A direct link between LY83583, a selective repressor of cyclic GMP formation, and glutathione metabolism.


:LY83583 (6-anilino-5,8-quinolinedione), considered to be a relatively specific repressor of cyclic GMP formation, is shown in the present study to inhibit (K(i) = 3 microM) glutathione reductase from bovine intestinal mucosa. As glutathione disulphide has been reported to inhibit guanylate cyclase irreversibly [Braughler, Biochem Pharmacol 32: 811-818, 1983], the inhibition of glutathione reductase should affect the activity of guanylate cyclase and may thus have physiological implications in the action of endothelium-derived relaxation factor and the design of muscle relaxants. LY83583 is reduced by NADPH and glutathione reductase in aerobic media and this may offer a route to the metabolic activation of LY83583. These results may have significant implications for the design of heart-regulating drugs (e.g. those used in angina), such as glyceryl trinitrate, which act via guanylate cyclase.


Biochem Pharmacol


Biochemical pharmacology


Lüönd RM,McKie JH,Douglas KT




Has Abstract


1993-06-22 00:00:00














  • Relationship of biochemical drug effects to their antitumor activity--II. Diacridines and membrane-related reactions.

    abstract::A method is presented that determines the degree of attachment of cancer cells to normal cells. This method may be useful in determining the extent to which treatment of normal cells (or of a tumor-bearing host) with a particular chemotherapeutic agent may affect the degree of attachment of cancer cells to the normal ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Elliott RE,Karadsheh NS,Kole J,Canellakis ES

    更新日期:1985-06-15 00:00:00

  • A novel role of protein kinase C-delta in cell signaling triggered by glutathione depletion.

    abstract::Current evidence demonstrates that protein kinase C (PKC) belongs to a group of cell-signaling molecules that are sensitive targets for redox modifications and functional alterations that mediate oxidant-induced cellular responses. Our studies have demonstrated that diminished intracellular GSH was associated to inact...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Domenicotti C,Marengo B,Nitti M,Verzola D,Garibotto G,Cottalasso D,Poli G,Melloni E,Pronzato MA,Marinari UM

    更新日期:2003-10-15 00:00:00

  • Resistin facilitates VEGF-C-associated lymphangiogenesis by inhibiting miR-186 in human chondrosarcoma cells.

    abstract::Chondrosarcoma is a common primary malignant tumor of the bone that can metastasize through the vascular system to other organs. A key step in the metastatic process, lymphangiogenesis, involves vascular endothelial growth factor-C (VEGF-C). However, the effects of lymphangiogenesis in chondrosarcoma metastasis remain...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Su CM,Tang CH,Chi MJ,Lin CY,Fong YC,Liu YC,Chen WC,Wang SW

    更新日期:2018-08-01 00:00:00

  • Hepatic protein tyrosine phosphatase 1B (PTP1B) deficiency protects against obesity-induced endothelial dysfunction.

    abstract::Growing evidence suggests that hepatic-insulin resistance is sufficient to promote progression to cardiovascular disease. We have shown previously that liver-specific protein-tyrosine-phosphatase 1B (PTP1B) deficiency improves hepatic-insulin sensitivity and whole-body glucose homeostasis. The aim of this study was to...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Agouni A,Tual-Chalot S,Chalopin M,Duluc L,Mody N,Martinez MC,Andriantsitohaina R,Delibegović M

    更新日期:2014-12-15 00:00:00

  • Metabolism and RNA incorporation of cyclopentenyl cytosine in human colorectal cancer cells.

    abstract::We studied the cytotoxicity and metabolism of the investigational cytidine analogue cyclopentenyl cytosine (CPE-C) in three human colorectal cancer cell lines: HCT 116, SNU-C4, and NCI-H630. CPE-C potently inhibited cell growth and decreased clonogenic capacity at concentrations achieved in murine and primate pharmaco...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Yee LK,Allegra CJ,Trepel JB,Grem JL

    更新日期:1992-04-01 00:00:00

  • Possible regulation mechanism of microsomal glutathione S-transferase activity in rat liver.

    abstract::After rats were injected with the reduced glutathione (GSH) depletor phorone (diisopropylidene acetone, 250 mg/kg, i.p.), there was a significant increase in microsomal glutathione S-transferase activity in the liver. The maximum activity was observed 24 hr after injection and was about 2-fold that of the control acti...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Masukawa T,Iwata H

    更新日期:1986-02-01 00:00:00

  • N-butyldeoxygalactonojirimycin: a more selective inhibitor of glycosphingolipid biosynthesis than N-butyldeoxynojirimycin, in vitro and in vivo.

    abstract::N-Butyldeoxynojirimycin (NB-DNJ) inhibits the ceramide glucosyltransferase which catalyses the first step in glycosphingolipid (GSL) biosynthesis. It has the potential to be used for the treatment of the GSL lysosomal storage diseases and is currently in clinical trials for the treatment of type 1 Gaucher's disease. H...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Andersson U,Butters TD,Dwek RA,Platt FM

    更新日期:2000-04-01 00:00:00

  • Cyclodextrin-complexed curcumin exhibits anti-inflammatory and antiproliferative activities superior to those of curcumin through higher cellular uptake.

    abstract::Curcumin, a yellow pigment present in the spice turmeric (Curcuma longa), has been linked with multiple beneficial activities, but its optimum potential is limited by poor bioavailability, in part due to the lack of solubility in aqueous solvents. To overcome the solubility problem, we have recently developed a novel ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,收录出版


    authors: Yadav VR,Prasad S,Kannappan R,Ravindran J,Chaturvedi MM,Vaahtera L,Parkkinen J,Aggarwal BB

    更新日期:2010-10-01 00:00:00

  • Differential patterns of inhibition of the sugar transporters GLUT2, GLUT5 and GLUT7 by flavonoids.

    abstract::Only limited data are available on the inhibition of the sugar transporter GLUT5 by flavonoids or other classes of bioactives. Intestinal GLUT7 is poorly characterised and no information exists concerning its inhibition. We aimed to study the expression of GLUT7 in Caco-2/TC7 intestinal cells, and evaluate inhibition ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Gauer JS,Tumova S,Lippiat JD,Kerimi A,Williamson G

    更新日期:2018-06-01 00:00:00

  • Synthesis and pharmacological evaluation of the novel pseudo-symmetrical tamoxifen derivatives as anti-tumor agents.

    abstract::Four pseudo-symmetrical tamoxifen derivatives, RID-B (13), RID-C (14), RID-D (15), and bis(dimethylaminophenetole) (16), were synthesized via the novel three-component coupling reaction, and the structure-activity relationships of these pseudo-symmetrical tamoxifen derivatives were examined. It was discovered that 13 ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Shiina I,Sano Y,Nakata K,Kikuchi T,Sasaki A,Ikekita M,Nagahara Y,Hasome Y,Yamori T,Yamazaki K

    更新日期:2008-03-01 00:00:00

  • P2X7 receptor antagonism: Implications in diabetic retinopathy.

    abstract::Diabetic retinopathy (DR) is the most frequent complication of diabetes and one of leading causes of blindness worldwide. Early phases of DR are characterized by retinal pericyte loss mainly related to concurrent inflammatory process. Recently, an important link between P2X7 receptor (P2X7R) and inflammation has been ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Platania CBM,Giurdanella G,Di Paola L,Leggio GM,Drago F,Salomone S,Bucolo C

    更新日期:2017-08-15 00:00:00

  • Fibrinolytic and anticoagulant activities of highly sulfated fucoidan.

    abstract::A series of fucoidan [sulfated poly(L-fucopyranose)] derivatives were prepared by chemical sulfation and desulfation, and they were tested for their abilities to stimulate tissue plasminogen activator (t-PA)-catalyzed plasminogen activation, clot lysis, and the inhibition of fibrin polymer formation. The magnitude of ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Soeda S,Sakaguchi S,Shimeno H,Nagamatsu A

    更新日期:1992-04-15 00:00:00

  • Use of comprehensive screening methods to detect selective human CAR activators.

    abstract::The so-called human xenosensors, constitutive androstane receptor (hCAR), pregnane X receptor (hPXR) and aryl hydrocarbon receptor (hAhR), participate in drug metabolism and transport as well as in several endogenous processes by regulating the expression of their target genes. While the ligand specificities for hPXR ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Küblbeck J,Laitinen T,Jyrkkärinne J,Rousu T,Tolonen A,Abel T,Kortelainen T,Uusitalo J,Korjamo T,Honkakoski P,Molnár F

    更新日期:2011-12-15 00:00:00

  • Thromboxane A2 synthase inhibition and thromboxane A2 receptor blockade by 2-[(4-cyanophenyl)amino]-3-chloro-1,4-naphthalenedione (NQ-Y15) in rat platelets.

    abstract::The effects of 2-[(4-acetylphenyl)amino]-3-chloro-1,4-naphthalenedione (NQ-Y15), a synthetic 1,4-naphthoquinone derivative, on platelet activity and its mechanism of action were investigated. NQ-Y15 caused a concentration-dependent inhibition of the aggregation induced by thrombin, collagen, arachidonic acid (AA), and...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Chang TS,Kim HM,Lee KS,Khil LY,Mar WC,Ryu CK,Moon CK

    更新日期:1997-07-15 00:00:00

  • (2,6-Dimethylphenylsulphonyl)nitromethane: a new structural type of aldose reductase inhibitor which follows biphasic kinetics and uses an allosteric binding site.

    abstract::Many of the complications of diabetes seem to be due to aldose reductase (aldehyde reductase 2, ALR2) catalysing the increased conversion of glucose to sorbitol. Therapy with aldose reductase inhibitors (ARIs) could, therefore, decrease the development of diabetic complications. (2,6-Dimethylphenylsulphonyl)nitrometha...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Ward WH,Cook PN,Mirrlees DJ,Brittain DR,Preston J,Carey F,Tuffin DP,Howe R

    更新日期:1991-11-06 00:00:00

  • Cytotoxicity of dichloromethane diphosphonate and of 1-hydroxyethane-1,1-diphosphonate in the amoebae of the slime mould Dictyostelium discoideum. A 31P NMR study.

    abstract::Two pyrophosphate analogues, dichloromethane diphosphonate (Cl2MDP), and 1-hydroxyethane-1,1-diphosphonate (EHDP), at concentrations of 0.5-1 mM, efficiently inhibited the growth of amoebae of the slime mould Dictyostelium discoideum. Cell viability decreased markedly upon incubation with the diphosphonates. The mecha...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Pelorgeas S,Martin JB,Satre M

    更新日期:1992-12-01 00:00:00

  • Cellular pharmacology of cisplatin in relation to the expression of human copper transporter CTR1 in different pairs of cisplatin-sensitive and -resistant cells.

    abstract::The molecular mechanism of cisplatin uptake remains poorly defined and impaired drug accumulation may be implicated in the acquisition of resistance to cisplatin. Thus, we used cell lines of different tumor types (ovarian carcinoma A2780 and IGROV-1, osteosarcoma U2-OS, cervix squamous cell carcinoma A431) and stable ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Beretta GL,Gatti L,Tinelli S,Corna E,Colangelo D,Zunino F,Perego P

    更新日期:2004-07-15 00:00:00

  • The role of specific cytochromes P450 in the formation of 7,12-dimethylbenz(a)anthracene-protein adducts in rat liver microsomes in vitro.

    abstract::The role of specific cytochrome P450 (P450) isoforms in the formation of adducts of 7,12-dimethylbenz(a)anthracene metabolites and membrane proteins has been investigated in vitro with microsomal fractions prepared from rats pretreated with various isoenzyme selective inducers. The effects of isoenzyme selective inhib...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Lambard SE,Burnett AK,Wolf CR,Craft JA

    更新日期:1991-09-27 00:00:00

  • Pharmacodynamic and pharmacokinetic analysis of apoE4 [L261A, W264A, F265A, L268A, V269A], a recombinant apolipoprotein E variant with improved biological properties.

    abstract::Physiological levels of wild-type (wt) apolipoprotein E (apoE) in plasma mediate the clearance of cholesterol-rich atherogenic lipoprotein remnants while higher than normal plasma apoE concentrations fail to do so and trigger hypertriglyceridemia. This property of wt apoE reduces significantly its therapeutic value as...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Lampropoulou A,Zannis VI,Kypreos KE

    更新日期:2012-12-01 00:00:00

  • Current perspectives on parathyroid hormone (PTH) and PTH-related protein (PTHrP) as bone anabolic therapies.

    abstract::Osteoporosis is characterized by low bone mineral density and/or poor bone microarchitecture leading to an increased risk of fractures. The skeletal alterations in osteoporosis are a consequence of a relative deficit of bone formation compared to bone resorption. Osteoporosis therapies have mostly relied on antiresorp...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审


    authors: Esbrit P,Alcaraz MJ

    更新日期:2013-05-15 00:00:00

  • 13-cis retinoic acid and isomerisation in paediatric oncology--is changing shape the key to success?

    abstract::Retinoic acid isomers have been used with some success as chemotherapeutic agents, most recently with 13-cis retinoic acid showing impressive clinical efficacy in the paediatric malignancy neuroblastoma. The aim of this commentary is to review the evidence that 13-cis retinoic acid is a pro-drug, and consider the impl...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审


    authors: Armstrong JL,Redfern CP,Veal GJ

    更新日期:2005-05-01 00:00:00

  • Unequivocal synthesis and characterisation of dopamine 3- and 4-O-sulphates.

    abstract::The major metabolic products of the endogeneous catecholamine dopamine are its 3- and 4-O-sulphates which have also been implicated as intermediates in noradrenaline biosynthesis. Because of the unsatisfactory status of the literature concerning the synthesis, isolation, purity and characterisation of the dopamine O-s...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Osikowska BA,Idle JR,Swinbourne FJ,Sever PS

    更新日期:1982-07-01 00:00:00

  • Protein kinase- and staurosporine-dependent induction of neurite outgrowth and plasminogen activator activity in PC12 cells.

    abstract::We analysed how interactions between protein kinase-dependent intracellular signalling pathways were implicated in the control of the production of tissue-type plasminogen activator (tPA) and the generation of neurite outgrowth by PC12 cells. To that aim, cells were treated with agents that interact with the trk recep...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Leprince P,Bonvoisin C,Rogister B,Mazy-Servais C,Moonen G

    更新日期:1996-11-08 00:00:00

  • Comparative study of clofibric acid and bilirubin glucuronidation in human liver microsomes.

    abstract::Hepatic microsomal glucuronoconjugation of the hypolipidemic drug clofibric acid was characterized in human liver and compared to the acylglucuronide formation of an endogenous substrate, bilirubin. The affinity of UDP-glucuronosyltransferase for bilirubin was 15-fold higher than for clofibric acid; the Vmax for the t...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Dragacci S,Hamar-Hansen C,Fournel-Gigleux S,Lafaurie C,Magdalou J,Siest G

    更新日期:1987-11-15 00:00:00

  • Probing the role of proline in peptide hormones. NMR studies of bradykinin and related peptides.

    abstract::The use of NMR methods to study conformational and dynamic aspects of the proline residues in the nonapeptide bradykinin is reviewed. NMR analyses involve considerations of bistable equilibria which include the cis/trans conformational heterogeneity of the imide bond, the cis'/trans' regions of conformational stabilit...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: London RE,Stewart JM,Cann JR

    更新日期:1990-07-01 00:00:00

  • Schedule dependence of sensitivity to 2',2'-difluorodeoxycytidine (Gemcitabine) in relation to accumulation and retention of its triphosphate in solid tumour cell lines and solid tumours.

    abstract::2',2'-Difluorodeoxycytidine (Gemcitabine, dFdC) is a relatively new deoxycytidine antimetabolite, with established activity against ovarian cancer and non-small-cell lung cancer. dFdC is assumed to exert its antitumour effect mainly by incorporation of the triphosphate dFdCTP into DNA. We determined the sensitivity to...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Ruiz van Haperen VW,Veerman G,Boven E,Noordhuis P,Vermorken JB,Peters GJ

    更新日期:1994-10-07 00:00:00

  • Unique inhibitory action of the synthetic compound 2-[N-(2-aminoethyl)-N-(5-isoquinolinesulfonyl)] amino-N-(4-chlorocinnamyl)-N-methylbenzylamine (CKA-1306) against calcium/calmodulin-dependent protein kinase I.

    abstract::A newly synthesized compound, 2-[N-(2-aminoethyl)-N-(5-isoquinolinesulfonyl)]amino-N-(4-chlorocinnamyl )-N-methylbenzylamine (CKA-1306), was found to inhibit cyclic AMP-dependent protein kinase (PKA) and Ca2+/calmodulin-dependent protein kinase I (CaMK I) with IC50 values of 1.6+/-0.14 and 2.5+/-0.16 microM, respectiv...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Sakaguchi H,Yokokura H,Terada O,Naito Y,Nimura Y,Hidaka H

    更新日期:1998-08-01 00:00:00

  • Subcellular localization of the camptothecin analogues, topotecan and gimatecan.

    abstract::Lipophilicity of camptothecins derivatives has been reported to improve the stability of the lactone ring and to favor rapid uptake and intracellular accumulation. Recently, a novel series of lipophilic camptothecins substituted at position 7 was developed, and gimatecan (ST1481) was selected for clinical development ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Croce AC,Bottiroli G,Supino R,Favini E,Zuco V,Zunino F

    更新日期:2004-03-15 00:00:00

  • Fas/CD95-mediated apoptosis in human glioblastoma cells: a target for sensitisation to topoisomerase I inhibitors.

    abstract::The expression of the death receptor Fas/CD95 is cell type-specific and can be modulated by different cytotoxic treatments. In spite of a frequent expression of Fas/CD95 in high-grade gliomas, these tumours are typically refractory to conventional therapy. Using a human glioblastoma cell line (GBM), we explored the po...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Ciusani E,Perego P,Carenini N,Corna E,Facchinetti F,Boiardi A,Salmaggi A,Zunino F

    更新日期:2002-03-01 00:00:00

  • Characterization of cholate-solubilized dopamine receptors from human, dog and rat brain.

    abstract::[3H]Spiperone binding sites were solubilized in high yield from human, dog and rat brain with a mixture of sodium cholate (0.3% w/v) and sodium chloride (1.4 M). The binding sites were not sedimented after one hour at 100,000 g, they passed freely through 0.20 micron filters, migrated as a single peak in gradient sedi...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章


    authors: Wouters W,van Dun J,Laduron PM

    更新日期:1984-12-15 00:00:00