abstract：:Multiple molecular forms of cyclic nucleotide phosphodiesterase have been characterized in various tissues and cells according to their substrate specificity, intracellular location, and calmodulin dependence. The purpose of this study was to evaluate the possible involvement of different molecular forms of phosphodie...

journal_title：Biochemical pharmacology

authors： Wright CD,Kuipers PJ,Kobylarz-Singer D,Devall LJ,Klinkefus BA,Weishaar RE

更新日期：1990-08-15 00:00:00

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：:Sulfation of tyrosyl residue(s) has been found to be a post-translational modification that precedes the secretion of many biologically active proteins or peptides. In the present paper, we report on the characterization of human liver tyrosylprotein sulfotransferase (TPST), the enzyme responsible for sulfation of tyr...

journal_title：Biochemical pharmacology

authors： Lin WH,Roth JA

更新日期：1990-08-01 00:00:00

abstract：:A 4',5'-unsaturated 5'-fluoroadenosine inhibitor of S-adenosyl-L-homocysteine hydrolase (SAH hydrolase; EC 3.3.1.1), MDL 28842, was found to inhibit markedly the growth of Plasmodium falciparum in vitro and Plasmodium berghei in mice. Inhibition of P. berghei growth was associated with a large increase in the concentr...

journal_title：Biochemical pharmacology

authors： Bitonti AJ,Baumann RJ,Jarvi ET,McCarthy JR,McCann PP

更新日期：1990-08-01 00:00:00

abstract：:Enhanced aggregation of platelets was observed in platelet-rich plasma, but not in washed platelet suspension (WPS), during acute inflammation in rats. Incubation of WPS with inflammatory plasma increased the aggregatory response to ADP, but the plasma itself did not cause aggregation of platelets. It potentiated the ...

journal_title：Biochemical pharmacology

authors： Srivastava R,Srimal RC

更新日期：1990-07-15 00:00:00

abstract：:The microbial alkaloid staurosporine is a member of a recently described family of protein kinase inhibitors. [N,N-dimethyl-3H]N-dimethylstaurosporine ([3H]DMS) was prepared from staurosporine by methylation with [3H]methyl iodide. Since staurosporine inhibits protein kinase C (PKC) most potently, the binding of [3H]D...

journal_title：Biochemical pharmacology

authors： Gross JL,Herblin WF,Do UH,Pounds JS,Buenaga LJ,Stephens LE

更新日期：1990-07-15 00:00:00

abstract：:Homogenization of rat kidney under isotonic conditions and in the presence of protease inhibitors showed that some 92% of the cyclic AMP phosphodiesterase activity and some 83% of the cyclic GMP phosphodiesterase activity was released into the soluble fraction. Analysis of soluble phosphodiesterase activity by FPLC on...

journal_title：Biochemical pharmacology

authors： Hoey M,Houslay MD

更新日期：1990-07-15 00:00:00

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：: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

authors： London RE,Stewart JM,Cann JR

更新日期：1990-07-01 00:00:00

abstract：:Acid secretion from isolated rabbit gastric parietal cells can be stimulated by gastric secretagogues, histamine (cyclic-AMP pathway) and carbachol (inositol phosphate pathway). Prostaglandins (PG) from E series are potent inhibitors of acid secretion. The intracellular mechanism of this inhibition was examined by usi...

journal_title：Biochemical pharmacology

authors： Choquet A,Leonard A,Magous R,Bali JP

更新日期：1990-06-15 00:00:00

abstract：:The (Na+ + K+)-ATPase is localized to the cerebral endothelium, i.e. the blood-brain barrier, and is important for the maintenance of the brain electrolyte environment. Data from the present study indicate that Pb2+ inhibits the binding of [3H]ouabain to the cerebral microvascular (Na+ + K+)-ATPase in a time- and dose...

journal_title：Biochemical pharmacology

authors： Caspers ML,Kwaiser TM,Grammas P

更新日期：1990-06-15 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：:We have demonstrated that the simplest steady-state random sequential Bi Bi mechanism is sufficient to explain the previously reported non-hyperbolic kinetics of glutathione S-transferase 3-3 [Pabst MJ et al., J Biol Chem 249: 7140-7150, 1974; Jakobson I et al., Biochem J 177: 861-868, 1979]. The metabolism of 1-chlor...

journal_title：Biochemical pharmacology

authors： Ivanetich KM,Goold RD,Sikakana CN

更新日期：1990-06-15 00:00:00

abstract：:SR 4233 (3-amino-1,2,4-benzotriazine-1,4-dioxide) is a novel benzotriazine di-N-oxide which shows unusually high selective toxicity towards hypoxic cells, probably as a result of reductive bioactivation. Using an HPLC assay for the parent drug and its 2- and 4-electron reduction products (SR 4317 and SR 4330, respecti...

journal_title：Biochemical pharmacology

authors： Walton MI,Workman P

更新日期：1990-06-01 00:00:00

abstract：:The structure and membrane interactions of lipophilic glucosyl phosphotriester derivatives of thymidine and 5-fluoro-deoxy thymidine are investigated by NMR spectroscopy. The self-association of these molecules, found in different solvents, presents a diastereoisomeric effect which is also observed in the transmembran...

journal_title：Biochemical pharmacology

authors： Debouzy JC,Hervé M,Neumann JM,Gouyette C,Dupraz B,Huynh-Dinh T

更新日期：1990-06-01 00:00:00

abstract：:The mechanism by which the substituted benzimidazole sulphoxide BY 1023/SK&F 96022 inhibited the (H+ + K+)-ATPase, the enzyme responsible for hydrogen ion secretion in the stomach, was studied in a variety of in vitro preparations. In gastric preparations that were capable of active hydrogen ion transport with consequ...

journal_title：Biochemical pharmacology

authors： Simon WA,Keeling DJ,Laing SM,Fallowfield C,Taylor AG

更新日期：1990-06-01 00:00:00

abstract：:The effect of 3'-deoxythymidin-2'-ene (d4T) on the metabolism of exogenously supplied radiolabeled nucleosides was investigated. Following a 24-hr exposure to 250 microM d4T, we observed no significant effect on the incorporation of [3H]thymidine or [3H]deoxycytidine into DNA. In contrast, the amounts of [3H]uridine, ...

journal_title：Biochemical pharmacology

authors： Marongiu ME,August EM,Prusoff WH

更新日期：1990-05-15 00:00:00

abstract：:Castanospermine (CS) is a potent but non-selective inhibitor of many glycohydrolases including the intestinal disaccharidases. Several CS-glucosides were synthesized to investigate the effect of an attached glucopyranosyl residue on the potency and selectivity of CS toward inhibition of intestinal disaccharidases. 8 a...

journal_title：Biochemical pharmacology

authors： Rhinehart BL,Robinson KM,King CH,Liu PS

更新日期：1990-05-15 00:00:00

abstract：:Colchiceine, a closely related structural analog of colchicine possessing a C-ring tropolone, has been shown to be a potent inhibitor of microtubule assembly in vitro (I50 = 20 microM). The mechanism of inhibition is mediated through binding to tubulin (KA = 1.2 +/- 0.7 x 10(4) M-1), although potentially not through t...

journal_title：Biochemical pharmacology

authors： Hastie SB,Macdonald TL

更新日期：1990-04-15 00:00:00

abstract：:The localization of [3H]forskolin binding to microscope slide mounted sections of rat kidney has been examined using autoradiography. Saturation studies showed [3H]forskolin binding to two sites, a high affinity site (KD = 8.7 nM, Bmax = 0.14 pmol/mg protein) and a low affinity site (KD = 6.7 microM, Bmax = 11.0 pmol/...

journal_title：Biochemical pharmacology

authors： McMartin LR,Summers RJ

更新日期：1990-03-15 00:00:00

abstract：:Enzymatic N,O-acyltransfer of carcinogenic N-arylhydroxamic acids such as N-hydroxy-2-acetylaminofluorene (N-OH-AAF) results in the production of reactive electrophiles that can bond covalently with nucleophiles and also can cause inactivation of acyltransferase activity in a mechanism-based manner. Incubation of part...

journal_title：Biochemical pharmacology

authors： Wick MJ,Hanna PE

更新日期：1990-03-15 00:00:00

abstract：:The effect of diethylcarbamazine (DEC) on microtubules was studied by using microtubule protein prepared from porcine brain. DEC inhibited assembly of microtubules and disassembled preformed microtubules in vitro. When the reassembled or disassembled products were examined in the presence of DEC by electron microscopy...

journal_title：Biochemical pharmacology

authors： Fujimaki Y,Ehara M,Kimura E,Shimada M,Aoki Y

更新日期：1990-03-01 00:00:00

abstract：:The stereoselective binding of carprofen enantiomers and carprofen glucuronide diastereomers to human serum albumin (HSA) was studied using an ultrafiltration method. Carprofen glucuronides exhibit a considerable and stereoselective affinity to HSA, although less than that seen for the parent enantiomers. The (S)-gluc...

journal_title：Biochemical pharmacology

authors： Iwakawa S,Spahn H,Benet LZ,Lin ET

更新日期：1990-03-01 00:00:00

abstract：:Energy-dependent drug efflux is a major factor in cellular resistance of P388/R84 mouse leukemic cells to anthracyclines such as doxorubicin (DOX), and blocking of efflux increases sensitivity. However, efflux does not play a significant role in resistance to N-trifluoroacetyladriamycin-14-valerate (AD 32), a DOX anal...

journal_title：Biochemical pharmacology

authors： Nair S,Singh SV,Samy TS,Krishan A

更新日期：1990-02-15 00:00:00

abstract：:gamma-Carbolines are tricyclic aromatic compounds which intercalate into DNA base pairs and exhibit significant cytotoxic and antitumor activities. These compounds which are structurally related to ellipticine by deletion of an aromatic ring, induce DNA breaks in cultured L1210 cells. Since the mechanism of cytotoxic ...

journal_title：Biochemical pharmacology

authors： Fossé P,René B,Saucier JM,Nguyen CH,Bisagni E,Paoletti C

更新日期：1990-02-15 00:00:00

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

authors： Djurhuus R,Svardal AM,Ueland PM

更新日期：1990-02-01 00:00:00

abstract：:Several monoclonal antibodies against human liver glutathione S-transferase mu were developed. One of these monoclonal antibodies, called GST-3H4 was further characterized and used in this study. In hepatic tissue, after immunoblotting, GST-3H4 strains a 27 kDa protein with a pI value of 6.2. GST-3H4 recognizes other ...

journal_title：Biochemical pharmacology

authors： Peters WH,Kock L,Nagengast FM,Roelofs HM

更新日期：1990-02-01 00:00:00

abstract：:Sodium nitroprusside (SNP) stimulates cGMP formation to a greater extent in 20,000 g supernatant fractions of the human neuroblastoma clones NB1-G and SH-SY5Y than in the human astrocytoma clone D384. This suggests that these cell lines contain the soluble form of guanylate cyclase. Arachidonic, 8,11,14- and 11,14,17-...

journal_title：Biochemical pharmacology

authors： Vaughan PF,Ball SG

更新日期：1990-02-01 00:00:00

abstract：:Engelbreth-Holm-Swarm (EHS) tumor cells were utilized as a model for investigating the production of basement membrane components. These cells contain two immunologically distinct NADPH-dependent reductases, aldose reductase (EC 1.1.1.21) and aldehyde reductase (EC 1.1.1.2), which were purified to apparent homogeneity...

journal_title：Biochemical pharmacology

authors： Tanimoto T,Sato S,Kador PF

更新日期：1990-02-01 00:00:00

abstract：:This study was designed to examine the relationship between the extent of Sandimmun (cyclosporin A, SIM) metabolism and SIM-induced hepatotoxicity both in vivo and in primary cultures of rat hepatocytes. Firstly, SIM (50 mg/kg p.o.) was administered daily to male Wistar rats for 10 days with or without co-administrati...

journal_title：Biochemical pharmacology

authors： Bouis P,Brouillard JF,Fischer V,Donatsch P,Boelsterli UA

更新日期：1990-01-15 00:00:00

abstract：:Structure-activity studies on a series of analogues of N-(3-methyl-S-(1-pyrrolidinyl carbonyl) butyl)-D-alanine ethyl ester hydrochloride (SC42619) have defined the features of this dipeptide analogue required for observation of thrombin receptor antagonist activity on the human platelet. The affinity for SC42619, and...

journal_title：Biochemical pharmacology

authors： Ruda EM,Scrutton MC,Manley PW,Tuffin DP

更新日期：1990-01-15 00:00:00

abstract：:The 2-haloethylnitrosoureas have been shown to form the cross-linked structure 1-(3-cytosinyl),2-(1-guanyl)ethane in DNA. This cross-link has now been synthesized by the reaction of O6-(2-fluoroethyl)guanosine with deoxycytidine in dimethyl sulfoxide followed by removal of the sugars by acid hydrolysis. This synthetic...

journal_title：Biochemical pharmacology

authors： MacFarland JG,Kirk MC,Ludlum DB

更新日期：1990-01-01 00:00:00

abstract：:Using the incorporation of [3H]isoleucine or [3H]hypoxanthine into acid-insoluble products as indices of protein- and nucleic acid-synthetic activity, respectively, it was shown that seven plant-derived quassinoids with differing chemical substitutions all inhibited protein synthesis more rapidly than nucleic acid syn...

journal_title：Biochemical pharmacology

authors： Kirby GC,O'Neill MJ,Phillipson JD,Warhurst DC

更新日期：1989-12-15 00:00:00

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

authors： Snead OC 3rd,Furner R,Liu CC

更新日期：1989-12-15 00:00:00

abstract：:Irradiation of a cytosolic fraction from vascular smooth muscle in the presence of [3H]felodipine resulted in the labelling of a protein with an apparent molecular weight of 62 kDa. The labelling was seen on UV-irradiation at 360 nm, but not at 254, 278 or at wavelengths above 410 nm. The photolabelling was enhanced i...

journal_title：Biochemical pharmacology

authors： Nilsson A,Westerlund C,Boström S

更新日期：1989-12-01 00:00:00

abstract：:Incubation of human carcinoma cells with mitoxantrone resulted in an intracellular distribution of the drug into cytoplasmic, nuclear and cytoskeletal compartments occurring within 1 min of drug treatment. Incubation of the cells in drug-free medium resulted in an efflux of the drug such that 80% of the intracellular ...

journal_title：Biochemical pharmacology

authors： Roberts RA,Cress AE,Dalton WS

更新日期：1989-12-01 00:00:00

abstract：:The antiepileptic sodium valproate (VPA) systematically induces an asymptomatic hyperammonemia of renal origin in fasting normal human volunteers and in fasting rats, accompanied by an increased renal glutamine uptake. Fasting rats were injected with VPA and their mitochondria isolated, or isolated mitochondria of fas...

journal_title：Biochemical pharmacology

authors： Rumbach L,Cremel G,Marescaux C,Warter JM,Waksman A

更新日期：1989-11-15 00:00:00

abstract：:Bovine serum albumin (BSA) catalyzes the o-rearrangement of the reactive electrophile, N-sulfooxy-2-acetylaminofluorene (NSF), a potential ultimate hepatocarcinogen in the rat, to the nonmutagenic sulfuric acid esters of 1- and 3-hydroxy-2-acetylaminofluorene. Conversion of NSF was proportional to BSA concentrations r...

journal_title：Biochemical pharmacology

authors： Smith BA,Gutmann HR,Springfield JR

更新日期：1989-11-15 00:00:00

abstract：:The triazolobenzodiazepine compound alprazolam may have unique clinical effects compared to other benzodiazepines, and both behavioral and neurochemical studies have indicated unusual results after acute doses of alprazolam. To determine the effects of chronic dosage in mice, alprazolam (2 mg/kg/day) was administered ...

journal_title：Biochemical pharmacology

authors： Miller LG,Woolverton S,Greenblatt DJ,Lopez F,Roy RB,Shader RI

更新日期：1989-11-01 00:00:00

abstract：:Tianeptine is a new tricyclic antidepressant which is metabolized mainly by beta-oxidation of its heptanoic side chain. We determined the effects of tianeptine on the mitochondrial oxidation of natural fatty acids in mice. In vitro, tianeptine (0.5 mM) inhibited by only 32% the formation of beta-oxidation products fro...

journal_title：Biochemical pharmacology

authors： Fromenty B,Freneaux E,Labbe G,Deschamps D,Larrey D,Letteron P,Pessayre D

更新日期：1989-11-01 00:00:00