liver microsomes

Summary

Summary: Closed vesicles of fragmented endoplasmic reticulum created when liver cells or tissue are disrupted by homogenization. They may be smooth or rough.

Top Publications

  1. Zhao Q, Hua W, Zhang L, Guo T, Zhao M, Yan M, et al. Antitumor activity of two gelsemine metabolites in rat liver microsomes. J Asian Nat Prod Res. 2010;12:731-9 pubmed publisher
    ..In this paper, metabolism of gelsemine has been investigated in vitro in phenobarbital-treated rat liver microsomes. The metabolites of gelsemine were separated and evaluated using the flash silica gel column, preparative ..
  2. Duhamel M, Troncy E, Beaudry F. Metabolic stability and determination of cytochrome P450 isoenzymes' contribution to the metabolism of medetomidine in dog liver microsomes. Biomed Chromatogr. 2010;24:868-77 pubmed publisher
    ..study was to establish the metabolic stability and determine the metabolic pathway of medetomidine in dog liver microsomes. Consequently, Michaelis-Menten parameters (V(max), K(m)), T(1/2) and CL(i) were determined...
  3. Bourcier K, Hyland R, Kempshall S, Jones R, Maximilien J, Irvine N, et al. Investigation into UDP-glucuronosyltransferase (UGT) enzyme kinetics of imidazole- and triazole-containing antifungal drugs in human liver microsomes and recombinant UGT enzymes. Drug Metab Dispos. 2010;38:923-9 pubmed publisher
    ..In this study, evidence for glucuronidation of azole-containing compounds was studied in human liver microsomes (HLM)...
  4. Benskin J, Holt A, Martin J. Isomer-specific biotransformation rates of a perfluorooctane sulfonate (PFOS)-precursor by cytochrome P450 isozymes and human liver microsomes. Environ Sci Technol. 2009;43:8566-72 pubmed publisher
  5. Simeonova R, Vitcheva V, Kondeva Burdina M, Krasteva I, Nikolov S, Mitcheva M. Effect of purified saponin mixture from Astragalus corniculatus on enzyme- and non-enzyme-induced lipid peroxidation in liver microsomes from spontaneously hypertensive rats and normotensive rats. Phytomedicine. 2010;17:346-9 pubmed publisher
    ..Fabaceae), on enzyme-induced and non-enzyme-induced lipid peroxidation (LPO), in liver microsomes from spontaneously hypertensive rats (SHRs) - strain Okamoto Aoki, as compared to normotensive Wistar rats (..
  6. Gao H, Steyn S, Chang G, Lin J. Assessment of in silico models for fraction of unbound drug in human liver microsomes. Expert Opin Drug Metab Toxicol. 2010;6:533-42 pubmed publisher
    ..In recent years, there have been considerable advances in understanding structure-microsomal binding relationships...
  7. Bae S, Cao S, Seo K, Kim H, Kim M, Shon J, et al. Cytochrome P450 2B6 catalyzes the formation of pharmacologically active sibutramine (N-{1-[1-(4-chlorophenyl)cyclobutyl]-3-methylbutyl}-N,N-dimethylamine) metabolites in human liver microsomes. Drug Metab Dispos. 2008;36:1679-88 pubmed publisher
    ..in humans using a combination chemical inhibition, correlation analyses in human liver microsomes (HLMs), and activity assays using recombinant P450s. Mechanism-based CYP2B6 inhibitors (i.e...
  8. Toda T, Eliasson E, Ask B, Inotsume N, Rane A. Roles of different CYP enzymes in the formation of specific fluvastatin metabolites by human liver microsomes. Basic Clin Pharmacol Toxicol. 2009;105:327-32 pubmed publisher
    ..to 5-hydroxy fluvastatin (M-2), 6-hydroxy fluvastatin (M-3) and N-desisopropyl fluvastatin (M-5) in human liver microsomes by primarily CYP2C9...
  9. Liu Z, Huang L, Dai M, Chen D, Tao Y, Wang Y, et al. Metabolism of cyadox in rat, chicken and pig liver microsomes and identification of metabolites by accurate mass measurements using electrospray ionization hybrid ion trap/time-of-flight mass spectrometry. Rapid Commun Mass Spectrom. 2009;23:2026-34 pubmed publisher
    ..In this study, the metabolic fate of CYX in the liver microsomes of animal was investigated firstly using high-performance liquid chromatography combined with hybrid ion trap/..

Scientific Experts

More Information

Publications62

  1. Bolling B, Court M, Blumberg J, Chen C. The kinetic basis for age-associated changes in quercetin and genistein glucuronidation by rat liver microsomes. J Nutr Biochem. 2010;21:498-503 pubmed publisher
    ..Thus, the capacity for flavonoid glucuronidation by rat liver microsomes is dependent on age, UGT isoenzymes and flavonoid structure.
  2. Zgoda V, Moshkovskii S, Ponomarenko E, Andreewski T, Kopylov A, Tikhonova O, et al. Proteomics of mouse liver microsomes: performance of different protein separation workflows for LC-MS/MS. Proteomics. 2009;9:4102-5 pubmed publisher
    ..The higher number of proteins identified in the workflow corresponded to the lesser percentage of run-to-run reproducibility. Gel-based method yielded a number of predicted membrane proteins similar to LC-based workflows...
  3. Turpeinen M, Hofmann U, Klein K, Mürdter T, Schwab M, Zanger U. A predominate role of CYP1A2 for the metabolism of nabumetone to the active metabolite, 6-methoxy-2-naphthylacetic acid, in human liver microsomes. Drug Metab Dispos. 2009;37:1017-24 pubmed publisher
    ..In human liver microsomes (HLMs) 6-MNA formation displayed monophasic Michaelis-Menten kinetics with apparent K(m) and V(max) values (..
  4. Stringer R, Nicklin P, Houston J. Reliability of human cryopreserved hepatocytes and liver microsomes as in vitro systems to predict metabolic clearance. Xenobiotica. 2008;38:1313-29 pubmed
    ..standard approaches to the prediction of in vivo metabolic clearance using drug-depletion profiles from human liver microsomes (HLMs) and cyropreserved hepatocytes...
  5. Argikar U, Remmel R. Effect of aging on glucuronidation of valproic acid in human liver microsomes and the role of UDP-glucuronosyltransferase UGT1A4, UGT1A8, and UGT1A10. Drug Metab Dispos. 2009;37:229-36 pubmed publisher
    ..The formation rates of VPAG in a bank of elderly (65 years onward) human liver microsomes (HLMs) were measured by liquid chromatography/tandem mass spectrometry and compared with those in a younger (..
  6. Kilford P, Stringer R, Sohal B, Houston J, Galetin A. Prediction of drug clearance by glucuronidation from in vitro data: use of combined cytochrome P450 and UDP-glucuronosyltransferase cofactors in alamethicin-activated human liver microsomes. Drug Metab Dispos. 2009;37:82-9 pubmed publisher
    ..gemfibrozil, ketoprofen, midazolam, naloxone, raloxifene, and zidovudine were determined in pooled human liver microsomes using the substrate depletion approach...
  7. Tang J, Yang H, Song X, Song X, Yan S, Shao J, et al. Inhibition of cytochrome P450 enzymes by rhein in rat liver microsomes. Phytother Res. 2009;23:159-64 pubmed publisher
    ..Therefore, caution should be paid to the possible drug interaction of medicinal plants containing rhein and CYP substrates...
  8. Madsen K, Grönberg G, Skonberg C, Jurva U, Hansen S, Olsen J. Electrochemical oxidation of troglitazone: identification and characterization of the major reactive metabolite in liver microsomes. Chem Res Toxicol. 2008;21:2035-41 pubmed publisher
    ..From incubations of TGZ with rat and human liver microsomes in the presence of either GSH or N-acetylcysteine, it was shown that similar conjugates were formed in vitro ..
  9. Xue X, Xiao Y, Zhu H, Wang H, Liu Y, Xie T, et al. Induction of P450 1A by 3-methylcholanthrene protects mice from aristolochic acid-I-induced acute renal injury. Nephrol Dial Transplant. 2008;23:3074-81 pubmed publisher
    ..This study was designed to investigate whether P450 1A plays a role in AAI-induced renal injury in C57BL/6 mice...
  10. Li W, Liu Y, He Y, Zhang J, Gao Y, Ge G, et al. Characterization of triptolide hydroxylation by cytochrome P450 in human and rat liver microsomes. Xenobiotica. 2008;38:1551-65 pubmed publisher
    ..In the present study, the metabolism of triptolide by cytochrome P450s was investigated in human and rat liver microsomes. Triptolide was converted to four metabolites (M-1, M-2, M-3, and M-4) in rat liver microsomes and three (M-2,..
  11. Zhang L, Wei M, Zhao C, Qi H. Determination of the inhibitory potential of 6 fluoroquinolones on CYP1A2 and CYP2C9 in human liver microsomes. Acta Pharmacol Sin. 2008;29:1507-14 pubmed publisher
  12. Ung D, Nagar S. Trans-resveratrol-mediated inhibition of beta-oestradiol conjugation in MCF-7 cells stably expressing human sulfotransferases SULT1A1 or SULT1E1, and human liver microsomes. Xenobiotica. 2009;39:72-9 pubmed
    ..25-2.25 microM) was characterized in human liver microsomes. The highest resveratrol concentration significantly decreased the intrinsic clearance of E2 glucuronidation...
  13. Shimizu M, Matsumoto Y, Yamazaki H. Effects of propofol analogs on glucuronidation of propofol, an anesthetic drug, by human liver microsomes. Drug Metab Lett. 2007;1:77-9 pubmed
    ..Propofol was predominately glucuronidated by human UGT1A9 and intestinal or liver microsomes. 2,5-Diisopropylphenol inhibited the propofol glucuronidation...
  14. Qiu F, Zhang R, Sun J, Jiye A, Hao H, Peng Y, et al. Inhibitory effects of seven components of danshen extract on catalytic activity of cytochrome P450 enzyme in human liver microsomes. Drug Metab Dispos. 2008;36:1308-14 pubmed publisher
    ..Probe substrates of cytochrome P450 enzymes were incubated in human liver microsomes (HLMs) with or without each component of danshen extract...
  15. Obach R, Kalgutkar A, Soglia J, Zhao S. Can in vitro metabolism-dependent covalent binding data in liver microsomes distinguish hepatotoxic from nonhepatotoxic drugs? An analysis of 18 drugs with consideration of intrinsic clearance and daily dose. Chem Res Toxicol. 2008;21:1814-22 pubmed publisher
    ..and nine nonhepatotoxins in humans) were assessed for in vitro covalent binding in NADPH-supplemented human liver microsomes. Of the two sets of nine drugs, seven in each set were shown to undergo some degree of covalent binding...
  16. Wen B, Chen Y, Fitch W. Metabolic activation of nevirapine in human liver microsomes: dehydrogenation and inactivation of cytochrome P450 3A4. Drug Metab Dispos. 2009;37:1557-62 pubmed publisher
    ..initiated to determine whether nevirapine undergoes cytochrome P450 (P450)-mediated bioactivation in human liver microsomes to electrophilic intermediates...
  17. Kaivosaari S, Toivonen P, Aitio O, Sipilä J, Koskinen M, Salonen J, et al. Regio- and stereospecific N-glucuronidation of medetomidine: the differences between UDP glucuronosyltransferase (UGT) 1A4 and UGT2B10 account for the complex kinetics of human liver microsomes. Drug Metab Dispos. 2008;36:1529-37 pubmed publisher
    ..Studying medetomidine glucuronidation by human liver microsomes (HLMs) and recombinant UDP glucuronosyltransferase (UGT) 1A4 indicated that another human UGT plays a major ..
  18. Wen B, Zhou M. Metabolic activation of the phenothiazine antipsychotics chlorpromazine and thioridazine to electrophilic iminoquinone species in human liver microsomes and recombinant P450s. Chem Biol Interact. 2009;181:220-6 pubmed publisher
    ..whether chlorpromazine and thioridazine undergo cytochrome P450 (P450)-mediated bioactivation in human liver microsomes to electrophilic intermediates...
  19. Kim A, Lim S, Lee B. Metabolic inhibition and kinetics of raloxifene by pharmaceutical excipients in human liver microsomes. Int J Pharm. 2009;368:37-44 pubmed publisher
    ..of pharmaceutical excipients (PEs) on drug metabolism in uridine diphosphoglucuronic acid-supplemented human liver microsomes. Poorly bioavailable raloxifene was chosen as a model drug...
  20. Tojcic J, Benoit Biancamano M, Court M, Straka R, Caron P, Guillemette C. In vitro glucuronidation of fenofibric acid by human UDP-glucuronosyltransferases and liver microsomes. Drug Metab Dispos. 2009;37:2236-43 pubmed publisher
    ..Additional studies are required to identify genetic factors contributing to the observed FA glucuronidation variability...
  21. Mori K, Hashimoto H, Takatsu H, Tsuda Tsukimoto M, Kume T. Cocktail-substrate assay system for mechanism-based inhibition of CYP2C9, CYP2D6, and CYP3A using human liver microsomes at an early stage of drug development. Xenobiotica. 2009;39:415-22 pubmed publisher
    We established a mechanism-based inhibition cocktail-substrate assay system using human liver microsomes and drug-probe substrates that enabled simultaneous estimation of the inactivation of main cytochrome P450 (CYP) enzymes, CYP2C9, ..
  22. Huang M, Ho P. Identification of metabolites of meisoindigo in rat, pig and human liver microsomes by UFLC-MS/MS. Biochem Pharmacol. 2009;77:1418-28 pubmed publisher
    ..of meisoindigo, the relevant metabolism studies were carried out for the first time in rat, pig and human liver microsomes of different genders by ultra fast liquid chromatography/tandem mass spectrometry (UFLC-MS/MS)...
  23. Murayama N, Kaneko N, Horiuchi K, Ohyama K, Shimizu M, Ito K, et al. Cytochrome P450-dependent drug oxidation activity of liver microsomes from Microminipigs, a possible new animal model for humans in non-clinical studies. Drug Metab Pharmacokinet. 2009;24:404-8 pubmed
    ..Cytochrome P450 (P450)-and flavin-containing monooxygenases (FMO)-dependent drug oxidation activity of liver microsomes prepared from male Microminipigs (8 months-old) was compared with that for pooled dogs, monkeys, and humans...
  24. Soulard P, McLaughlin M, Stevens J, Connolly B, Coli R, Wang L, et al. Development of a high-throughput screening assay for stearoyl-CoA desaturase using rat liver microsomes, deuterium labeled stearoyl-CoA and mass spectrometry. Anal Chim Acta. 2008;627:105-11 pubmed publisher
    ..based high-throughput screening (HTS) assay using deuterium labeled stearoyl-CoA substrate and induced rat liver microsomes. The methodology developed allows the use of a nonradioactive substrate which avoids interference by the ..
  25. Asha S, Vidyavathi M. Role of human liver microsomes in in vitro metabolism of drugs-a review. Appl Biochem Biotechnol. 2010;160:1699-722 pubmed publisher
    ..Different approaches are provided and emphasis is placed on the potential of human liver microsomes for drug metabolism and inhibition studies...
  26. Chan E, New L. In vitro metabolism of leflunomide by mouse and human liver microsomes. Drug Metab Lett. 2007;1:299-305 pubmed
    ..M1 and M2 were proposed to be the hydroxylated alpha-cyanoenol form of A77-1726 and the hydroxylated 5 methyl-isoxazole form of leflunomide, respectively...
  27. Liu H, Liu Y, Zhang J, Li W, Liu H, Yang L. UDP-glucuronosyltransferase 1A6 is the major isozyme responsible for protocatechuic aldehyde glucuronidation in human liver microsomes. Drug Metab Dispos. 2008;36:1562-9 pubmed publisher
    ..Here, we characterized PAL glucuronidation by human liver microsomes (HLMs), human intestine microsomes (HIMs), and 12 recombinant UGT (rUGT) isozymes to identify what kinds of ..
  28. Ma S, Subramanian R, Xu Y, Schrag M, Shou M. Structural characterization of novel adenine dinucleotide phosphate conjugates of imatinib in incubations with rat and human liver microsomes. Drug Metab Dispos. 2008;36:2414-8 pubmed publisher
    ..In vitro metabolism of imatinib was investigated in rat and human liver microsomes. Besides several oxidative metabolites and an N-desmethyl metabolite, as previous reported, a novel ..
  29. Gan L, von Moltke L, Trepanier L, Harmatz J, Greenblatt D, Court M. Role of NADPH-cytochrome P450 reductase and cytochrome-b5/NADH-b5 reductase in variability of CYP3A activity in human liver microsomes. Drug Metab Dispos. 2009;37:90-6 pubmed publisher
    ..CPR and b(5) were measured in human liver microsomes (HLMs) by spectrophotometry and immunoblotting...
  30. Sistkova J, Hudecek J, Hodek P, Frei E, Schmeiser H, Stiborova M. Human cytochromes P450 1A1 and 1A2 participate in detoxication of carcinogenic aristolochic acid. Neuro Endocrinol Lett. 2008;29:733-7 pubmed
    ..The aim of the study was to resolve which cytochromes P450 (CYP) detoxicate the major component of AA, aristolochic acid I (AAI), to its O-demethylated metabolite, aristolochic acid Ia (AAIa)...
  31. Garcia C, Rodriguez Navarro A, Diaz J, Torres R, Lagos N. Evidence of in vitro glucuronidation and enzymatic transformation of paralytic shellfish toxins by healthy human liver microsomes fraction. Toxicon. 2009;53:206-13 pubmed publisher
    ..This data is the first evidence of in vitro glucuronidation of PST, given a metabolic pathway of detoxification and excretion of PST in human...
  32. Kneip C, Terlinden R, Beier H, Chen G. Investigations into the drug-drug interaction potential of tapentadol in human liver microsomes and fresh human hepatocytes. Drug Metab Lett. 2008;2:67-75 pubmed
    ..It was concluded that no clinically relevant drug-drug interactions are likely to occur through either mechanism...
  33. Lang D, Freudenberger C, Weinz C. In vitro metabolism of rivaroxaban, an oral, direct factor Xa inhibitor, in liver microsomes and hepatocytes of rats, dogs, and humans. Drug Metab Dispos. 2009;37:1046-55 pubmed publisher
    ..14)C]Rivaroxaban was incubated with liver microsomes and hepatocytes of rats, dogs, and humans...
  34. Payne J, Bonnefous C, Symons K, Nguyen P, Sablad M, Rozenkrants N, et al. Discovery of dual inducible/neuronal nitric oxide synthase (iNOS/nNOS) inhibitor development candidate 4-((2-cyclobutyl-1H-imidazo[4,5-b]pyrazin-1-yl)methyl)-7,8-difluoroquinolin-2(1H)-one (KD7332) part 2: identification of a novel, potent, and selec. J Med Chem. 2010;53:7739-55 pubmed publisher
    ..Further 42 did not affect motor coordination up to doses of 1000 mg/kg, demonstrating a wide therapeutic margin...
  35. Choi Y, Lee U, Lee B, Lee M. Pharmacokinetic interaction between itraconazole and metformin in rats: competitive inhibition of metabolism of each drug by each other via hepatic and intestinal CYP3A1/2. Br J Pharmacol. 2010;161:815-29 pubmed publisher
  36. Cross R, Monastyrskyi A, Mutka T, Burrows J, Kyle D, Manetsch R. Endochin optimization: structure-activity and structure-property relationship studies of 3-substituted 2-methyl-4(1H)-quinolones with antimalarial activity. J Med Chem. 2010;53:7076-94 pubmed publisher
  37. Hodgetts K, Blum C, Caldwell T, Bakthavatchalam R, Zheng X, Capitosti S, et al. Pyrido[2,3-b]pyrazines, discovery of TRPV1 antagonists with reduced potential for the formation of reactive metabolites. Bioorg Med Chem Lett. 2010;20:4359-63 pubmed publisher
    ..In vivo, 26 significantly attenuated carrageenan-induced thermal hyperalgesia (CITH) and dose-dependently reduced complete Freund's adjuvant (CFA)-induced chronic inflammatory pain after oral administration...
  38. Bézière N, Frapart Y, Rockenbauer A, Boucher J, Mansuy D, Peyrot F. Metabolic stability of superoxide and hydroxyl radical adducts of a cyclic nitrone toward rat liver microsomes and cytosol: A stopped-flow ESR spectroscopy study. Free Radic Biol Med. 2010;49:437-46 pubmed publisher
    ..and hydroxyl radicals with 5-tert-butoxycarbonyl-5-methyl-1-pyrroline N-oxide (BocMPO) in the presence of rat liver microsomes (RLM) and rat liver cytosol (RLC) was studied by using a stopped-flow device coupled to an electron spin ..
  39. Cheng H, Hoffman J, Le P, Nair S, Cripps S, Matthews J, et al. The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors. Bioorg Med Chem Lett. 2010;20:2897-902 pubmed publisher
    ..In an in vivo assay, PF-877423 inhibited the conversion of cortisone to cortisol. Structure guided optimization effort yielded potent and stable 11beta-HSD1 selective inhibitor 42...
  40. Czuczwar P, Kaczmarczyk K, Wierzchowska Cioch E, Łuszczki J, Czuczwar S. [Drug resistance in epilepsy]. Przegl Lek. 2009;66:963-6 pubmed
    ..Consequently, there are a great deal of experimental and clinical studies aimed at finding mechanisms responsible for this phenomenon. Characterization of these mechanisms could result in new, more efficient treatment strategies...
  41. Kijima K, Morita J, Suzuki K, Aoki M, Kato K, Hayashi H, et al. [Pharmacokinetics of tebipenem pivoxil, a novel oral carbapenem antibiotic, in experimental animals]. Jpn J Antibiot. 2009;62:214-40 pubmed
    ..4% and 11.4% of radioactivity was excreted in urine and bile, respectively, by 24 hours after administration. The majority of dosage was excreted out of body by 4 hours after administration...
  42. Pérez V, Sánchez Parra C, Serrano Villar S. [Etravirine drug interactions]. Enferm Infecc Microbiol Clin. 2009;27 Suppl 2:27-31 pubmed publisher
    ..Interaction with fosamprenavir/ritonavir is not clinically significant, although their plasma levels vary slightly when used in combination with ETR. ETR shows no interactions with darunavir/ritonavir...
  43. Hedge J, Devito M, Crofton K. In vivo acute exposure to polychlorinated biphenyls: effects on free and total thyroxine in rats. Int J Toxicol. 2009;28:382-91 pubmed publisher
    ..These data demonstrate that neither PCB 153 nor PCB169 increased FT4, which supports the conclusion that these PCBs do not displace thyroxine from serum TTR, or if it does occur, there is no subsequent increase in serum FT4 in vivo...
  44. Toselli F, Matthias A, Bone K, Gillam E, Lehmann R. Metabolism of the major Echinacea alkylamide N-isobutyldodeca-2E,4E,8Z,10Z-tetraenamide by human recombinant cytochrome P450 enzymes and human liver microsomes. Phytother Res. 2010;24:1195-201 pubmed publisher
    ..human cytochrome P450 enzymes involved in the metabolism of this alkylamide using recombinant P450s, human liver microsomes and pure synthetic compound...
  45. Dostalek M, Macwan J, Chitnis S, Ionita I, Akhlaghi F. Development and validation of a rapid and sensitive assay for simultaneous quantification of midazolam, 1'-hydroxymidazolam, and 4-hydroxymidazolam by liquid chromatography coupled to tandem mass-spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2010;878:1629-33 pubmed publisher
    ..This method is suitable for characterizing the P450 3A4/5 activity in vitro or in human pharmacokinetic studies allowing administration of smaller doses of midazolam...
  46. Brand W, Shao J, Hoek van den Hil E, van Elk K, Spenkelink B, De Haan L, et al. Stereoselective conjugation, transport and bioactivity of s- and R-hesperetin enantiomers in vitro. J Agric Food Chem. 2010;58:6119-25 pubmed publisher
    ..This is an important finding since at present hesperetin is only commercially available as a racemic mixture, while it exists in nature mainly as an S-enantiomer...
  47. Wang Y, Arsenault G, Riddell N, McCrindle R, McAlees A, Martin J. Perfluorooctane sulfonate (PFOS) precursors can be metabolized enantioselectively: principle for a new PFOS source tracking tool. Environ Sci Technol. 2009;43:8283-9 pubmed publisher
    ..center was developed and applied to evaluate the enantioselectivity of 1m-PreFOS biotransformation in human liver microsomes. Gradient elution in reversed-phase mode on a Chiralpak IC column permitted the near-baseline separation of ..
  48. Hum M, McLaughlin B, Roman G, Vlahakis J, Szarek W, Nakatsu K. The effects of azole-based heme oxygenase inhibitors on rat cytochromes P450 2E1 and 3A1/2 and human cytochromes P450 3A4 and 2D6. J Pharmacol Exp Ther. 2010;334:981-7 pubmed publisher
    ..Four structural regions of QC-xx were analyzed, leading to the identification of structures that confer a decreased effect on both rat and human P450 isoforms studied while maintaining an inhibitory effect on the HOs...
  49. Miksits M, Maier Salamon A, Vo T, Sulyok M, Schuhmacher R, Szekeres T, et al. Glucuronidation of piceatannol by human liver microsomes: major role of UGT1A1, UGT1A8 and UGT1A10. J Pharm Pharmacol. 2010;62:47-54 pubmed publisher
    ..Piceatannol, a dietary polyphenol present in grapes and wine, is known for its promising anticancer and anti-inflammatory activity. The aim of this study was to analyse the concentration-dependent glucuronidation of piceatannol in vitro...
  50. Li F, Wang L, Guo G, Ma X. Metabolism-mediated drug interactions associated with ritonavir-boosted tipranavir in mice. Drug Metab Dispos. 2010;38:871-8 pubmed publisher
    ..In vitro study using human liver microsomes recapitulated five TPV metabolites, all of which were suppressed by RTV...
  51. Lundquist J, Harnish D, Kim C, Mehlmann J, Unwalla R, Phipps K, et al. Improvement of physiochemical properties of the tetrahydroazepinoindole series of farnesoid X receptor (FXR) agonists: beneficial modulation of lipids in primates. J Med Chem. 2010;53:1774-87 pubmed publisher
    ..These data are the first to demonstrate the dramatic lowering of serum LDLc levels by a FXR agonist in primates and supports the potential utility of 14cc in treating dyslipidemia in humans beyond just TG lowering...
  52. Subramanian R, Lee M, Allen J, Bourbeau M, Fotsch C, Hong F, et al. Cytochrome P450-mediated epoxidation of 2-aminothiazole-based AKT inhibitors: identification of novel GSH adducts and reduction of metabolic activation through structural changes guided by in silico and in vitro screening. Chem Res Toxicol. 2010;23:653-63 pubmed publisher
    ..When incubated in rat and human liver microsomes in the presence of NADPH, 1 underwent significant metabolic activation on its 2-aminothiazole ring, leading ..
  53. Romão S, Cadena S, Amorim J, Méndez Sánchez S, Echevarria A, Silva E, et al. Metabolism of the mesoionic compound (MI-D) by mouse liver microsome, detection of its metabolite in vivo, and acute toxicity in mice. J Biochem Mol Toxicol. 2009;23:394-405 pubmed publisher
    ..Abdominal adhesions, inflammatory foci, and formation of granulomas were observed. Altogether, the results contribute to the advancement of research in support of MI-D as a future chemotherapeutic drug...