Suppression of beta-catenin signaling by liver X receptor ligands.

abstract：:Cyclophilin (163 amino acids; 17,737 daltons) is a ubiquitous cytosolic protein that specifically binds the potent immunosuppressive drug cyclosporin A (CsA). To characterize the structural details of this interaction, extensive use has been made of two-dimensional (2D) NMR methods. For studies on CsA, these methods a...

journal_title：Biochemical pharmacology

authors： Hsu VL,Heald SL,Harding MW,Handschumacher RE,Armitage IM

更新日期：1990-07-01 00:00:00

abstract：:Recent experiments from our laboratory have indicated that the inhibitory effect of 3'-azido-3'-deoxythymidine (AZT) on oxidative phosphorylation may occur directly, in addition to being brought about by its inhibition of mtDNA replication. We report here studies on the effect of AZT on adenylate kinase, an enzyme cru...

journal_title：Biochemical pharmacology

authors： Barile M,Valenti D,Hobbs GA,Abruzzese MF,Keilbaugh SA,Passarella S,Quagliariello E,Simpson MV

更新日期：1994-10-07 00:00:00

abstract：:Three grams of nafazatrom (Bay g 6575), given orally to healthy male volunteers in a single dose, significantly reduce the formation of leukotriene B4 in polymorphonuclear leukocytes. LTB4 synthesis fell from 57.1 +/- 17.0 ng/10(7) PMNL, mean +/- S.D., in control to 34.3 +/- 14.4 ng/10(7) PMNL 3 hr after nafazatrom (2...

journal_title：Biochemical pharmacology

authors： Strasser T,Fischer S,Weber PC

更新日期：1985-06-01 00:00:00

abstract：:MRP1 overexpression in multidrug-resistant cancer cells has been shown to be responsible for collateral sensitivity to some flavonoids that stimulate a huge MRP1-mediated GSH efflux. This massive GSH depletion triggers the death of these cancer cells. We describe here that bivalent flavonoid dimers strikingly stimulat...

journal_title：Biochemical pharmacology

authors： Dury L,Nasr R,Lorendeau D,Comsa E,Wong I,Zhu X,Chan KF,Chan TH,Chow L,Falson P,Di Pietro A,Baubichon-Cortay H

更新日期：2017-01-15 00:00:00

abstract：:In artificially ventilated beagle dogs a severe hypoglycemic condition was induced by insulin injection, while the posthypoglycemic recovery was induced by glucose treatment at the end of a 20-min period of spontaneous electroencephalographic silence. The motor area of the cerebral cortex was analyzed for glycolytic m...

journal_title：Biochemical pharmacology

authors： Benzi G,Gorini A,Dossena M,Taglietti M,Fulle D,Pastoris O

更新日期：1983-03-15 00:00:00

abstract：:In the present study, a novel synthetic compound 4-(2-(cyclohex-2-enylidene)hydrazinyl)quinolin-2(1H)-one (CYL-4d) was found to inhibit lipopolysaccharide (LPS)-induced nitric oxide (NO) production without affecting cell viability or enzyme activity of expressed inducible NO synthase (iNOS) in RAW 264.7 macrophages. C...

journal_title：Biochemical pharmacology

authors： Lin MW,Tsao LT,Chang LC,Chen YL,Huang LJ,Kuo SC,Tzeng CC,Lee MR,Wang JP

更新日期：2007-06-01 00:00:00

abstract：:Tetranitromethane (TNM) is a reagent which reacts with the tyrosine and cysteine residues of proteins. Chemical modification of partially purified human platelet alpha 2-adrenoceptors with TNM resulted in an irreversible loss of binding activity. Typically, an 80-90% decrease in binding activity occurred with a 60-min...

journal_title：Biochemical pharmacology

authors： Nakata H,Regan JW,Lefkowitz RJ

更新日期：1986-11-15 00:00:00

abstract：:Oligodendrocytes and activated macrophages are involved in the immunopathology of demyelinating disease. In this study, we investigated the in vitro effect of dietary compounds, in particular flavonoids, on oxidative damage in OLN-93 oligodendrocytes and on nitric oxide (NO) production by NR8383 macrophages. Using a c...

journal_title：Biochemical pharmacology

authors： van Meeteren ME,Hendriks JJ,Dijkstra CD,van Tol EA

更新日期：2004-03-01 00:00:00

abstract：:The Na(+), K(+)-ATPase is a ubiquitous membrane transport protein in mammalian cells, responsible for establishing and maintaining high K(+) and low Na(+) in the cytoplasm required for normal resting membrane potentials and various cellular activities. The ionic homeostasis maintained by the Na(+), K(+)-ATPase is also...

journal_title：Biochemical pharmacology

authors： Yu SP

更新日期：2003-10-15 00:00:00

abstract：:The enhanced nitric oxide (NO) and prostaglandin (PG) generation of activated macrophages is controlled by glucocorticoid-sensitive inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), respectively. Negative feedback regulation of iNOS expression by the products of both pathways has been suggested, but...

journal_title：Biochemical pharmacology

authors： Pang L,Hoult JR

更新日期：1997-02-21 00:00:00

abstract：:Several reports suggest that the antimalarial mode of action of quinoline drugs may differ in their mechanistic details. The malaria parasite Plasmodium falciparum was treated in culture with chloroquine, amodiaquine, quinine and mefloquine in a dose- and time-dependent fashion. After removal of the drug, the viabilit...

journal_title：Biochemical pharmacology

authors： Famin O,Ginsburg H

更新日期：2002-02-01 00:00:00

abstract：:The metabolism of (1R)[1-3H]ethanol, [2-3H]lactate or [2-3H]xylitol was studied in hepatocytes from fed or T3-treated rats in the presence or absence of fructose or xylitol. The yields of tritium in ethanol, lactate, water, glycerol and glucose were determined. A simple model, describing the metabolic fate of tritium ...

journal_title：Biochemical pharmacology

authors： Vind C,Grunnet N

更新日期：1985-03-01 00:00:00

abstract：:The effect of ifosfamide and its metabolites on intracellular levels of glutathione in P388 cells in vitro has been studied. It is demonstrated that glutathione depletion occurs only in the presence of 4-hydroperoxyifosfamide and chloroacetaldehyde. In contrast isophosphoramide mustard had no effect on glutathione lev...

journal_title：Biochemical pharmacology

authors： Lind MJ,McGown AT,Hadfield JA,Thatcher N,Crowther D,Fox BW

更新日期：1989-06-01 00:00:00

abstract：:Dexamethasone and etoposide both induce apoptosis in immature rat thymocytes. We investigated the dependence of apoptosis on the phase of the cell cycle after incubation with these drugs. Cell cycle progression was followed by a combination of pulse labelling with 5-bromo-2'-deoxyuridine (BrdU), labelling fixed cells ...

journal_title：Biochemical pharmacology

authors： Fearnhead HO,Chwalinski M,Snowden RT,Ormerod MG,Cohen GM

更新日期：1994-09-15 00:00:00

abstract：:β1-Adrenergic receptor (β1-AR) agonists and antagonists are widely used in the treatment of major cardiovascular diseases such as heart failure and hypertension. The β1-AR like other G protein-coupled receptors (GPCRs) are endocytosed in response to intense agonist activation. Recycling of the agonist-internalized β1-...

journal_title：Biochemical pharmacology

authors： Nooh MM,Mancarella S,Bahouth SW

更新日期：2016-11-15 00:00:00

abstract：:There is increasing evidence that S-nitrosylation is a mechanism for the regulation of protein function via the modification of critical sulfhydryl groups. The activity of rat liver microsomal glutathione S-transferase (GST) is increased after treatment with N-ethylmaleimide (NEM), a sulfhydryl alkylating reagent, and...

journal_title：Biochemical pharmacology

authors： Ji Y,Toader V,Bennett BM

更新日期：2002-04-15 00:00:00

abstract：:Recently, accumulated statistical data indicate the protective effect of caffeine consumption against several types of cancer diseases. There are also reports about protective effect of caffeine and other xanthines against tumors induced by polycyclic aromatic hydrocarbons. One of the explanations is based on biologic...

journal_title：Biochemical pharmacology

authors： Kapuscinski J,Ardelt B,Piosik J,Zdunek M,Darzynkiewicz Z

更新日期：2002-02-15 00:00:00

abstract：:Phospho-tyrosol-indomethacin (PTI; MPI 621), a novel anti-cancer agent, is more potent and safer than conventional indomethacin. Here, we show that PTI was extensively metabolized in vitro and in vivo. PTI was rapidly hydrolyzed by carboxylesterases to generate indomethacin as its major metabolite in the liver microso...

journal_title：Biochemical pharmacology

authors： Xie G,Zhou D,Cheng KW,Wong CC,Rigas B

更新日期：2013-04-15 00:00:00

abstract：:Suramin, a drug intensively used in the chemotherapy of African trypanosomiasis and onchocerciasis, is currently being tested in clinical trials for AIDS treatment. Its effects on mitochondrial energy metabolism in mammals were studied. At low concentrations it inhibited ATP synthesis and ATPase activity in submitocho...

journal_title：Biochemical pharmacology

authors： Calcaterra NB,Vicario LR,Roveri OA

更新日期：1988-07-01 00:00:00

abstract：:Repertaxin is a new non-competitive allosteric blocker of interleukin-8 (CXCL8/IL-8) receptors (CXCR1/R2), which by locking CXCR1/R2 in an inactive conformation prevents receptor signaling and human polymorphonuclear leukocyte (PMN) chemotaxis. Given the unique mode of action of repertaxin it was important to examine ...

journal_title：Biochemical pharmacology

authors： Casilli F,Bianchini A,Gloaguen I,Biordi L,Alesse E,Festuccia C,Cavalieri B,Strippoli R,Cervellera MN,Di Bitondo R,Ferretti E,Mainiero F,Bizzarri C,Colotta F,Bertini R

更新日期：2005-02-01 00:00:00

abstract：:Male mice were exposed via their diet to perfluoro fatty acids of various chain-lengths (2-10 carbon atoms) at different doses (0.02 and 0.1% weight) and for different periods of time (2-10 days). Thereafter, we monitored effects on liver and body weights and a number of hepatic parameters, including mitochondrial pro...

journal_title：Biochemical pharmacology

authors： Permadi H,Lundgren B,Andersson K,DePierre JW

更新日期：1992-09-25 00:00:00

abstract：:The chemotherapeutic drug cisplatin is an important treatment for many types of solid tumours, in particular non-small cell lung cancer (NSCLC). Platinum(IV) complexes offer several advantages to cisplatin due to their requirement for reduction to the active platinum(II) form to elicit cytotoxicity. This should minimi...

journal_title：Biochemical pharmacology

authors： Mellor HR,Snelling S,Hall MD,Modok S,Jaffar M,Hambley TW,Callaghan R

更新日期：2005-10-15 00:00:00

abstract：:Human ABCG2 is a plasma membrane glycoprotein that provides physiological protection against xenobiotics. ABCG2 also significantly influences biodistribution of drugs through pharmacological tissue barriers and confers multidrug resistance to cancer cells. Moreover, ABCG2 is the molecular determinant of the side popul...

journal_title：Biochemical pharmacology

authors： Hegedüs C,Truta-Feles K,Antalffy G,Várady G,Német K,Ozvegy-Laczka C,Kéri G,Orfi L,Szakács G,Settleman J,Váradi A,Sarkadi B

更新日期：2012-08-01 00:00:00

abstract：:Interferon and interferon inducers are well known to depress the cytochrome P450-dependent hepatic mixed-function oxidase system and cause a decrease in the capacity of the liver to metabolize drugs and xenobiotics. In this study we have shown that the interferon-mediated changes in an induced form of hepatic cytochro...

journal_title：Biochemical pharmacology

authors： Knickle LC,Spencer DF,Renton KW

更新日期：1992-08-04 00:00:00

abstract：:The effects of staurosporine, a protein kinase inhibitor, on the signal transduction and proliferation of thymocytes were studied. Signal transduction in response to Concanavalin A (Con A) as well as Concanavalin A (Con A)-induced augmentation of [3H]inositol incorporation into phospholipids were inhibited by staurosp...

journal_title：Biochemical pharmacology

authors： Zilberman Y,Gutman Y

更新日期：1992-10-20 00:00:00

abstract：:The antidepressant minaprine (3-(2-morpholino-ethylamino) 4-methyl 6-phenyl pyridazine, dihydrochloride) and its main metabolites were examined for their monoamine oxidase (MAO) inhibitory effects in the rat. In our experimental conditions, minaprine displayed in vitro a very weak affinity for brain MAO A and B with I...

journal_title：Biochemical pharmacology

authors： Kan JP,Mouget-Goniot C,Worms P,Biziere K

更新日期：1986-03-15 00:00:00

abstract：:With the aid of a chiral derivatizing reagent and a sensitive and specific nitrogen-phosphorus gas chromatographic assay, metabolism of para-chloroamphetamine (PCA) enantiomers has been studied following incubation of racemic (RS)-, R(-)- and S(+)-PCA with rabbit liver microsomal preparations. Significant metabolism o...

journal_title：Biochemical pharmacology

authors： Ames MM,Frank SK

更新日期：1982-01-01 00:00:00

abstract：:Circumvention of multidrug resistance in vitro by resistance modulators is well documented but their clinical use may be limited by effects on normal tissues. We have compared four resistance modifiers, both in terms of modulation of doxorubicin sensitivity in vitro and toxicity in vivo, in order to determine whether ...

journal_title：Biochemical pharmacology

authors： Plumb JA,Wishart GC,Setanoians A,Morrison JG,Hamilton T,Bicknell SR,Kaye SB

更新日期：1994-01-20 00:00:00

abstract：:Cyclophosphamides are pro-drugs whose killing agent is produced from an aldehyde that is formed by the action of a P450 oxidation step. The mustard from the aldehyde can destroy bone marrow cells as well as the tumor. Aldehyde dehydrogenase (EC 1.2.1.3) can oxidize the aldehyde and hence inactivate the cytotoxic inter...

journal_title：Biochemical pharmacology

authors： Ho KK,Mukhopadhyay A,Li YF,Mukhopadhyay S,Weiner H

更新日期：2008-09-01 00:00:00

abstract：:Eighteen linear analogues of [Arg8]vasopressin (AVP) were synthesized by systematically substituting the cysteine residues at positions 1 and 6 with a range of L-amino acids. Screening by competition ligand binding revealed that the combinations of amino acid residues tolerated at these positions was very restricted w...

journal_title：Biochemical pharmacology

authors： Howl J,Filer AD,Parslow RA,Kirk CJ,Jurzak M,Smith AI,Wheatley M

更新日期：1994-04-29 00:00:00