8 Hatanodai, Shinagawa ku, Tokyo 142 8555, Japan
J Biol Chem 275:32783-92. 2000..Thus, COX-2 and mPGES are essential components for delayed PGE(2) biosynthesis, which may be linked to inflammation, fever, osteogenesis, and even cancer...
- Lyso-glycosphingolipids mobilize calcium from brain microsomes via multiple mechanismsEmyr Lloyd-Evans
Department of Biological Chemistry, Weizmann Institute of Science, Rehovot 76100, Israel
Biochem J 375:561-5. 2003..GSL (glycosphingolipid), GlcCer (glucosylceramide), modulates Ca2+ release from intracellular stores and from microsomes by sensitizing the RyaR (ryanodine receptor), a major Ca2+-release channel of the endoplasmic reticulum, whereas ..
- Functional co-expression of xenobiotic metabolizing enzymes, rat cytochrome P450 1A1 and UDP-glucuronosyltransferase 1A6, in yeast microsomesShin ichi Ikushiro
Department of Life Science, Graduate School of Science, Himeji Institute of Technology, Harima Science Garden City, Hyogo 678 1297, Japan
Biochim Biophys Acta 1672:86-92. 2004..Co-expression of P450 1A1 and UGT1A6 in yeast microsomes was confirmed by immunoblot analysis...
- Inhibition by allyl sulfides and phenethyl isothiocyanate of methyl-n-pentylnitrosamine depentylation by rat esophageal microsomes, human and rat CYP2E1, and Rat CYP2A3Chantey R Morris
Eppley Institute for Research in Cancer, Omaha, Nebraska 68198, USA
Nutr Cancer 48:54-63. 2004..The test inhibitors were incubated with [3H]-MPN, NADPH-generating system and rat esophageal microsomes (REM) or a cytochrome P450 (CYP)...
- Anti-P450lpr antiserum inhibits specific monooxygenase activities in LPR house fly microsomesG D Wheelock
Department of Entomology, Cornell University, Ithaca, New York 14853
J Exp Zool 264:153-8. 1992Monooxygenase activity in microsomes from the LPR strain of house fly (Musca domestica L.) was inhibited by anti-P450lpr, and antiserum specific for house fly cytochrome P450lpr...
- Characterization of the novel defective CYP2C9*24 alleleDarja Herman
Institute of Biochemistry, Faculty of Medicine, Vrazov trg 2, SI 1000 Ljubljana, Slovenia
Drug Metab Dispos 35:831-4. 2007..Carbon monoxide difference spectra were recorded on dithionite-reduced microsomes, and protein was determined by Western blotting. Transfection with CYP2C9...
- N-acetylaspartate synthesis in the brain: mitochondria vs. microsomesPrasanth S Ariyannur
Rm C 2069, Department of Anatomy, Physiology and Genetics, Uniformed Services University of the Health Sciences, 4301 Jones Bridge Road, Bethesda, MD 20814, USA
Brain Res 1227:34-41. 2008..in the crude supernatant was present in the mitochondrial fraction which is about 5 times more than that in the microsomes. We found similar results in the case of the enzyme from bovine brain...
- Effect of the beta-glucuronidase inhibitor saccharolactone on glucuronidation by human tissue microsomes and recombinant UDP-glucuronosyltransferasesLauren Oleson
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, 136 Harrison Ave, M V Rm 308, Boston, MA 02111, USA
J Pharm Pharmacol 60:1175-82. 2008Glucuronidation studies using microsomes and recombinant uridine diphosphoglucuronosyltransferases (UGTs) can be complicated by the presence of endogenous beta-glucuronidases, leading to underestimation of glucuronide formation rates...
- Development of an optimized procedure for the preparation of rat intestinal microsomes: comparison of hepatic and intestinal microsomal cytochrome P450 enzyme activities in two rat strainsA Bruyere
Department of Pharmacokinetics and Drug Metabolism, Technologie Servier, Orleans, France
Xenobiotica 39:22-32. 2009The objective of this study was to characterize cytochrome P450 (CYP) activities in both intestinal and hepatic microsomes from Wistar and Sprague-Dawley rats...
- Human native soluble CD40L is a biologically active trimer, processed inside microsomesF Pietravalle
Glaxo Institute for Molecular Biology, Geneva, Switzerland
J Biol Chem 271:5965-7. 1996..Subcellular fractionation experiments have shown that the transmembrane CD40L is processed inside the microsomes and that its cleavage is stimulation-dependent...
- Substrate-dependent functional alterations of seven CYP2C9 variants found in Japanese subjectsKeiko Maekawa
Division of Functional Biochemistry and Genomics, National Institute of Health Sciences, 1 18 1 Kamiyoga, Setagaya Ku, Tokyo 158 8501, Japan
Drug Metab Dispos 37:1895-903. 2009..3, CYP2C9.13, CYP2C9.26, and CYP2C9.33 and by 56 to 75% in CYP2C9.28 and CYP2C9.30. These findings suggest the necessity for careful administration of losartan and glimepiride to patients bearing these six alleles...
- Topology of 3 beta-hydroxy-5-ene-steroid dehydrogenase/delta 5-delta 4-isomerase in adrenal cortex mitochondria and microsomesL A Sauer
Institute for Medical Research, Mary Imogene Bassett Hospital, Cooperstown, New York 13326
Endocrinology 134:751-9. 1994..Enzyme activity is located in both microsomes and mitochondria...
- Triclosan reduces microsomal prostaglandin E synthase-1 expression in human gingival fibroblastsM Mustafa
Department of Pediatric Dentistry, Institute of Odontology, Huddinge, Sweden
J Clin Periodontol 32:6-11. 2005....
- Cell-free synthesis of membrane proteins: tailored cell models out of microsomesSusanne F Fenz
Leiden Institute of Physics, Leiden University, PO Box 9504, 2300 RA Leiden, The Netherlands
Biochim Biophys Acta 1838:1382-8. 2014..system in this study is based on insect lysates, which provide endoplasmic reticulum derived vesicles named microsomes. It enables signal-induced translocation and posttranslational modification of de novo synthesized membrane ..
- Coumarin metabolism by rat esophageal microsomes and cytochrome P450 2A3L B von Weymarn
Department of Biochemistry, Molecular Biology and Biophysics, University of Minnesota Cancer Center, Minneapolis, Minnesota 55455, USA
Chem Res Toxicol 14:1386-92. 2001..In the study described here, the products of 14C-coumarin metabolism by rat esophageal microsomes were identified and quantified...
- Detection of aromatase inhibitors in vitro using rat ovary microsomesJ Odum
Syngenta Central Toxicology Laboratory, Alderley Park, Macclesfield, Cheshire SK10 4TJ, UK
Toxicol Lett 129:119-22. 2002..Rat ovary microsomes were used as the enzyme source, as endocrine disruption studies are most commonly carried out in this species...
- Evaluation of cytochrome P450 activity in vitro, using dermal and hepatic microsomes from four species and two keratinocyte cell lines in cultureKamilla Rolsted
Department of Pharmaceutics and Analytical Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, Universitetsparken 2, 2100, Copenhagen, Denmark
Arch Dermatol Res 300:11-8. 2008..To achieve this, a cocktail of six selective CYP450 probe substrates were incubated with dermal and hepatic microsomes isolated from mouse, rat, minipig and man...
- Biotransformation of 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK) in peripheral human lung microsomesGraeme B J Smith
Department of Pharmacology and Toxicology, Queen s University Kingston, Ontario, Canada
Drug Metab Dispos 31:1134-41. 2003..enzymes to 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK) biotransformation were assessed in human lung microsomes prepared from peripheral lung specimens obtained from seven subjects...
- Inhibitors of CYP6D1 in house fly microsomesJ G Scott
Department of Entomology, Cornell University, Ithaca, NY 14853 0901, USA
Insect Biochem Mol Biol 26:645-9. 1996..a non-CYP6D1-specific monooxygenase activity, 21 compounds were evaluated as inhibitors of CYP6D1 in house fly microsomes. CYP6D1 was strongly inhibited by xanthotoxin, chlorpyrifos, beta-naphthoflavone, piperonyl butoxide and 5-..
- Identification and development of mPGES-1 inhibitors: where we are at?Hui Hua Chang
Arizona Cancer Center, University of Arizona, Tucson, AZ 85724, USA
Future Med Chem 3:1909-34. 2011..This review summarizes the structures, and the in vitro and in vivo activities of these novel mPGES-1 inhibitors. Challenges that have been encountered are also discussed...
- The effect of beta-naphthoflavone on the metabolism of amiodarone by hepatic and extra-hepatic microsomesMarwa E Elsherbiny
Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, Edmonton, Alberta, Canada T6G 2N8
Toxicol Lett 195:147-54. 2010..In rats, beta-naphthoflavone was found to increase desethylamiodarone forming activity in lung and kidney microsomes. Amiodarone increased beta-naphthoflavone mediated induction of CYP1A1 gene expression in liver, lung and kidney...
- Molecular cloning and characterization of p64, a chloride channel protein from kidney microsomesD Landry
Department of Medicine, College of Physicians and Surgeons, Columbia University, New York, New York 10032
J Biol Chem 268:14948-55. 1993..of its mRNA in Xenopus laevis oocytes led to the insertion of a protein with the appropriate molecular mass in microsomes but not in the plasma membrane. It is likely that p64 represents the chloride channel of intracellular organelles...
- The effect of alpha-tocopherol on lipid peroxidation of microsomes and mitochondria from rat testisM B Gavazza
Catedra de Bioquimica, Facultad de Ciencias Veterinarias, Argentina
Prostaglandins Leukot Essent Fatty Acids 74:247-54. 2006..out to evaluate the effect of alpha-tocopherol in vitro on ascorbate-Fe(++) lipid peroxidation of rat testis microsomes and mitochondria...
- Toluene monooxygenase from the fungus Cladosporium sphaerospermumDion M A M Luykx
Division of Industrial Microbiology, Wageningen University, PO Box 8129, 6700 EV Wageningen, The Netherlands
Biochem Biophys Res Commun 312:373-9. 2003..These results indicated that TOMO is a cytochrome P450. TOMO and its corresponding reductase were eventually purified by a simultaneous purification revealing apparent molecular masses of 58 and 78 kDa, respectively...
- A preliminary characterization of the mutagenicity of atmospheric particulate matter collected during sugar cane harvesting using the Salmonella/microsome microsuspension assayGisela de Aragão Umbuzeiro
CETESB Cia de Tecnologia de Saneamento Ambiental, Av Prof Frederico Hermann Jr, 345, 05459 900, Sao Paulo, SP, Brazil
Environ Mol Mutagen 49:249-55. 2008..The Salmonella/microsome assay can be an important tool to monitor the atmosphere for mutagenicity during sugar cane harvesting season...
- Assembly of ER-associated protein degradation in vitro: dependence on cytosol, calnexin, and ATPA A McCracken
University of Nevada, Biology Department, Reno 89557, USA
J Cell Biol 132:291-8. 1996..procedures for post-translational translocation of radiolabeled prepro-alpha factor into isolated yeast microsomes were modified to inhibit glycosylation and to include a posttranslocation "chase" incubation period to monitor ..
- Identification of cytochrome P450 enzymes involved in the metabolism of 4'-methoxy-alpha-pyrrolidinopropiophenone (MOPPP), a designer drug, in human liver microsomesD Springer
Department of Experimental and Clinical Toxicology, University of Saarland, Homburg Saar, Germany
Xenobiotica 33:989-98. 2003..demethylated major metabolite 4'-hydroxy-pyrrolidinopropio-phenone (HO-PPP) was studied in pooled human liver microsomes (HLM) and in cDNA-expressed human hepatic cytochrome P450 (CYP) enzymes. 2...
- Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: comparison with liver and intestinal glucuronidation and impact of albuminKatherine L Gill
Centre for Applied Pharmacokinetic Research, School of Pharmacy and Pharmaceutical Sciences, University of Manchester, Manchester, United Kingdom
Drug Metab Dispos 40:825-35. 2012..This study characterized glucuronidation clearance (CL(int, UGT)) in human kidney, liver, and intestinal microsomes in the presence and absence of bovine serum albumin (BSA) for seven drugs with differential UDP-..
- Structural requirements for transport of preprocecropinA and related presecretory proteins into mammalian microsomesG Schlenstedt
Zentrum Biochemie/Abt. Biochemie II, , Germany
J Biol Chem 267:24328-32. 1992..reductase (which comprises 252 amino acid residues) are processed by and transported into mammalian microsomes. Transport of both precursor proteins can take place cotranslationally, i.e...
- Inhibition of lipid peroxidation and protein oxidation by endogenous and exogenous antioxidants in rat brain microsomes in vitroCesare Mancuso
Institute of Pharmacology, Catholic University School of Medicine, Largo F Vito, 1, 00168 Rome, Italy
Neurosci Lett 518:101-5. 2012..and its precursor biliverdin, was compared with that of the dietary antioxidant alpha-tocopherol in rat brain microsomes exposed to peroxyl radical or peroxynitrite in vitro...
- TFPIβ is the GPI-anchored TFPI isoform on human endothelial cells and placental microsomesThomas J Girard
Division of Hematology, Washington University School of Medicine, 660 SEuclid Ave, St Louis, MO 63110, USA
Blood 119:1256-62. 2012..Our studies show that the form of TFPI released by PIPLC treatment of cultured endothelial cells and placental microsomes is actually TFPIβ based on (1) migration on SDS-PAGE before and after deglycosylation, (2) the lack of a Kunitz-..
- Identification of a novel class of anti-inflammatory compounds with anti-tumor activity in colorectal and lung cancersHui Hua Chang
Arizona Cancer Center, The University of Arizona, Tucson, AZ 85724, USA
Invest New Drugs 30:1865-77. 2012..p. of PGE0001 at 100 mg/kg decreases serum PGE(2) levels in mice within 5 h. In summary, our data suggest that the identified compound PGE0001 exerts anti-tumor activity via the inhibition of the PGE(2) synthesis pathway...
- Cleavage of a tail-anchored protein by signal peptidaseIngmarie Nilsson
Department of Biochemistry and Biophysics, Stockholm University, SE 106 91, Stockholm, Sweden
FEBS Lett 516:106-8. 2002..Here, we show that a tail-anchored protein can be cleaved by signal peptidase and that the sequence requirements for efficient cleavage seem to be the same as for cleavage of co-translationally targeted SRP-dependent proteins...
- Na+, K+-ATPase activity in gill microsomes from the blue crab, Callinectes danae, acclimated to low salinity: novel perspectives on ammonia excretionDouglas C Masui
Departamento de Quimica, Faculdade de Filosofia, Ciencias e Letras de Ribeirao Preto, Universidade de São Paulo Ribeirão Preto 14040 901, SP, Brasil
Comp Biochem Physiol A Mol Integr Physiol 153:141-8. 2009..Ammonium and potassium ions synergistically stimulated specific activity up to 72%, inferring that these ions bind to different sites on the enzyme molecule, each modulating stimulation by the other...
- Structure-based discovery of inhibitors of microsomal prostaglandin E2 synthase-1, 5-lipoxygenase and 5-lipoxygenase-activating protein: promising hits for the development of new anti-inflammatory agentsRosa De Simone
Department of Pharmaceutical Sciences, University of Salerno, Via Ponte Don Melillo, 84084 Fisciano SA, Italy
J Med Chem 54:1565-75. 2011..2 μM, (II) compound 20 that dually inhibits 5-lipoxygenase and mPGES-1, and (III) compound 7 apparently acting as 5-lipoxygenase-activating protein inhibitor (IC(50) = 0.4 μM)...
- Glucuronidation of the green tea catechins, (-)-epigallocatechin-3-gallate and (-)-epicatechin-3-gallate, by rat hepatic and intestinal microsomesVanessa Crespy
Nestle Research Center, PO Box 44, CH 1000 Lausanne 26, Switzerland
Free Radic Res 38:1025-31. 2004..We investigated the glucuronidation of these compounds and of quercetin by microsomes. Quercetin was almost fully glucuronidated by liver microsomes after 3 h, whereas ECg and ECGg were conjugated ..
- A low degree of fatty acid unsaturation leads to high resistance to lipid peroxidation in mitochondria and microsomes of different organs of quail (Coturnix coturnix japonica)Ana María Gutiérrez
Catedra de Bioquimica, Facultad de Ciencias Veterinarias, Universidad Nacional de La Plata, La Plata, Argentina
Mol Cell Biochem 282:109-15. 2006..present study was to analyse the fatty acid composition and non-enzymatic lipid peroxidation of mitochondria and microsomes obtained from liver, heart and brain of quail (Coturnix coturnix japonica), a short-lived bird...
- beta-Dystroglycan can be revealed in microsomes from mdx mouse muscle by detergent treatmentNicolas Cluchague
Faculte de Medecine, UMR CNRS 6026, CS 34317, 35043 Rennes Cedex France
FEBS Lett 572:216-20. 2004..This result shows that, in dystrophin-deficient muscles, beta-dystroglycan is indeed targeted to the plasma membrane but remains inaccessible to classical solubilizing treatments and to antibodies used for immunolocalization...
- Inhibition of hypoxia inducible factor-1alpha by dihydroxyphenylethanol, a product from olive oil, blocks microsomal prostaglandin-E synthase-1/vascular endothelial growth factor expression and reduces tumor angiogenesisErika Terzuoli
Department of Molecular Biology, University of Siena, Siena, Italy
Clin Cancer Res 16:4207-16. 2010..2-(3,4-dihydroxyphenil)-ethanol (DPE), a polyphenol present in olive oil, has been found to attenuate the growth of colon cancer cells, an effect presumably related to its anti-inflammatory activity...
- Effects of drugs with muscle-related side effects and affinity for calsequestrin on the calcium regulatory function of sarcoplasmic reticulum microsomesEunjung Kim
Department of Chemistry, Washington State University, Pullman, Washington 99164 4660, USA
Mol Pharmacol 68:1708-15. 2005..clearly showed that these compounds affect Ca2+ release and reduce the total Ca2+ content of the purified SR microsomes, matching well with our previous results with purified recombinant CSQ...
- The Role of Cyp2b in Toxicant Metabolism and SensitivityWilliam S Baldwin; Fiscal Year: 2012..In aim 1, we will use this mouse model to estimate Cyp2b metabolism using microsomes from untreated and TCPOBOP-treated wild-type and Cyp2b-KD mice...
- Rational Development of Anti-Trypanosoma Cruzi DrugsMichael H Gelb; Fiscal Year: 2013..Follow up studies will test aqueous solubility, stability in liver microsomes, and inhibition of human CYP450 enzymes...
- ELECTROCATALYTIC STUDIES OF TOXIC POLLUTANT ACTIVATIONJames F Rusling; Fiscal Year: 2013..b>Microsomes or pure enzymes can be used...
- Membrane-associated PDE3-binding proteins in human myocardiumMatthew A Movsesian; Fiscal Year: 2013..with membrane-associated PDE3 isoforms in human myocardium: PDE3A-binding proteins in purified high-density microsomes from human left ventricular myocardium will be co-immunoprecipitated with anti-PDE3 antibodies and co-affinity ..
- A Diarylheptanoid Scaffold to Treat TaopathiesChad A Dickey; Fiscal Year: 2013..The eADME studies will include metabolism in mouse and human liver microsomes, human plasma protein binding, water solubility testing, broad receptor and ion channel profiling including hERG,..
- Pharmacokinetics and Metabolism of Oxidized CurcuminClaus Schneider; Fiscal Year: 2013..tissue distribution, and metabolism of the oxidative metabolites of curcumin in the mouse and in human liver microsomes. The following specific aims will be performed: (1) To develop a specific and accurate isotope- dilution based ..
- Bifunctional Nitric Oxide Donor Refractory to Nitrate ToleranceGARRY JOHN SOUTHAN; Fiscal Year: 2012..Aim #2: Establish the in vitro metabolic profile of R-100 induced by exposure to human liver and intestinal microsomes. Prominent metabolites will be synthesized and evaluated for secondary metabolism in human microsomes...
- Factors Determining Bisphenol A Disposition in Human InfantsD Gail McCarver; Fiscal Year: 2013..ontogeny and the developmental changes in BPA metabolism in a large, well-characterized bank of human liver microsomes from donors ranging in age from 8 weeks gestation to 18 years postnatal age...
- Cholesterol metabolizing P450s: structure and functionIrina A Pikuleva; Fiscal Year: 2013..24S-hydroxylation (6-10-fold) mediated by either purified recombinant CYP46A1 or isolated bovine brain microsomes. Also, we found that some of the drugs that inhibit CYP46A1 inhibit CYP11A1 whose crystal structure we ..
- PGRMC1: A Regulator of CYP3A ActivityErin G Schuetz; Fiscal Year: 2010..without expressed PGRMC;(b) CYP3A4/POR supersomes reconstituted with purified PGRMC1;and (c) pooled human liver microsomes in which PGRMC1 activity is decreased with PGRMC1 inhibitory antibodies...
- Halogenated Alkenes and Microsomal GSH-transferasesMichael J Kelner; Fiscal Year: 2010..the nephrotoxic and nephrocarcinogenic effects of vicinal haloalkenes stems from their conversion in hepatic microsomes by the enzyme microsomal glutathione transferase-1 (MGST1) to GSH S-conjugates, which are transported to ..
- Metabolism of Carcinogenic Tobacco-Specific NitrosaminesStephen S Hecht; Fiscal Year: 2013..the structure of an inhibitor of carcinogen metabolic activation, which we have identified in human lung microsomes. 6...
- Development of a novel agent for lung cancer preventionArun Kumar Sharma; Fiscal Year: 2013..Furthermore, to begin establishing the mechanism, we will carry out its metabolism using liver microsomes to establish if p-XS-Asp will cleave into active metabolites p-XSeH and aspirin, and evaluate COX-2-mediated pro-..
- Bioactivation of PBDEs by Human Cytochrome P-450James R Olson; Fiscal Year: 2013..Interindividua variability in the in vitro metabolism of PBDEs will be assessed utilizing both human liver microsomes, with up to a 100-fold range in the level of CYP2B6 activity, and recombinant polymorphic variants of human ..
- IND-enabling Studies and GMP Scale-up of 18-Methoxycoronaridine hydrochloride(18-Scott Freeman; Fiscal Year: 2013..bacterial reverse mutation, chromosome aberration in human peripheral blood lymphocytes, p450 using human liver microsomes and cardiac action potential duration in rabbit Purkinje fibers and in vivo mouse micronucleus, all of which ..
- Enantioselective Metabolism Influences PCB Developmental NeurotoxicityIsaac N Pessah; Fiscal Year: 2013..binding and metabolism of pure PCB atropisomers by P450 enzymes will be investigated using murine and human microsomes and tissue slices, as well as recombinant human P450 enzymes...
- MOLECULAR BASIS OF HUMAN CYTOCHROME P450 3A FUNCTIONJames R Halpert; Fiscal Year: 2013..physiological effectors on cooperativity, catalytic efficiency, and functional heterogeneity of CYP3A4 in microsomes and model membranes RELEVANCE (See instructions): Cytochromes P450 3A break down a wide variety of compounds to ..
- Acinar Biology and Pancreatic DiseaseGuy E Groblewski; Fiscal Year: 2011..that D52 is a phosphatidylinositol-3-phosphate binding protein that copurifies with clathrin-coats from acinar microsomes. This proposal aims to delineate the precise functional roles of VAMP2- and VAMP8-positive ZGs in the acinar ..
- Characterization of a Novel Selective Cytochrome P450 3A5 SubstrateMICHAEL DARIN CAMERON; Fiscal Year: 2013..using a CYP3A assay measuring testosterone hydroxylation or midazolam hydroxylation by pooled human liver microsomes. While both of these substrates are metabolized by CYP3A4 and CYP3A5, the resulting inhibition constants ..
- Role of CYP2J2 in Xenobiotic Induced QT-prolongationRHEEM ANGELA TOTAH; Fiscal Year: 2013..effect of CYP2J2 inhibition by drugs that cause QT- prolongation in both a recombinant system and cardiac microsomes from transgenic mice that express CYP2J2 in their hearts...
- CYP2A5 and alcoholic liver diseaseYongke Lu; Fiscal Year: 2013..of CYP2E1 is a novel new finding, because most studies about microsomal ethanol metabolism were carried with rat microsomes, which lack CYP2A3, the ortholog of mouse CYP2A5...
- In vitro detection of anti-TB liver metabolites in early drug discoveryScott G Franzblau; Fiscal Year: 2013..Enzymatic MGS includes liver microsomes, S9 fractions, recombinant CYP450 enzymes and combinations of these systems and can be used in a one-pot assay...
- Drug Discovery for Human African TrypanosomiasisRichard Tidwell; Fiscal Year: 2013..vitro experiments will be done to assess aqueous solubility, the stability of compounds to metabolism by liver microsomes, and membrane permeability...
- Preclinical Pharmacological Studies of Antitumor & Other Therapeutic AgentsPatricia Noker; Fiscal Year: 2010..g., S9 fractions, microsomes, hepatocytes, P450 isoforms, liver slices);and (5) assessment of pharmacodynamic effects in tumor or surrogate ..
- Preclinical Pharmacological Studies of Antitumor and Other Therapeutic AgentsMatthew Ames; Fiscal Year: 2011..g., S9 fractions, microsomes, hepatocytes, P450 isoforms, liver slices);and (5) assessment of pharmacodynamic effects in tumor or surrogate ..
- Preclinical Pharmacological Studies of Antitumor and Other Therapeutic AgentsMatthew Ames; Fiscal Year: 2010..g., S9 fractions, microsomes, hepatocytes, P450 isoforms, liver slices);and (5) assessment of pharmacodynamic effects in tumor or surrogate ..
- Preclinical Pharmacological Studies of Antitumor &Other Therapeutic AgentsPatricia Noker; Fiscal Year: 2011
- Preclinical Pharmacological Studies of Antitumor &Other Therapeutic AgentsPatricia Noker; Fiscal Year: 2009
- Preclinical Pharmacological Studies of Antitumor and Other Therapeutic AgentsMatthew Ames; Fiscal Year: 2009
- Preclinical Pharmacological Studies of Antitumor &Other Therapeutic AgentsEISEMAN JULIE; Fiscal Year: 2011
- Preclinical Pharmacological Studies of Antitumor and Other Therapeutic AgentsRuiwen Zhang; Fiscal Year: 2009
- PRECLINICAL PHARMACOLOGICAL STUDIESKenneth Chan; Fiscal Year: 2009
- Preclinical Pharmacological Studies of Antitumor and Other Therapeutic AgentsRuiwen Zhang; Fiscal Year: 2010
- Medications for the Treatment of Alcohol Abuse and Dependence and RelapseLAWRENCE SNELL; Fiscal Year: 2009..DCUKA in blood and tissues;(3) ascertain in vivo oral pharmacokinetics and in vitro metabolism of DCUKA in liver microsomes;and (4) toxicology and safety studies in rats (acute and multiple dose tolerance, genetic toxicity, chronic ..
- Antileishmanial Lead Optimization of QuinazolinesKarl A Werbovetz; Fiscal Year: 2013..and metabolic stability testing for active 2,4-diaminoquinazolines will be performed using mouse and human liver microsomes to inform our synthesis efforts in Aim 1 to enhance oral bioavailability and systemic exposure...
- HYPOGLYCEMIC ACTION OF 2-CHLOROPROPIONATERobert Harris; Fiscal Year: 1980..Studies will be conducted with hepatocytes, perfused rat heart, kidney tubules, adipocytes, microsomes, and a partially purified enzyme system...
- Advancing lead dipiperidine compound into preclinical developmentMarina Protopopova; Fiscal Year: 2009..We will investigate the pharmacological properties of SQ609: stability evaluation in plasma and liver microsomes and plasma protein binding of SQ609;determination of pharmacokinetic parameters of SQ609 and bioavailability in ..
- Role of cholesteryl ester transfer protein in cellular lipid homeostasisRichard E Morton; Fiscal Year: 2013..cells CETP assists in both lipid droplet formation and the reverse transport of stored lipids to microsomes for lipoprotein assembly...
- Nomethiazoles Harnessing GABA and NO mimetic activity for Alzheimer's therapyGregory R J Thatcher; Fiscal Year: 2013..Stability in human/rodent plasma and liver microsomes will be investigated and PK profiles generated for nomethiazole and MZ metabolite in brain and plasma after i.p...
- MATURATION OF LIVER FOR THE METABOLISM OF BILIRUBINGlenn Gourley; Fiscal Year: 1993..The "activator" peptide of the B-UPDGt will be isolated from the solubilized liver microsomes from the KCI gradient elutions of the initial anion-exchange chromatography of the B-UPDGt...
- BIOCHEMICAL PROBES OF THE ACTIVE SITE OF AROMATASEROBERT BRUEGGEMEIER; Fiscal Year: 1993..Isolation and purification of cytochrome P450arom from human placental microsomes is accomplished employing sodium cholate solubilization, ammonium sulfate fractionation, and gel chromatography...
- CYTOCHROME P450 DEPENDENT METABOLISM OF DRUGS IN BRAINHENRY STROBEL; Fiscal Year: 2000..abstract): A role for brain cytochromes P450 in metabolism of therapeutic drugs has been suspected since brain microsomes were first shown to be able to activate carcinogens and neurotoxic agents...
- MECHANISM AND ROLE OF MICROSOMAL ETHANOL OXIDATIONCharles Lieber; Fiscal Year: 2001..In vivo, we will determine how changes in dietary lipids alter the activity of enzymes (including 2E1) in liver microsomes and how the latter correlates with changes in phospholipid composition...
- MECHANISMS OF TUMOR INITIATION BY BP AND DERIVATIVESErcole Cavalieri; Fiscal Year: 1993..are involved in the formation of 3- and 9-hydroxyBP, we will study the metabolism of 3- and 9-FBP with rat liver microsomes and analyze the formation of the respective hydroxy derivatives by high pressure liquid chromatography...
- REDUCED DRUG INTERACTIONS OF AZOLE ANTIFUNGAL DRUGSJoseph Gal; Fiscal Year: 2003..b>Microsomes from lymphoblasts expressing recombinant human CYP3A4 will be used to define the Ki and IC50 of the various ..
- REGULATION OF GLCNAC-PI DEACETYLATIONVictoria Stevens; Fiscal Year: 1999..b>Microsomes from the GlcNAc-Pl deacetylase mutant will also be mixed with microsomes from a mutant cell line defective in ..
- BIOCHEMICAL TOXICOLOGY OF CYTOCHROME P-450Andrew Parkinson; Fiscal Year: 1990..P-450e (or enzymes immunochemically related to these five rat liver microsomal isozymes) in extrahepatic microsomes from rats and in liver microsomes from other laboratory animals by immunochemical analysis and by analysis of ..
- BIOCHEMICAL TOXICOLOGY OF CARBOXYESTERASESAndrew Parkinson; Fiscal Year: 1992..studies is to determine the molecular basis for the existence of multiple forms of carboxyesterases in rat liver microsomes, and to determine the function and regulation of these hydrolytic enzymes...
- ROLE OF METABOLISM IN THE BILIARY EXCRETION OF DRUGWALTER LEVINE; Fiscal Year: 1990..Rat liver microsomes metabolize butter yellow (dimethylaminoazobenzene, DAB) by oxidative and reductive pathways...
- SHORT-CHAIN ACYLCARNITINES--FUNCTION AND ENZYMOLOGYLORAN BIEBER; Fiscal Year: 1993..Rev, BCH 57, 261 (1988(]; however, the roles for CAT and COT of liver microsomes are unknown due, in part, to the limited studies with these two enzymes...
- NOVEL DRUGS TO TREAT URINARY INCONTINENCEJAN CHEN; Fiscal Year: 2009..To perform metabolism studies of TBDT in vitro, using human microsomes and hepatocytes, and in vivo, in relevant animal species to be used for toxicology;4...
- Human Brain CYP P450s and Psychoactive Drug MetabolismHENRY STROBEL; Fiscal Year: 2007..Moreover, using human and rat brain microsomes, the P450-dependent metabolism of drugs and stercids has been demonstrated showing that brain cytochromes P450 ..
- Renal tubular 20-HETE and EETs on sodium retention in Mong Heng Wang; Fiscal Year: 2009..and the enzymes CYP4A1, CYP4A8, and 2C23, which catalyze this production, are significantly decreased in renal microsomes after rats have been fed the HF diet for 10 weeks...