Novel kainic acid analogues. Effects on cyclic GMP content of adult rat cerebellar slices.

abstract：:2',3'-Dideoxy-beta-L-5-fluorocytidine (beta-L-FddC) and 2',3'-dideoxy-beta-L-cytidine (beta-L-ddC), two nucleosides with "unnatural L-configuration," have been synthesized and found to have potent antiviral activity against hepatitis B virus (HBV) and human immunodeficiency virus type 1 (HIV-1) in vitro with very litt...

journal_title：Biochemical pharmacology

authors： Lin TS,Luo MZ,Liu MC,Pai SB,Dutschman GE,Cheng YC

更新日期：1994-01-20 00:00:00

abstract：:N-Nitrosoguanidines are potential carcinogens. However, the toxicity of these agents is attenuated significantly in laboratory rodents by processes that remove the nitroso group to generate the relatively innocuous parent guanidinium compound. The denitrosation of 1,3-dimethyl-2-cyano-1-nitrosoguanidine (CyanoDMNG) me...

journal_title：Biochemical pharmacology

authors： Jensen DE,Belka GK,Dworkin C

更新日期：1997-05-09 00:00:00

abstract：:Cancer metastasis is a major cause for cancer-related death and inhibiting cancer metastasis is an alternative way to treat cancer. Several lines of reported evidence suggest that NADPH oxidase 4 (NOX4) is a potential target for intervention of cancer metastasis, as the reactive oxygen species (ROS) generated by this ...

journal_title：Biochemical pharmacology

authors： Zhang B,Liu Z,Hu X

更新日期：2013-07-15 00:00:00

abstract：:In eukaryotic cells, the DNA molecule is found in the form of a nucleoprotein complex named chromatin. The basic unit of the chromatin is the nucleosome, which comprises 147 base pairs of DNA wrapped around an octamer of core histones (made of two molecules of each H2A, H2B, H3, and H4 histones). Each nucleosome is li...

journal_title：Biochemical pharmacology

authors： Quina AS,Buschbeck M,Di Croce L

更新日期：2006-11-30 00:00:00

abstract：:The microsomal fraction of bone marrow contains cytochrome P-450 (39 +/- 11 pmoles/mg microsomal protein) and monooxygenase activity could be demonstrated by the O-dealkylation of 7-ethoxycoumarin (114 +/- 65 pmoles/(min X mg microsomal protein] and the hydroxylation of benzene to phenol (51 +/- 8.6 pmol/45 min X mg m...

journal_title：Biochemical pharmacology

authors： Gollmer L,Graf H,Ullrich V

更新日期：1984-11-15 00:00:00

abstract：:Itch, a member of the E6AP carboxy terminus (HECT) domain-containing family of ubiquitin E3 ligases, acts in concert with the ubiquitin activating enzyme (E1) and the ubiquitin conjugating enzyme (E2) to catalyze ubiquitylation of protein targets. This sub-family of E3s shares a 350 residue C-terminal HECT domain havi...

journal_title：Biochemical pharmacology

authors： Raimondo D,Giorgetti A,Bernassola F,Melino G,Tramontano A

更新日期：2008-12-01 00:00:00

abstract：:Metformin, a commonly used agent in the treatment of type 2 diabetes, is also associated with reduced risk of cancer development and improvement in cancer survival. Although much is known about metformin, the mechanisms behind its anti-cancer properties are not fully understood. In this study we addressed the role of ...

journal_title：Biochemical pharmacology

authors： Zhao Q,Zhou X,Curbo S,Karlsson A

更新日期：2018-10-01 00:00:00

abstract：:The mechanism of aerobic resistance to the quinone-containing anti-tumour agents mitomycin C (MMC) and porfiromycin (PM) has been investigated using non-transformed human cells. One of the cell strains used (3437T) was derived from an afflicted member of a cancer-prone family. This cell strain had been shown previousl...

journal_title：Biochemical pharmacology

authors： Marshall RS,Paterson MC,Rauth AM

更新日期：1991-05-01 00:00:00

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

authors： Chazot PL,Fotherby A,Stephenson FA

更新日期：1993-02-09 00:00:00

abstract：:The effects of ticlopidine and six of its analogues on mitochondrial functions were studied in isolated rat liver mitochondria. The influence of ticlopidine and each of the following analogues: PCR 5325, PCR 4099, PCR 3787, PCR 2362, PCR 4499 and PCR 0665 was evaluated by determining their interaction with three major...

journal_title：Biochemical pharmacology

authors： Abou-Khalil WH,Lim LO,Yunis AA,Abou-Khalil S

更新日期：1984-12-01 00:00:00

abstract：:The role of Ca2+ and protein kinase C (PKC) activity in the release of immunoreactive endothelin-1 (ET-1) from cultured porcine aortic endothelial cells of first or second passage has been studied. ET-1 accumulation within cells and secretion into cell-conditioned medium over 3 and/or 5 hr was measured. Confluent cell...

journal_title：Biochemical pharmacology

authors： Brunner F

更新日期：1995-06-16 00:00:00

abstract：:Toll-like receptors (TLRs) are key components of the innate immune system, functioning as pattern recognition receptors that recognise a wide range of microbial pathogens. TLRs represent a primary line of defence against invading pathogens in mammals, plants and insects. Recognition of microbial components by TLRs tri...

journal_title：Biochemical pharmacology

authors： Doyle SL,O'Neill LA

更新日期：2006-10-30 00:00:00

abstract：:Studies have shown that CYP2C9.1 mediated metabolism of flurbiprofen or naproxen is activated by co-incubation with dapsone. However, dapsone activation has not been examined in the known variant forms of CYP2C9. Six concentrations of flurbiprofen (2-300microM) or naproxen (10-1800 microM) were co-incubated with six c...

journal_title：Biochemical pharmacology

authors： Hummel MA,Dickmann LJ,Rettie AE,Haining RL,Tracy TS

更新日期：2004-05-15 00:00:00

abstract：:Cyclosporine A (CsA) is the immunosuppressor most frequently used in transplant surgery and in the treatment of autoimmune diseases because of its specific inhibiting effect on signal transduction pathways of cell T receptor. It has been shown that CsA is able to generate reactive oxygen species and lipid peroxidation...

journal_title：Biochemical pharmacology

authors： Andrés D,Bautista M,Cascales M

更新日期：2005-02-01 00:00:00

abstract：:Drug addiction is a chronic relapsing disorder that produces a dramaticglobal health burden worldwide. Not effective treatment of drug addiction is currently available probably due to the difficulties to find an appropriate target to manage this complex disease raising the needs for further identification of novel the...

journal_title：Biochemical pharmacology

authors： Manzanares J,Cabañero D,Puente N,García-Gutiérrez MS,Grandes P,Maldonado R

更新日期：2018-11-01 00:00:00

abstract：:The O2 dependence of the metabolism of benzylamine to benzaldehyde, benzoate and hippurate was studied in isolated rat hepatocytes. The initial oxidation to benzaldehyde, catalyzed by monoamine oxidase, had an apparent Kmo2 value of 34 microM in cells and 40 microM in isolated rat liver mitochondria. The conversion of...

journal_title：Biochemical pharmacology

authors： Jones DP

更新日期：1984-02-01 00:00:00

abstract：:The Wnt/Frizzled signaling pathway plays multiple functions in animal development and, when deregulated, in human disease. The G-protein coupled receptor (GPCR) Frizzled and its cognate heterotrimeric Gi/o proteins initiate the intracellular signaling cascades resulting in cell fate determination and polarization. In ...

journal_title：Biochemical pharmacology

authors： Koval A,Purvanov V,Egger-Adam D,Katanaev VL

更新日期：2011-11-15 00:00:00

abstract：:Mitochondrial carriers are proteins that shuttle a variety of metabolites, nucleotides and coenzymes across the inner mitochondrial membrane. The mitochondrial ADP/ATP carriers (AACs) specifically translocate the ATP synthesized within mitochondria to the cytosol in exchange for the cytosolic ADP, playing a key role i...

journal_title：Biochemical pharmacology

authors： Todisco S,Di Noia MA,Onofrio A,Parisi G,Punzi G,Redavid G,De Grassi A,Pierri CL

更新日期：2016-01-15 00:00:00

abstract：:[3H]Morphine, PL-017[prolyl-3,4-3H,D-prolyl,3,4-3H] ([3H]PL-017) and enkephalin-(2-D-penicillamine,5-D-penicillamine)[tyrosyl-2,6-3H] ([3H]DPDPE) were directly cross-linked to mouse brain opiate receptors by an ultraviolet (254 nm) irradiation procedure. [3H]Morphine preferentially and specifically labeled a 58 kDa pr...

journal_title：Biochemical pharmacology

authors： Nagamatsu K,Tagawa Y,Uchida S,Hasegawa A

更新日期：1993-10-05 00:00:00

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

authors： Wouters W,van Dun J,Laduron PM

更新日期：1984-12-15 00:00:00

abstract：:N-[5-[N-(3,4-Dihydro-2-methyl-4-oxoquinazolin-6-ylmethyl)-N- methylamino]-2-thenoyl]-L-glutamic acid (ZD1694) is a folate-based thymidylate synthase (TS; EC 2.1.1.45) inhibitor. Metabolism to higher chain length polyglutamates is essential for its optimal cytotoxic effect. A ZD1694-resistant (300-fold) human ileocecal...

journal_title：Biochemical pharmacology

authors： Lu K,Yin MB,McGuire JJ,Bonmassar E,Rustum YM

更新日期：1995-07-31 00:00:00

abstract：:The fallen concentration of one of the two isomers of soman (1,2,2-trimethylpropyl methylphosphonofluoridate), i.e., C(+)P(-)-soman, was investigated in plasma and in homogenates of brain, lung, liver, kidney, diaphragm, skeletal muscle and mucosa of small intestines from rat, guinea pig and marmoset, and in human pla...

journal_title：Biochemical pharmacology

authors： de Jong LP,van Dijk C,Berhitoe D,Benschop HP

更新日期：1993-10-19 00:00:00

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

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

更新日期：1991-09-27 00:00:00

abstract：:Double-labelled [methyl-14C,5-3H]CDPcholine has been synthesized and subjected to a pharmacokinetic analysis in several biological systems. In transport experiments with intact human erythrocytes no incorporation of radioactivity is observable. On the other hand the results obtained with perfused rat liver suggest a r...

journal_title：Biochemical pharmacology

authors： Galletti P,De Rosa M,Nappi MA,Pontoni G,del Piano L,Salluzzo A,Zappia V

更新日期：1985-12-01 00:00:00

abstract：:An abnormally high rate of aerobic glycolysis is characteristic of many transformed cells. Here we report the polyphenolic compound, resveratrol, inhibited phosphatidylinositol 3-kinase (PI-3K) signaling and glucose metabolism, coinciding with cell-cycle arrest, in germinal center (GC)-like LY1 and LY18 human diffuse ...

journal_title：Biochemical pharmacology

authors： Faber AC,Dufort FJ,Blair D,Wagner D,Roberts MF,Chiles TC

更新日期：2006-11-15 00:00:00

abstract：:Phentermine was shown in the 1970s to inhibit the metabolism of serotonin by monoamine oxidase (MAO), but never was labeled as an MAO inhibitor; hence, it was widely used in combination with fenfluramine, and continues to be used, in violation of their labels, with other serotonin uptake blockers. We examined the effe...

journal_title：Biochemical pharmacology

authors： Ulus IH,Maher TJ,Wurtman RJ

更新日期：2000-06-15 00:00:00

abstract：:We have performed a systematic study of the interaction of 36 di- and tri-phenylethylene derivatives (DPEs and TPEs) with protein kinase C (PKC). The results were submitted to a multivariate analysis in order to identify the structural features that might be implicated in interference with the activity of three PKC su...

journal_title：Biochemical pharmacology

authors： Bignon E,Pons M,Doré JC,Gilbert J,Ojasoo T,Miquel JF,Raynaud JP,Crastes de Paulet A

更新日期：1991-09-12 00:00:00

abstract：:In this study we compared two methods, electron spin resonance (ESR) spectroscopy and high performance liquid chromatography (HPLC), which are currently used to detect directly hydroxyl radical (OH.) formation in the ischemic and reperfused heart. Isolated buffer-perfused rat hearts were subjected to 30 min of normoth...

journal_title：Biochemical pharmacology

authors： Tosaki A,Bagchi D,Pali T,Cordis GA,Das DK

更新日期：1993-02-24 00:00:00

abstract：:We have studied the effects of the recently reported two new metabolites of the antitumor agent VP-16-213, the ortho-dihydroxy derivative or catechol and the ortho-quinone, on the biological activity of single-stranded and double-stranded phi X174 DNA, the binding of the metabolites to calf thymus DNA and the conversi...

journal_title：Biochemical pharmacology

authors： van Maanen JM,Lafleur MV,Mans DR,van den Akker E,de Ruiter C,Kootstra PR,Pappie D,de Vries J,Retèl J,Pinedo HM

更新日期：1988-10-01 00:00:00

abstract：:GABAB receptors assemble from GABAB1 and GABAB2 subunits. GABAB2 additionally associates with auxiliary KCTD subunits (named after their K(+) channel tetramerization-domain). GABAB receptors couple to heterotrimeric G-proteins and activate inwardly-rectifying K(+) channels through the βγ subunits released from the G-p...

journal_title：Biochemical pharmacology

authors： Adelfinger L,Turecek R,Ivankova K,Jensen AA,Moss SJ,Gassmann M,Bettler B

更新日期：2014-10-01 00:00:00