Stimulation of mucus glycoprotein biosynthesis in rat gastric mucosa by gastrin.

abstract：:We compared the anti-proliferative properties of 4-benzylphenoxy-N ethyl morpholine (morpho-BPE) and trifluopromazine (TFP) on both the human breast cancer cell lines, MCF7, and its tamoxifen-resistant variant RTx6. We found that the calmodulin antagonist trifluopromazine (TFP) which bound ABS weakly, inhibited MCF7 c...

journal_title：Biochemical pharmacology

authors： Poirot M,Garnier M,Bayard F,Riviere I,Traore M,Wilson M,Fargin A,Faye JC

更新日期：1990-08-01 00:00:00

abstract：:Polyamines (putrescine, spermidine and spermine) are aliphatic amines that are produced by the action of ornithine decarboxylase (ODC) in a rate-limiting and protein kinase C (PKC)-regulated step. Because high levels of polyamines are found in the synovial fluid of arthritic patients, the aim of the present study was ...

journal_title：Biochemical pharmacology

authors： Silva MA,Klafke JZ,Rossato MF,Gewehr C,Guerra GP,Rubin MA,Ferreira J

更新日期：2011-08-01 00:00:00

abstract：:These studies were designed to investigate the effects of the chrysotherapeutic agents auranofin and myochrysine (GST) on hepatic and renal drug-metabolizing enzymes and heme metabolism. Male Sprague-Dawley rats were either administered a single dose of auranofin (17, 34, or 68 mg/kg, p.o.) or administered daily doses...

journal_title：Biochemical pharmacology

authors： Leonard TB,Graichen ME,Dahm LJ,Dent JG

更新日期：1986-09-15 00:00:00

abstract：:The present study investigated the mechanism by which theophylline decreases cis-diamminedichloroplatinum(II) (DDP)-induced DNA crosslinking in L1210 cells. Alkaline elution of DNA from L1210 cells treated with DDP in the presence and absence of 1 mM theophylline showed that theophylline decreased interstrand crosslin...

journal_title：Biochemical pharmacology

authors： Ducore JM

更新日期：1986-02-15 00:00:00

abstract：:Epilepsy is characterised by spontaneous recurrent seizures that are caused by an imbalance between neuronal excitability and inhibition. Since ion channels play fundamental roles in the generation and propagation of action potentials as well as neurotransmitter release at a subset of excitatory and inhibitory synapse...

journal_title：Biochemical pharmacology

authors： Chow CY,Absalom N,Biggs K,King GF,Ma L

更新日期：2020-11-01 00:00:00

abstract：:The aim of this study was to test if human platelet leukotriene C4-synthase (LTC4-S) is pharmacologically different from cloned and expressed LTC4-S and, in light of the significant homologies between 5-lipoxygenase activating protein (FLAP) and LTC4-S, if different potencies of leukotriene synthesis inhibitors acting...

journal_title：Biochemical pharmacology

authors： Sala A,Folco G,Henson PM,Murphy RC

更新日期：1997-03-21 00:00:00

abstract：:The differentiation-inducing factor-1 (DIF-1) is a lipophilic signal molecule (chlorinated alkylphenone) that induces stalk-cell differentiation in the cellular slime mould Dictyostelium discoideum. It has also been shown that DIF-1 and its derivative (DIF-3) suppress cell growth in mammalian tumor cells. In the prese...

journal_title：Biochemical pharmacology

authors： Gokan N,Kikuchi H,Nakamura K,Oshima Y,Hosaka K,Kubohara Y

更新日期：2005-09-01 00:00:00

abstract：:Human butyrylcholinesterase (E.C. 3.1.1.8) purified from blood plasma has previously been shown to provide protection against up to five and a half times the median lethal dose of an organophosphorus nerve agent in several animal models. In this study the stoichiometric nature of the protection afforded by human butyr...

journal_title：Biochemical pharmacology

authors： Cerasoli DM,Armstrong SJ,Reeves TE,Hodgins SM,Kasten SA,Lee-Stubbs RB,Cadieux CL,Otto TC,Capacio BR,Lenz DE

更新日期：2020-01-01 00:00:00

abstract：:The toxicity of the organophosphorus poison soman (pinacolylmethylphosphonofluoridate) is attributable to its irreversible inhibition of the enzyme acetylcholinesterase. In addition, soman binds irreversibly to a number of noncholinesterase tissue binding sites which appear to be its major means of in vivo detoxificat...

journal_title：Biochemical pharmacology

authors： Little JS,Maxwell DM,Fox-Talbot MK,Brecht K,Lenz DE

更新日期：1990-10-15 00:00:00

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

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

abstract：:Curcumin (diferuloylmethane) is a well-known agent with anti-inflammatory, antioxidant, and anticarcinogenic properties. In this study, we observed that curcumin inhibited the kinase activity of v-Src, which led to a decrease in tyrosyl substrate phosphorylation of Shc, cortactin, and FAK. Our in vitro kinase experime...

journal_title：Biochemical pharmacology

authors： Leu TH,Su SL,Chuang YC,Maa MC

更新日期：2003-12-15 00:00:00

abstract：:AMP-activated protein kinase (AMPK) activates endothelial nitric oxide synthase (eNOS) via phosphorylation at the activating site. The eNOS-nitric oxide (NO)/soluble guanylate cyclase (sGC)-cGMP/cGMP-dependent protein kinase (PKG) signaling axis is a major antiaggregatory mechanism residing in platelets. Based on the ...

journal_title：Biochemical pharmacology

authors： Liu Y,Oh SJ,Chang KH,Kim YG,Lee MY

更新日期：2013-10-01 00:00:00

abstract：:The cytoprotective effect of curcumin, a natural constituent of Curcuma longa, on the cytotoxicity of paracetamol in rat hepatocytes was studied. Paracetamol was selected as a model-toxin, since it is known to be bioactivated by 3-methylcholanthrene inducible cytochromes P450 presumably to N-acetyl-p-benzoquinone imin...

journal_title：Biochemical pharmacology

authors： Donatus IA,Sardjoko,Vermeulen NP

更新日期：1990-06-15 00:00:00

abstract：:A series of cytotoxic propenal (3-oxoprop-1-enyl) derivatives of pyrimidine bases and deoxynucleosides was evaluated for their ability to block thymidylate synthesis in intact and permeabilized murine leukemia L1210 cells. Several were potent inhibitors of this process, likely contributing to their cytotoxicity. The I...

journal_title：Biochemical pharmacology

authors： Kalman TI,Marinelli ER,Xu B,Reddy AR,Johnson F,Grollman AP

更新日期：1991-07-05 00:00:00

abstract：:Chemokines and their receptors play fundamental roles in many physiological and pathological processes such as leukocyte trafficking, inflammation, cancer and HIV-1 infection. Chemokine-receptor interactions are particularly intricate and therefore require precise orchestration. The flexible N-terminal domain of human...

journal_title：Biochemical pharmacology

authors： Szpakowska M,Fievez V,Arumugan K,van Nuland N,Schmit JC,Chevigné A

更新日期：2012-11-15 00:00:00

abstract：:High-affinity binding of [3H](+/-)2-amino-6,7-dihydroxy-1,2,3,4-tetrahydronaphthalene [( 3H]-ADTN) was improved by use of a subcellular fraction (P4) of tissue obtained from calf brain. The highest concentration of binding sites was found in caudate nucleus which was evaluated extensively. Binding of 0.5 nM [3H]-ADTN ...

journal_title：Biochemical pharmacology

authors： Arana GW,Baldessarini RJ,Lamont JS,Amlicke D,Neumeyer JL

更新日期：1983-10-01 00:00:00

abstract：:Metastatic migration of murine L1210 leukemia cells, sensitive and resistant to the antitumor agent L-phenylalanine mustard, from the peritoneal cavity of mice to the liver resulted in a 2-fold elevation in their GSH content. This increase in GSH was accompanied by a corresponding increase in their resistance to the d...

journal_title：Biochemical pharmacology

authors： Ahmad S,Mulberg A,Aljian J,Vistica DT

更新日期：1986-05-15 00:00:00

abstract：:To identify needed human equilibrative nucleoside transporter 4 (hENT4) inhibitors, we cloned and stably expressed the recombinant protein in PK15NTD (nucleoside transporter deficient) cells, and, investigated its interaction with a series of dipyridamole analogs synthesized in our laboratory. Compounds were tested in...

journal_title：Biochemical pharmacology

authors： Wang C,Lin W,Playa H,Sun S,Cameron K,Buolamwini JK

更新日期：2013-12-01 00:00:00

abstract：:The metabolism of toluene in human liver microsomes and by cDNA-expressed human cytochrome P450s (CYPs) was investigated. Toluene was metabolized mainly to benzyl alcohol and slightly to o- and p-cresol by human liver microsomes. Formation of o-cresol was elevated in microsomes from human livers derived from cigarette...

journal_title：Biochemical pharmacology

authors： Nakajima T,Wang RS,Elovaara E,Gonzalez FJ,Gelboin HV,Raunio H,Pelkonen O,Vainio H,Aoyama T

更新日期：1997-02-07 00:00:00

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

authors： Prüfer K,Jirikowski GF

更新日期：1996-02-09 00:00:00

abstract：:It has been hypothesized that oxidative modification of low density lipoprotein plays a key role in the pathogenesis of atherosclerosis. In order to elucidate the role of lipid oxidation and its inhibition in vivo, apolipoprotein E and alpha-tocopherol (alphaT) transfer protein double knockout (ApoE(-/-)alpha-TTP(-/-)...

journal_title：Biochemical pharmacology

authors： Yoshida Y,Hayakawa M,Itoh N,Habuchi Y,Inoue R,Chen ZH,Cao J,Cynshi O,Jishage K,Niki E

更新日期：2007-10-01 00:00:00

abstract：:The molecular mechanism(s) underlying induction of the hepatic microsomal cytochrome P4502E1 (2E1) by xenobiotics (e.g. ethanol and acetone) is controversial. Proposed mechanisms include increased rates of enzyme synthesis due to elevated 2E1 mRNA levels, enhanced translation of pre-existing mRNA, or stabilization of ...

journal_title：Biochemical pharmacology

authors： Kraner JC,Lasker JM,Corcoran GB,Ray SD,Raucy JL

更新日期：1993-04-06 00:00:00

abstract：:Thromboxane A2 is a potent mediator of inflammation and platelet aggregation exerting its effects through the activation of a G protein-coupled receptor (GPCR), termed TP. Although the existence of dimers/oligomers in Class A GPCRs is widely accepted, their functional significance still remains controversial. Recently...

journal_title：Biochemical pharmacology

authors： Capra V,Mauri M,Guzzi F,Busnelli M,Accomazzo MR,Gaussem P,Nisar SP,Mundell SJ,Parenti M,Rovati GE

更新日期：2017-01-15 00:00:00

abstract：:Binding of the selective D-1 dopamine receptor ligand 125I SCH 23982 was studied using crude plasma membranes derived from human renal cortex. 125I SCH 23982 bound saturably to a single high affinity site (Kd = 650 pM, Bmax = 19 fmol/mg protein). Binding at 37 degrees was rapid and reversible with forward and reverse ...

journal_title：Biochemical pharmacology

authors： Hughes A,Sever P

更新日期：1989-03-01 00:00:00

abstract：:A growing body of evidence suggests that mitochondria take up calcium upon receptor (agonist) stimulation and that this contributes to the dynamics of spatiotemporal calcium signaling. We have previously shown that engagement of the high-affinity receptor for immunoglobulin E (FcepsilonRI) stimulates mitochondrial cal...

journal_title：Biochemical pharmacology

authors： Suzuki Y,Yoshimaru T,Inoue T,Nunomura S,Ra C

更新日期：2008-04-01 00:00:00

abstract：AIMS:Protein Kinase R (PKR) plays a key role in inflammation and insulin resistance. Cytokines, high fat diet, infection and various stress signals can activate PKR. However, the functional significance of PKR in diabetic cardiomyopathy (DCM) is not explored so far. Thus the aim of the present study was to investigate ...

journal_title：Biochemical pharmacology

authors： Mangali S,Bhat A,Jadhav K,Kalra J,Sriram D,Vamsi Krishna Venuganti V,Dhar A

更新日期：2020-07-01 00:00:00

abstract：:F 11782, or 2',3'-bis-pentafluorophenoxyacetyl-4',6'-ethylidene-beta-D-glucoside of 4'-phosphate-4'-dimethylepipodophyllotoxin 2-N-methyl glucamine salt, a novel dual catalytic inhibitor of topoisomerases I and II, was identified as a potent inhibitor of nucleotide excision repair (NER) by screening procedures using t...

journal_title：Biochemical pharmacology

authors： Barret JM,Cadou M,Hill BT

更新日期：2002-01-15 00:00:00

abstract：:Superoxide radicals have been implicated in the pathogenesis of aging, cataract, ischemia-reperfusion, cancer and inflammatory diseases. In the present work, we found that deferiprone (L1), an iron-chelating drug, and dietary dihydroxycinnamic acids (catechols) were much more effective at protecting isolated rat hepat...

journal_title：Biochemical pharmacology

authors： Moridani MY,O'Brien PJ

更新日期：2001-12-15 00:00:00

abstract：:Dinucleotides of adenosine and thymidine in the ApnT series (n = 3,4,5 and 6) and their corresponding phosphonate analogues, where a methylene group replaces the oxygen between the alpha and beta phosphorus atoms adjacent to thymidine, have been evaluated as inhibitors of human leukaemic thymidylate kinase (dTMP kinas...

journal_title：Biochemical pharmacology

authors： Orr RM,Davies LC,Stock JA,Taylor GA,Powles RL,Harrap KR

更新日期：1988-02-15 00:00:00

abstract：:Induction of cytosolic long-chain acyl-CoA hydrolases was investigated in rat liver after administration of various peroxisome proliferators and related compounds. Treatment of rats with di-(2-ethylhexyl)-phthalate, di-(2-ethylhexyl)-adipate or tiadenol induced hydrolases I and II, while acetylsalicylic acid induced o...

journal_title：Biochemical pharmacology

authors： Katoh H,Nakajima S,Kawashima Y,Kozuka H,Uchiyama M

更新日期：1984-04-01 00:00:00