5-Substituted-2,2'-anhydrouridines, potent inhibitors of uridine phosphorylase.


:5-Substituted-2,2'-anhydrouridines are a new class of competitive inhibitors of uridine phosphorylase. The most potent member of the series is 2,2'-anhydro-5-ethyluridine with an apparent Ki value of 25 nM. These compounds are selective inhibitors of uridine phosphorylase and have no effect on thymidine phosphorylase. 5-Substituted-2,2'-anhydrouridines are no substrates of either uridine phosphorylase or thymidine phosphorylase.


Biochem Pharmacol


Biochemical pharmacology


Veres Z,Szabolcs A,Szinai I,Dénes G,Kajtár-Peredy M,Otvös L




Has Abstract


1985-05-15 00:00:00














  • Novel orally available salvinorin A analog PR-38 protects against experimental colitis and reduces abdominal pain in mice by interaction with opioid and cannabinoid receptors.

    abstract:BACKGROUND:Salvinorin A (SA) is a potent anti-inflammatory diterpene isolated from the Mexican plant S. divinorum. Recently we showed that the novel SA analog, PR-38 has an inhibitory effect on mouse gastrointestinal (GI) motility mediated by opioid and cannabinoid (CB) receptors. The aim of the study was to characteri...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Sałaga M,Polepally PR,Zakrzewski PK,Cygankiewicz A,Sobczak M,Kordek R,Zjawiony JK,Krajewska WM,Fichna J

    更新日期:2014-12-15 00:00:00

  • Expression and activity of the DNA repair enzyme uracil DNA glycosylase during organogenesis in the rat conceptus and following methotrexate exposure in vitro.

    abstract::Uracil incorporation into DNA occurs under conditions that limit thymidine biosynthesis; uracil is removed by two isoforms of uracil DNA glycosylase (UNG; EC, UNG1 and UNG2. We hypothesize that UNG is important in protecting the mid-organogenesis stage [gestational day (GD) 10-12] rat conceptus against condit...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Vinson RK,Hales BF

    更新日期:2002-08-15 00:00:00

  • Involvement of nitric oxide/cyclic GMP signaling pathway in the regulation of fatty acid metabolism in rat hepatocytes.

    abstract::The role of nitric oxide (NO)/guanosine 3',5'-cyclic monophosphate (cGMP) signaling pathway in the regulation of fatty acid metabolism was investigated in rat hepatocytes. Treatment with NO donors, which are known to activate soluble guanylyl cyclase, inhibited in parallel fatty acid synthesis de novo and acetyl-CoA c...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: García-Villafranca J,Guillén A,Castro J

    更新日期:2003-03-01 00:00:00

  • Receptor-mediated mitogenic effect of thromboxane A2 in vascular smooth muscle cells.

    abstract::The effects of thromboxane A2 (TXA2) on the proliferation of vascular smooth muscles cells (VSMC) were examined using primary cultures of VSMC from rat aorta. U46619, a stable TXA2 mimetic, stimulated DNA synthesis of VSMC only in the presence of insulin. The effect was concentration-dependent with a half-maximal effe...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Hanasaki K,Nakano T,Arita H

    更新日期:1990-12-01 00:00:00

  • Reduction and transport of lipoic acid by human erythrocytes.

    abstract::Reduction of exogenous lipoic acid to dihydrolipoate is known to occur in several mammalian cells and tissues. Dihydrolipoate is a potent radical scavenger, and may provide significant antioxidant protection. Because lipoic acid appears in the bloodstream after oral administration, we have examined the reduction of ex...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Constantinescu A,Pick U,Handelman GJ,Haramaki N,Han D,Podda M,Tritschler HJ,Packer L

    更新日期:1995-07-17 00:00:00

  • Differential effects of sedative and anticonvulsant barbiturates on specific [3H]GABA binding to membrane preparations from rat brain cortex.

    abstract::The sensitivity to barbiturates of [3H]GABA binding to synaptosomal membrane fractions from rat cortex has been examined. We show that a range of anaesthetic/sedative barbiturates enhance GABA binding in the presence of chloride or other ions that interact with the associated ionophore. Furthermore, picrotoxinin and t...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Whittle SR,Turner AJ

    更新日期:1982-09-15 00:00:00

  • UNBS1450, a steroid cardiac glycoside inducing apoptotic cell death in human leukemia cells.

    abstract::Cardiac steroids are used to treat various diseases including congestive heart failure and cancer. The aim of this study was to investigate the anti-leukemic activity of UNBS1450, a hemi-synthetic cardenolide belonging to the cardiac steroid glycoside family. Here, we report that, at low nanomolar concentrations, UNBS...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Juncker T,Cerella C,Teiten MH,Morceau F,Schumacher M,Ghelfi J,Gaascht F,Schnekenburger M,Henry E,Dicato M,Diederich M

    更新日期:2011-01-01 00:00:00

  • Interspecies homology of liver microsomal cytochrome P-450. A form of dog cytochrome P-450 (P-450-D1) crossreactive with antibodies to rat P-450-male.

    abstract::P-450-male is a male specific form of cytochrome P-450 in rat liver microsomes. Cytochrome P-450 crossreactive with anti-P-450-male antibodies was purified to an electrophoretical homogeneity from liver microsomes of male beagle dogs. The specific content of the purified cytochrome P-450 (P-450-D1) was 16.9 nmol/mg pr...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Komori M,Shimada H,Miura T,Kamataki T

    更新日期:1989-01-15 00:00:00

  • Molecular and functional characterization of flavin-containing monooxygenases in cynomolgus macaque.

    abstract::Flavin-containing monooxygenases (FMOs), drug-metabolizing enzymes essential for the metabolism of endogenous biochemicals and foreign compounds, have been characterized in human (including FMO1-5 and FMO6P), but remain to be investigated in cynomolgus macaque. In this study, cDNAs of cynomolgus FMO1-5 and FMO6 were i...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Uno Y,Shimizu M,Yamazaki H

    更新日期:2013-06-15 00:00:00

  • Ferulic acid suppresses activation of hepatic stellate cells through ERK1/2 and Smad signaling pathways in vitro.

    abstract::Hepatic stellate cells (HSCs) are the primary source of matrix components in hepatic fibrosis. Ferulic acid (FA) has antifibrotic potential in renal and cardiac disease. However, whether FA comprises inhibitive effects of HSCs activation remains to be clarified. This study aims at evaluating the hypothesis that FA inh...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Xu T,Pan Z,Dong M,Yu C,Niu Y

    更新日期:2015-01-01 00:00:00

  • Effect of okadaic acid on immunologic and non-immunologic histamine release in rat mast cells.

    abstract::We have studied the effect of the protein phosphatase (PP) inhibitor, okadaic acid (OKA) on histamine release elicited by immunologic and non-immunologic stimuli in peritoneal and pleural rat mast cells. When cells were stimulated with antigen (egg albumin), OKA strongly inhibited histamine release. This finding sugge...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Estévez MD,Vieytes MR,Louzao MC,Botana LM

    更新日期:1994-02-09 00:00:00

  • Modulatory effect of 4 beta-phorbol 12-myristate 13-acetate (PMA) on carbachol-induced Ca2+ mobilization in rat parotid acinar cells.

    abstract::Treatment of rat parotid acinar cells with 4 beta-phorbol 12-myristate 13-acetate (PMA) significantly inhibited an increase in cytosolic free Ca2+ concentration ([Ca2+]i) induced by carbachol (CCh), a muscarinic agonist. The CCh-induced increase in [Ca2+]i was also inhibited by another active phorbol ester, 4 beta-pho...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Tojyo Y,Tanimura A,Matsumoto Y

    更新日期:1994-06-01 00:00:00

  • Stereoselective and substrate-dependent inhibition of hepatic mitochondria beta-oxidation and oxidative phosphorylation by the non-steroidal anti-inflammatory drugs ibuprofen, flurbiprofen, and ketorolac.

    abstract::Non-steroidal anti-inflammatory drugs (NSAIDs) cause a range of adverse effects, some of which have been associated with perturbances of lipid metabolic pathways. Previous data demonstrating stereoselective formation of the CoA thioester of R-ibuprofen in particular were suggestive of possible stereoselective effects ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Browne GS,Nelson C,Nguyen T,Ellis BA,Day RO,Williams KM

    更新日期:1999-04-01 00:00:00

  • Mechanistic studies on metabolic chiral inversion of 4-(4-methylphenyl)-2-methylthiomethyl-4-oxobutanoic acid (KE-748), an active metabolite of the new anti-rheumatic agent 2-acetylthiomethyl-4-(4-methylphenyl)-4-oxobutanoic acid (KE-298), in rats.

    abstract::The chiral inversion properties of 4-(4-methylphenyl)-2-methylthiomethyl-4-oxobutanoic acid (KE-748), an active metabolite of 2-acetylthiomethyl-4-(4-methylphenyl)-4-oxobutanoic acid (KE-298), were compared with those of ibuprofen in rats. After administration of R(-)-[2 alpha-2H]KE-748, S(+)-KE-748 was present in the...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Yoshida H,Kohno Y,Endo H,Yamaguchi J,Fukushima K,Suwa T,Hayashi M

    更新日期:1997-01-24 00:00:00

  • Liposomal incorporation changes the effect of 1.25-dihydroxyvitamin D3 on the phospholipase C signal transduction pathway and the eicosanoid cascade on keratinocytes in vitro.

    abstract::1.25-dihydroxyvitamin D3 is of clinical importance (e.g. in the treatment of psoriasis) given its ability to regulate the proliferation and differentiation of human keratinocytes. 1.25-Dihydroxyvitamin D3 mediates its action via genomic and nongenomic pathways. The nongenomic actions begin with the activation of phosp...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Prüfer K,Jirikowski GF

    更新日期:1996-02-09 00:00:00

  • Alcohol and local anesthetic effects on Na+-dependent Ca2+ fluxes in brain synaptic membrane vesicles.

    abstract::Resealed synaptic plasma membrane vesicles exhibit Na+-dependent Ca2+ transport activity which may participate in regulation of free Ca2+ concentrations in nerve endings. Sodium chloride-loaded vesicles took up Ca2+ from the external medium (150 mM KCl-25 mM Tris/HCl) in the presence of an outward-directed Na+ gradien...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Michaelis ML,Michaelis EK

    更新日期:1983-03-15 00:00:00

  • Degradation of endomorphin-2 at the supraspinal level in mice is initiated by dipeptidyl peptidase IV: an in vitro and in vivo study.

    abstract::Endomorphin-2 (Tyr-Pro-Phe-PheNH(2)) was discovered as an endogenous ligand for the mu-opioid receptor. The physiological function of endomorphin-2 as a neurotransmitter or neuromodulator may cease through the rapid enzymatic process in the synapse of brain, as for other neuropeptides. The present study was conducted ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Sakurada C,Sakurada S,Hayashi T,Katsuyama S,Tan-No K,Sakurada T

    更新日期:2003-08-15 00:00:00

  • Effects of chronic ethanol feeding on glutathione turnover in the rat.

    abstract::Glutathione (GSH) is important in protection of cells against electrophilic drug injury and against reactive oxygen species. Both steady-state concentrations and turnover of GSH are important determinants of susceptibility of the hepatocyte to injury. Chronic ethanol administration is known to enhance susceptibility t...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Morton S,Mitchell MC

    更新日期:1985-05-01 00:00:00

  • Effects of cationic diamidines on polyamine content and uptake on Leishmania infantum in in vitro cultures.

    abstract::The effect of a series of cationic diamidines recently synthesized by Ciba Geigy, bearing diarylic (CGP040215A and CGP039937A) or monoarylic moieties (CGP033829A, CGP035537A and CGP036958A), was analyzed on some metabolic targets and cell proliferation of in vitro cultures of Leishmania infantum promastigotes (insect ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Calonge M,Johnson R,Balaña-Fouce R,Ordóñez D

    更新日期:1996-09-27 00:00:00

  • Minocycline enhances mitomycin C-induced cytotoxicity through down-regulating ERK1/2-mediated Rad51 expression in human non-small cell lung cancer cells.

    abstract::Minocycline is a semisynthetic tetracycline derivative; it has anti-inflammatory and anti-cancer effects distinct from its antimicrobial function. However, the molecular mechanism of minocycline-induced cytotoxicity in non-small cell lung cancer (NSCLC) cells has not been identified. Rad51 plays a central role in homo...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Ko JC,Wang TJ,Chang PY,Syu JJ,Chen JC,Chen CY,Jian YT,Jian YJ,Zheng HY,Chen WC,Lin YW

    更新日期:2015-10-01 00:00:00

  • Involvement of all-trans-retinoic acid in the breakdown of retinoic acid receptors alpha and gamma through proteasomes in MCF-7 human breast cancer cells.

    abstract::Most studies have reported an up-regulation of retinoic acid receptor (RAR) mRNA expression by all-trans retinoic acid (RA). We aimed to study the effect of RA on RAR protein levels in MCF-7 human breast cancer cells. Incubation of these cells with 10(-6) M RA induced a rapid breakdown of both RARalpha and RARgamma in...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Tanaka T,Rodríguez de la Concepción ML,De Luca LM

    更新日期:2001-06-01 00:00:00

  • In vivo conversion of gamma-aminobutyric acid and 1,4-butanediol to gamma-hydroxybutyric acid in rat brain. Studies using stable isotopes.

    abstract::The formation of 4-[1,4-13C]hydroxybutyric acid ([13C]gamma-hydroxybutyric acid; [13C]GHB) in rat brain was studied following intracerebroventricular (i.c.v.) administration of either 4-[1,4-13C]aminobutyric acid ([13C]GABA or 1,4-[1,4-13C]butanediol ([13C]1,4-BD) to awake, freely moving animals. GHB and [13C]GHB were...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Snead OC 3rd,Furner R,Liu CC

    更新日期:1989-12-15 00:00:00

  • Investigation of the cellular mechanism of inhibition of formyl-methionyl-leucyl-phenylalanine-induced superoxide anion generation in rat neutrophils by 2-benzyloxybenzaldehyde.

    abstract::The inhibition of formyl-methionyl-leucyl-phenylalanine (fMLP)-induced superoxide anion (O2(.-)) generation by 2-benzyloxybenzaldehyde (CCY1a) was investigated in rat neutrophils, and the underlying mechanism of this inhibition was assessed. CCY1a concentration-dependently inhibited O2(.-) generation (IC(50)=18.5+/-4....

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Wang JP,Chang LC,Lin YL,Hsu MF,Chang CY,Huang LJ,Kuo SC

    更新日期:2003-04-01 00:00:00

  • The effect of chronic ritanserin and clorgyline administration on 5-HT2 receptor linked inositol phospholipid hydrolysis.

    abstract::We have previously shown that chronic administration of the 5-hydroxytryptamine (5-HT) receptor antagonist, ritanserin (10 mg/kg/day) or the monoamine oxidase type A inhibitor (MAOI), clorgyline (2 mg/kg/day), results in a reduction in 5-HT2 receptor number in rat cerebral cortex. This study investigates the effects o...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Twist EC,Brammer MJ,Stephenson JD,Corn TH,Campbell IC

    更新日期:1990-11-01 00:00:00

  • Matrix metalloproteinase (MMP)-2 decreases calponin-1 levels and contributes to arterial remodeling in early hypertension.

    abstract::Increased matrix metalloproteinase (MMP)-2 is implicated in the vascular remodeling of hypertension. Calponin-1 is a contractile protein, and its absence is associated with vascular smooth muscle cell (VSMC) phenotype switch, which leads to migration and remodeling. We evaluated whether increased MMP-2 activity preced...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Belo VA,Parente JM,Tanus-Santos JE,Castro MM

    更新日期:2016-10-15 00:00:00

  • Growth state dependent increase of glutathione by homocysteine and other thiols, and homocysteine formation in glutathione depleted mouse cell lines.

    abstract::Homocysteine has been shown to increase glutathione levels in C3H/10T1/2 Cl 8 cells. The present paper confirms that this increase was specific for non-dividing cells. Several other thiols and disulfides, including cysteamine, mercaptoethanol and dithioerythritol, also increased glutathione, but the specificity for qu...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Djurhuus R,Svardal AM,Ueland PM

    更新日期:1990-02-01 00:00:00

  • Glutathione-dependent biliary excretion of arsenic.

    abstract::This study aimed to clarify whether glutathione (GSH) plays a role in the hepatobiliary transport of arsenic. For this purpose, the biliary excretion of 74As was measured in urethane-anaesthetized rats for 2 hr after the administration of labelled sodium arsenite (50 mumol/kg, i.v.) or arsenate (150 mumol/kg, i.v.) an...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Gyurasics A,Varga F,Gregus Z

    更新日期:1991-07-15 00:00:00

  • Inactivation of mouse epidermal 12-lipoxygenase by anthralin--implications for the role of oxygen radicals.

    abstract::In activation of 12-lipoxygenase (12-LO) in mouse epidermal homogenate by the antipsoriatic drug anthralin has been studied in detail. In view of the chemical instability of anthralin in a physiological buffer, the biological effects ascribed to the molecule itself may be related to some of its breakdown products. How...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Müller K,Gawlik I

    更新日期:1996-05-03 00:00:00

  • Induction of G(2)/M phase arrest and apoptosis by a new synthetic anti-cancer agent, DW2282, in promyelocytic leukemia (HL-60) cells.

    abstract::We studied the effect of DW2282-,[(S)-(+)-4-phenyl-1-[N-(4-aminobenzoyl)-indoline-5-sulfonyl-4,5-dihydro-2-imidazolone].hydrochloride], a newly developed anti-cancer agent, on cell proliferation, cell cycle progression, and induction of apoptosis in human promyelocytic leukemia (HL-60) cells. DW2282, a diarylsulfonylu...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Piao W,Yoo J,Lee DK,Hwang HJ,Kim JH

    更新日期:2001-12-01 00:00:00

  • A synthesized cationic tetradecapeptide from hornet venom kills bacteria and neutralizes lipopolysaccharide in vivo and in vitro.

    abstract::Sepsis is a complex clinical syndrome that results from a harmful host response to infection, in which foreign bacteria and lipopolysaccharide (LPS) are potent activators of different immune cells, including monocytes and macrophages. To date, there are currently few effective adjuvant therapies in clinical use except...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Yibin G,Jiang Z,Hong Z,Gengfa L,Liangxi W,Guo W,Yongling L

    更新日期:2005-07-15 00:00:00