Potent and selective hydroxynaphthoquinone inhibitors of mitochondrial electron transport in Eimeria tenella (Apicomplexa: Coccidia).

abstract：:The effects of three phenothiazines, promethazine, thiazinamium chloride and chlorpromazine, on macrophage function were investigated in rat alveolar macrophages. The study focused on thromboxane B2 (TxB2) synthesis, zymosan phagocytosis, and hexosemonophosphate (HMP) shunt activity in these phagocytes. TxB2 synthesis...

journal_title：Biochemical pharmacology

authors： Chang J,Piperata S,Skowronek M,Lewis AJ

更新日期：1983-09-15 00:00:00

abstract：:Change in the membrane fluidity of human erythrocytes on transformation to stomatocytes was observed by ESR spectroscopy using 12-doxyl stearic acid or its methyl ester as a probe. When the transformation to stomatocytes was induced by four qualitatively different methods, i.e. (a) addition of cationic amphiphilic age...

journal_title：Biochemical pharmacology

authors： Noji S,Takahashi T,Kon H

更新日期：1982-10-15 00:00:00

abstract：:We previously reported that in hyperuricemic rats, renal impairment occurred and organic ion transport activity decreased, accompanied with a specific decrease in the expression of rat organic anion transporters, rOAT1 and rOAT3, and organic cation transporter, rOCT2. In the present study, we investigated the reversib...

journal_title：Biochemical pharmacology

authors： Habu Y,Yano I,Okuda M,Fukatsu A,Inui K

更新日期：2005-03-15 00:00:00

abstract：:The cytochrome P450-dependent metabolism of benzo(a)pyrene and other xenobiotics has been investigated in liver microsomes prepared from a local marine safi fish, Siganus canaliculatus. The safi fish was found to have a well-developed microsomal monooxygenase system consisting of cytochrome P450, cytochrome b5 and NAD...

journal_title：Biochemical pharmacology

authors： Raza H,Otaiba A,Montague W

更新日期：1995-10-26 00:00:00

abstract：:The binding of phenylbutazone (PB) to human serum albumin (HSA) at different pH and in the presence of different NaSCN and urea concentrations that alter the conformation of the protein was examined qualitatively on the basis of extrinsic elliptical strength at 288 nm by means of circular dichroism (CD). The values of...

journal_title：Biochemical pharmacology

authors： Watanabe S,Saito T

更新日期：1992-03-03 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：:Miconazole and clotrimazole, members of a class of imidazole agents which have broad spectrum antimycotic activity, were shown to be potent inhibitors of steroid aromatase activity of human placental microsomes. The I50 values for the inhibition of aromatase activity by miconazole, clotrimazole, ketoconazole, and amin...

journal_title：Biochemical pharmacology

authors： Mason JI,Murry BA,Olcott M,Sheets JJ

更新日期：1985-04-01 00:00:00

abstract：:Endotoxin (LPS) and interleukin-1 beta (IL-1 beta) increased the expression of tissue factor, a membrane-anchored glycoprotein that initiates blood coagulation on the surface of cultured human umbilical vein endothelial cells (HUVEC) and human monocyte/macrophages. On monocyte/macrophages, oleic acid strongly inhibite...

journal_title：Biochemical pharmacology

authors： Lalé A,Herbert JM

更新日期：1994-07-19 00:00:00

abstract：:The anticancer drug cis-diamminedichloroplatinum(II) (cisplatin) has been shown previously to form adducts preferentially within internucleosomal or linker DNA rather than to DNA within the nucleosome. To determine whether other "open" regions of chromatin have an increased affinity for cisplatin, adduct formation wit...

journal_title：Biochemical pharmacology

authors： Bubley GJ,Xu J,Kupiec N,Sanders D,Foss F,O'Brien M,Emi Y,Teicher BA,Patierno SR

更新日期：1996-03-08 00:00:00

abstract：:We examined whether any changes were induced in cellular proteins by an inhibitor of acylpeptide hydrolase (ACPH) (EC 3.4.19.1), acetylleucine chloromethyl ketone (ALCK), which was shown in our previous report to induce apoptosis of human U937 cells. Extract prepared from U937 cells in 0.05% Triton X-100-PBS was incub...

journal_title：Biochemical pharmacology

authors： Yamaguchi M,Tsuchiya Y,Chikuma T,Hojo H

更新日期：2002-05-15 00:00:00

abstract：:The increasing incidence of severe liver diseases worldwide has resulted in a high demand for curative liver transplantation. Unfortunately, the need for transplants by far eclipses the availability of suitable grafts leaving many waitlisted patients to face liver failure and often death. Routine use of smaller grafts...

journal_title：Biochemical pharmacology

authors： Greenbaum LE,Ukomadu C,Tchorz JS

更新日期：2020-05-01 00:00:00

abstract：:We have previously found that repeated exposure to heroin reduces liver synthesis of morphine-3-glucuronide (M3G) and increases the production of morphine-6-glucuronide (M6G), which normally is not formed in the rat. By contrast repeated exposure to naltrexone does not activate M6G synthesis but increases the V(max) o...

journal_title：Biochemical pharmacology

authors： Antonilli L,Brusadin V,Milella MS,Sobrero F,Badiani A,Nencini P

更新日期：2008-09-01 00:00:00

abstract：:The regulation of neurotensin-induced phosphoinositide turnover was studied in transfected CHO cells expressing the rat neurotensin receptor. Stimulation of these cells with neurotensin resulted in an important, but transient, increase in inositol phosphate cell content. Preincubation of the cells with neurotensin dra...

journal_title：Biochemical pharmacology

authors： Hermans E,Maloteaux JM

更新日期：1996-06-28 00:00:00

abstract：:Thioredoxin reductase (TR1) is a selenoprotein that is involved in cellular redox status control and deoxyribonucleotide biosynthesis. Many cancers, including lung, overexpress TR1, making it a potential cancer therapy target. Previous work has shown that TR1 knockdown enhances the sensitivity of cancer cells to antic...

journal_title：Biochemical pharmacology

authors： Poerschke RL,Moos PJ

更新日期：2011-01-15 00:00:00

abstract：:Developmental correlation of higher levels of estrogen binding by macromolecules in rat liver supernatant and of increases in plasma renin substrate levels after estrogen administration is reported. Gel filtration columns were used to separate bound from free radioactivity in studying binding of radioactive estradiol...

journal_title：Biochemical pharmacology

authors： Eisenfeld AJ,Krakoff LR,Aten RF

更新日期：1977-05-15 00:00:00

abstract：:The formyl peptide receptor (FPR) gene family has a complex evolutionary history and comprises eight murine members but only three human representatives. To enable translation of results obtained in mouse models of human diseases, more comprehensive knowledge of the pharmacological similarities/differences between the...

journal_title：Biochemical pharmacology

authors： Skovbakke SL,Winther M,Gabl M,Holdfeldt A,Linden S,Wang JM,Dahlgren C,Franzyk H,Forsman H

更新日期：2016-11-01 00:00:00

abstract：:HeLa S3 cells exposed to Adriamycin and Daunomycin for 3 hr at EC90 and 10 x EC90 concentrations and incubated in drug-free medium demonstrated the characteristics of apoptosis, morphological changes and fragmentation of DNA into oligonucleosome-sized fragments. The kinetics of DNA degradation after incubation with Ad...

journal_title：Biochemical pharmacology

authors： Skladanowski A,Konopa J

更新日期：1993-08-03 00:00:00

abstract：:Purification of functional nucleoside transporters has been hampered by the instability of detergent-solubilized proteins. The present study was undertaken to determine if the presence of specific transporter ligands in the solubilization medium could enhance the functional stability of the isolated proteins. Ehrlich ...

journal_title：Biochemical pharmacology

authors： Hammond JR

更新日期：1997-03-07 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：:Oral administration of tobacco to rats for 21 days caused remarkable stimulation of the metabolism of phenacetin, aniline and benzo[a]pyrene, a carcinogen, by hepatic microsomal mixed function oxidases (MFO). Such treatment for 6 days resulted in a small increase in the activities of phenacetin O-dealkylase and aromat...

journal_title：Biochemical pharmacology

authors： Kaur S,Ali B

更新日期：1982-04-15 00:00:00

abstract：:Taxol is an antineoplastic agent with significant activity against ovarian as well as breast cancer. To investigate mechanisms by which taxol exerts its cytotoxic action, taxol-induced apoptosis, characterized by morphologic changes and internucleosomal DNA fragmentation, was examined in a human ovarian tumor cell lin...

journal_title：Biochemical pharmacology

authors： Liu Y,Bhalla K,Hill C,Priest DG

更新日期：1994-09-15 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：:The effect of naturally occurring hydroxystilbene, 3,3',4,5-tetrahydroxystilbene (piceatanol), and its derivatives on gastric H+, K(+)-ATPase was studied. Piceatanol inhibited H+, K(+)-ATPase in a dose-dependent manner. The 50% inhibition value was 4.3 x 10(-6) M. It was found from the kinetic study that the inhibitio...

journal_title：Biochemical pharmacology

authors： Murakami S,Arai I,Muramatsu M,Otomo S,Baba K,Kido T,Kozawa M

更新日期：1992-11-17 00:00:00

abstract：:Chronic exposure to the divalent heavy metals, such as iron, lead, manganese (Mn), and chromium, has been linked to the development of severe, often irreversible neurological disorders and increased vulnerability to developing Parkinson's disease. Although the mechanisms by which these metals elicit or facilitate neur...

journal_title：Biochemical pharmacology

authors： Roth JA,Garrick MD

更新日期：2003-07-01 00:00:00

abstract：:Interleukin-6 (IL-6) is known to differentiate the rat pheochromocytoma cell line PC12 to neuron-like cells. We examined the effect of IL-6 on the death of PC12 cells. IL-6 significantly blocked the death of PC12 cells by serum deprivation. The protective effect of IL-6 was increased by preincubation of PC12 with IL-6...

journal_title：Biochemical pharmacology

authors： Umegaki H,Yamada K,Naito M,Kameyama T,Iguchi A,Nabeshima T

更新日期：1996-09-27 00:00:00

abstract：:We previously demonstrated that the widely used immunosuppressive drugs cyclosporin A (CsA) and tacrolimus (FK506), independent of immunophilin binding, can activate profibrogenic transforming growth factor β (TGFβ)/Smad signaling cascades in rat renal mesangial cells (MC). Here we report that both peptidyl-prolyl cis...

journal_title：Biochemical pharmacology

authors： Akool el-S,Gauer S,Osman B,Doller A,Schulz S,Geiger H,Pfeilschifter J,Eberhardt W

更新日期：2012-01-15 00:00:00

abstract：:BAY X 1005 ((R)-2-[4-(quinolin-2-yl-methoxy)phenyl]-2-cyclopentyl acetic acid) has been demonstrated to be a potent inhibitor of leukotriene B4 (LTB4) and 5-hydroxyeicosatetraenoic acid (5-HETE) synthesis in various in vitro systems. Using mainly human polymorphonuclear leukocytes (PMNL) this study elucidates the mech...

journal_title：Biochemical pharmacology

authors： Hatzelmann A,Fruchtmann R,Mohrs KH,Raddatz S,Müller-Peddinghaus R

更新日期：1993-01-07 00:00:00

abstract：:The antimicrobial peptide human beta-defensin-3 (hBD-3) is produced by epidermal keratinocytes and protects the skin from infections. This peptide induces the release of a lipid mediator, prostaglandin D(2) from dermal mast cells. Prostaglandin D(2) binds to cell-surface G protein-coupled receptors, D prostanoid recep...

journal_title：Biochemical pharmacology

authors： Kanda N,Ishikawa T,Watanabe S

更新日期：2010-04-01 00:00:00

abstract：:Cystic fibrosis (CF) is a common lethal genetic disease caused by autosomal recessive mutations of the cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel that belongs to the ATP-Binding Cassette (ABC) family of transporters. The class III CF mutations G551D and G1349D are located within the "s...

journal_title：Biochemical pharmacology

authors： Melin P,Thoreau V,Norez C,Bilan F,Kitzis A,Becq F

更新日期：2004-06-15 00:00:00

abstract：:The effect of methotrexate (MTX) on 6-mercaptopurine (6-MP) metabolism was studied in four human leukemic cell lines in vitro. CCRF-CEM, WI-L2, TBJ, and HL-60 all expressed thiopurine methyltransferase (TPMT) activity. The cells were grown in horse serum-supplemented RPMI 1640 medium to which was added 4 microM of 6-M...

journal_title：Biochemical pharmacology

authors： Giverhaug T,Loennechen T,Aarbakke J

更新日期：1998-05-15 00:00:00