Use of thiocarbamides as selective substrate probes for isoforms of flavin-containing monooxygenases.


:The oxidation of thiourea, phenylthiourea, 1,3-diphenylthiourea, 1,3-bis-(3,4-dichlorophenyl)-2-thiourea and 1,1-dibenzyl-3-phenyl-2-thiourea was measured in reactions catalyzed by purified pig liver flavin-containing monooxygenase (FMO-1) and by microsomal fractions isolated from pig, guinea pig, chicken, rat and rabbit tissues. The reactions, followed by measuring substrate-dependent thiocholine oxidation [Guo and Ziegler, Anal Biochem 198: 143-148, 1991], were carried out in the presence of 2 mM 1-benzylimidazole to minimize potential interference from reactions other than those catalyzed by isoforms of the flavin-containing monooxygenase (FMO). While at saturating substrate concentrations the Vmax for purified FMO-1 catalyzed oxidation of all five thiocarbamides was essentially constant, velocities for the microsomal catalyzed reactions varied not only with tissue and species but also with the van der Waals' surface area of the thiocarbamide. Rat liver, rat kidney and rabbit liver microsomes failed to catalyze detectable oxidation of thiocarbamides larger than 1,3-diphenylthiourea and lung microsomes from a female rabbit only accepted substrates smaller than 1,3-diphenylthiourea. On the other hand, liver microsomes from chickens, pigs and guinea pigs catalyzed the oxidation of larger thiocarbamides, but the rates decreased with increasing substrate size and chicken liver microsomes showed no detectable activity with the largest thiocarbamide tested. To define more precisely the parameters affecting thiocarbamide substrate specificity of microsomal preparations, activities present in detergent extracts of guinea pig liver microsomes were separated into three distinct fractions. The substrate specificities of these partially purified fractions were different and consistent with the difference observed with microsomal catalyzed reactions. This strongly suggests that thiocarbamides that differ in size may be useful probes for measuring the number of activities of FMO isoforms in crude tissue preparations.


Biochem Pharmacol


Biochemical pharmacology


Guo WX,Poulsen LL,Ziegler DM




Has Abstract


1992-11-17 00:00:00














  • Regulation of cyclic AMP metabolism in bovine adrenal medullary cells.

    abstract::The capacity of cultured bovine adrenal medullary cells to metabolize and export cyclic AMP has been studied. Basal cellular cyclic AMP levels were increased 50% by 100 microM 3-isobutyl-1-methylxanthine (IBMX) and rolipram, a class IV (cyclic AMP-specific) phosphodiesterase (PDE) inhibitor. They were not affected by ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Marley PD,Thomson KA

    更新日期:1992-12-01 00:00:00

  • Interactions of 5-hydroxytryptamine with oxidative enzymes.

    abstract::Peroxidase (EC, ceruloplasmin (human type X)/O2, and tyrosinase (EC all oxidized the indolic neurotransmitter 5-hydroxytryptamine (5-HT) in the physiological pH domain. Peroxidase/H2O2 oxidized 5-HT at pH values down to about 2.5. All oxidation reactions generated complex mixtures of produ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Wrona MZ,Dryhurst G

    更新日期:1991-04-15 00:00:00

  • TGF-beta in cancer and as a therapeutic target.

    abstract::Cancer develops through a series of genetic changes leading to malignant transformation. Numerous gene and pathways involved in stages of progression to frank malignancy have been elucidated. These genetic changes result in aberrations in fundamental cellular processes controlling proliferation, apoptosis, differentia...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Pinkas J,Teicher BA

    更新日期:2006-08-28 00:00:00

  • Tricyclic antidepressant-induced lipidosis in human peripheral monocytes in vitro, as well as in a monocyte-derived cell line, as monitored by spectrofluorimetry and flow cytometry after staining with Nile red.

    abstract::Human mono- and lymphocytes from peripheral blood and the monoblastoid cell line U-937 were used in this in vitro study of drug-induced lipidosis. Mono- and lymphocytes were exposed for 4 days to three different tricyclic antidepressants (TCAs), imipramine (25 microM), clomipramine (10 microM) and citalopram (80 micro...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Xia Z,Appelkvist EL,DePierre JW,Nässberger L

    更新日期:1997-05-15 00:00:00

  • Iron interactions and other biological reactions mediating the physiological and toxic actions of manganese.

    abstract::Chronic exposure to the divalent heavy metals, such as iron, lead, manganese (Mn), and chromium, has been linked to the development of severe, often irreversible neurological disorders and increased vulnerability to developing Parkinson's disease. Although the mechanisms by which these metals elicit or facilitate neur...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审


    authors: Roth JA,Garrick MD

    更新日期:2003-07-01 00:00:00

  • A new nomenclature for the aldo-keto reductase superfamily.

    abstract::The aldo-keto reductases (AKRs) represent a growing oxidoreductase superfamily. Forty proteins have been identified and characterized as AKRs, and an additional fourteen genes may encode proteins related to the superfamily. Found in eukaryotes and prokaryotes, the AKRs metabolize a wide range of substrates, including ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Jez JM,Flynn TG,Penning TM

    更新日期:1997-09-15 00:00:00

  • gamma-Aminobutyric acid uptake and localization in bovine chromaffin cells in primary culture.

    abstract::gamma-Aminobutyric acid (GABA) uptake was studied in bovine chromaffin cells maintained in primary culture. Uptake was found to be dependent on Na+, but not on K+ and Ca2+ ions; it was found that 2 Na+ ions were necessary for each molecule of GABA transported. 2,4-Dinitrophenol, ouabain and vanadate inhibited GABA upt...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Oset-Gasque MJ,Aunis D

    更新日期:1989-07-15 00:00:00

  • Homo- and hetero-dimerization of human UDP-glucuronosyltransferase 2B7 (UGT2B7) wild type and its allelic variants affect zidovudine glucuronidation activity.

    abstract::Most human UDP-glucuronosyltransferase (UGT; EC genes contain non-synonymous single nucleotide polymorphisms (nsSNPs) which cause amino acid substitutions. Allelic variants caused by nsSNPs may exhibit absent or reduced enzyme activity. UGT2B7 is one of the most important UGTs that glucuronidates abundant en...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Yuan L,Qian S,Xiao Y,Sun H,Zeng S

    更新日期:2015-05-01 00:00:00

  • Effect of vascular endothelial growth factor and epidermal growth factor on iatrogenic apoptosis in human endothelial cells.

    abstract::To study the effect of growth factors on iatrogenic apoptosis, we examined the influence of vascular endothelial growth factor (VEGF) and epidermal growth factor (EGF) on staurosporine-induced apoptosis in primary cultures of human umbilical vein endothelial cells (HUVEC). Apoptosis was evaluated by a cell viability t...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Vinci MC,Visentin B,Cusinato F,Nardelli GB,Trevisi L,Luciani S

    更新日期:2004-01-15 00:00:00

  • Quilamine HQ1-44, an iron chelator vectorized toward tumor cells by the polyamine transport system, inhibits HCT116 tumor growth without adverse effect.

    abstract::Tumor cell growth requires large iron quantities and the deprivation of this metal induced by synthetic metal chelators is therefore an attractive method for limiting the cancer cell proliferation. The antiproliferative effect of the Quilamine HQ1-44, a new iron chelator vectorized toward tumor cells by a polyamine ch...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Renaud S,Corcé V,Cannie I,Ropert M,Lepage S,Loréal O,Deniaud D,Gaboriau F

    更新日期:2015-08-01 00:00:00

  • Properties of the mineralocorticoid receptor immunopurified from bovine kidney.

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    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Pagano M,Mirshahi M,Mirshahi F,Monnot M,Lazar G,Chassaing CG,Fermandjian S,Agarwal MK

    更新日期:1994-09-15 00:00:00

  • Differential inhibitory effects of auranofin on leukotriene B4 and leukotriene C4 formation by human polymorphonuclear leukocytes.

    abstract::Auranofin (AF) is a newly introduced oral gold compound having antirheumatic properties, and its efficacy in the treatment of bronchial asthma is now under investigation. In this study, we examined the effects of AF on leukotriene (LT) formation by human polymorphonuclear leukocytes (PMNs) stimulated with the calcium ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Honda Z,Iizasa T,Morita Y,Matsuta K,Nishida Y,Miyamoto T

    更新日期:1987-05-01 00:00:00

  • Effect of n-butyrate on the synthesis of sulfated glycosaminoglycans and hyaluronate by rat liver fat-storing cells (Ito cells).

    abstract::The effect of naturally occurring aliphatic carboxylic acid n-butyrate on total and type-specific synthesis of sulfated proteoglycans and hyaluronic acid by rat liver fat-storing cells (Ito cells, vitamin A-storing cells), the main connective tissue producing cell type in liver, was studied. Concentrations of n-butyra...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Gressner AM,Haarmann R

    更新日期:1988-10-01 00:00:00

  • Pyroptotic and apoptotic cell death in iNOS and nNOS overexpressing K562 cells: A mechanistic insight.

    abstract::Previous studies from this lab and others have demonstrated that nitric oxide (NO) in a concentration dependent manner, modulated neutrophil and leukemic cell survival. Subsequent studies delineated importance of iNOS in neutrophil differentiation and leukemic cell death. On the contrary, role of nNOS in survival of t...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Sadaf S,Awasthi D,Singh AK,Nagarkoti S,Kumar S,Barthwal MK,Dikshit M

    更新日期:2020-06-01 00:00:00

  • Decrease in arachidonoyl-containing phosphatidylinositols in pancreas of rats fed an ethanol-containing diet.

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    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Cronholm T,Curstedt T

    更新日期:1984-04-01 00:00:00

  • Differences between induction effects of 1,4-bis[2-(3,5-dichloropyridyloxy)]benzene and phenobarbitone.

    abstract::The inductive effects of phenobarbitone (PB) and 1,4-bis[2-(3,5-dichloropyridyloxy)]benzene (TCPOBOP) were compared in C57BL/6J mice. Induction parameters included six substrates: ethylmorphine (EM), benzphetamine (Bph), biphenyl, ethoxycoumarin (EtoC), pentoxyresorufin and dichloro-p-nitroanisole (DPNA). In order to ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Heubel F,Reuter T,Gerstner E

    更新日期:1989-04-15 00:00:00

  • Evidence for the involvement of a carboxyl group in the vicinity of the MK801 and magnesium ion binding site of the N-methyl-D-aspartate receptor.

    abstract::A series of protein modifying reagents were tested for their effects on the specific binding of [3H]MK801 to adult rat brain membranes. N-Bromosuccinimide, acetyl imidazole, 2,3-butanedione, 5,5'-dithiobis-(2-nitrobenzoic acid) and dithiothreitol all had no significant effect on binding. The carboxylic acid residue mo...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Chazot PL,Fotherby A,Stephenson FA

    更新日期:1993-02-09 00:00:00

  • Potential of phytochemicals as immune-regulatory compounds in atopic diseases: A review.

    abstract::Atopic diseases (atopic dermatitis, asthma and allergic rhinitis) affects a huge number of people around the world and their incidence rate is on rise. Atopic dermatitis (AD) is more prevalent in paediatric population which sensitizes an individual to develop allergic rhinitis and asthma later in life. The complex pat...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审


    authors: Sharma S,Naura AS

    更新日期:2020-03-01 00:00:00

  • Poly(ADP-ribose) polymerase regulates myocardial calcium handling in doxorubicin-induced heart failure.

    abstract::Reactive oxygen and nitrogen species are overproduced in the cardiovascular system in response to the exposure to doxorubicin, a cardiotoxic anticancer compound. Oxidant-induced cell injury involves the activation of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) and pharmacological inhibition of PARP has recen...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Szenczi O,Kemecsei P,Holthuijsen MF,van Riel NA,van der Vusse GJ,Pacher P,Szabó C,Kollai M,Ligeti L,Ivanics T

    更新日期:2005-03-01 00:00:00

  • Characterization of histamine H-1 receptors on human peripheral lung.

    abstract::Histamine H-1 receptors in human peripheral lung were characterized by radioligand and biochemical assays employing binding of the H-1 receptor antagonist [3H]pyrilamine to plasma membrane preparations. Simultaneous computerized analyses of the data from fourteen separate equilibrium-binding assays indicated the prese...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Casale TB,Rodbard D,Kaliner M

    更新日期:1985-09-15 00:00:00

  • Cellular uptake, cytotoxicity, and transport kinetics of anthracyclines in human sensitive and multidrug-resistant K562 cells.

    abstract::Multidrug resistance in tumor cells is often associated with the presence of an approximately 170 kDa plasma membrane glycoprotein (Pgp) that acts as a drug-efflux pump and decreases intracellular antitumor drug concentration. We measured the uptake of seven anthracyclines (daunorubicin, doxorubicin, 4'-epi-doxorubici...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Praet M,Stryckmans P,Ruysschaert JM

    更新日期:1996-05-17 00:00:00

  • Tumor anti-angiogenic effect and mechanism of action of delta-tocotrienol.

    abstract::Anti-angiogenic therapy mediated by drugs and food components is an established strategy for cancer prevention. Our previous cell-culture studies identified a food-derived anti-angiogenic compound, tocotrienol (T3, an unsaturated vitamin E), as a potential angiogenic inhibitor. Among T3 isomers, delta-T3 is considered...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Shibata A,Nakagawa K,Sookwong P,Tsuzuki T,Oikawa S,Miyazawa T

    更新日期:2008-08-01 00:00:00

  • P2X7 receptor and the NLRP3 inflammasome: Partners in crime.

    abstract::Adenosine triphosphate (ATP) is a molecule that on one hand plays a central role in cellular energetics and which on the other is a ubiquitous signaling molecule when released into the extracellular media. Extracellular ATP accumulates in inflammatory environments where it acts as a damage-associated molecular pattern...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审


    authors: Pelegrin P

    更新日期:2020-12-20 00:00:00

  • Evidence for the involvement of Ca2+-calmodulin and cyclic AMP in the regulation of the tyrosine hydroxylase system in rat striatal tissue slices.

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    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Hirata Y,Nagatsu T

    更新日期:1985-08-01 00:00:00

  • Human CYP2E1 is regulated by miR-378.

    abstract::Human CYP2E1 is one of the pharmacologically and toxicologically important cytochrome P450 isoforms. Earlier studies have reported that the CYP2E1 expression is extensively regulated by post-transcriptional and post-translational mechanisms, but the molecular basis remains unclear. In the present study, we examined th...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Mohri T,Nakajima M,Fukami T,Takamiya M,Aoki Y,Yokoi T

    更新日期:2010-04-01 00:00:00

  • Microglia-neuron interactions in the models of neuropathic pain.

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    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审


    authors: Tozaki-Saitoh H,Tsuda M

    更新日期:2019-11-01 00:00:00

  • Cytoprotection against neutrophil-delivered oxidant attack by antibiotics.

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    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Ottonello L,Dallegri F,Dapino P,Pastorino G,Sacchetti C

    更新日期:1991-11-27 00:00:00

  • Effects of vitamin E deficiency and glutathione depletion on stress protein heme oxygenase 1 mRNA expression in rat liver and kidney.

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    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Ito K,Yano T,Hagiwara K,Ozasa H,Horikawa S

    更新日期:1997-11-15 00:00:00

  • Statins inhibit aminoglycoside accumulation and cytotoxicity to renal proximal tubule cells.

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    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Antoine DJ,Srivastava A,Pirmohamed M,Park BK

    更新日期:2010-02-15 00:00:00

  • Mono- and Diglucuronide formation from benzo[a]pyrene and chrysene diphenols by AHH-1 cell-expressed UDP-glucuronosyltransferase UGT1A7.

    abstract::Polycyclic aromatic hydrocarbon (PAH)-type compounds induce at least two rat UDP-glucuronosyltransferase isoforms, UGT1A6 and UGT1A7. Among the glucuronidation reactions of PAH metabolites studied, mono- and diglucuronide formation of benzo[a]pyrene and chrysene-3,6-diphenol showed the highest induction factors in rat...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Bock KW,Raschko FT,Gschaidmeier H,Seidel A,Oesch F,Grove AD,Ritter JK

    更新日期:1999-03-15 00:00:00