Substrates for arachidonic acid co-oxidation with peroxidase/hydrogen peroxide. Further evidence for radical intermediates.

abstract：:Improved syntheses, based on Lewis acid-catalyzed nucleosidation, are described for the preparation of 5-alkyl-2'-deoxyuridines. These were converted to their 5'-phosphates with the use of wheat shoot phosphotransferase. The dUMP analogues, 5-ethyl-dUMP and 5-propyl-dUMP, were competitive vs dUMP inhibitors of thymidy...

journal_title：Biochemical pharmacology

authors： Rode W,Kulikowski T,Kedzierska B,Jastreboff M,Shugar D

更新日期：1984-09-01 00:00:00

abstract：:Recently, the marked decline in renal carnitine reabsorption has been thought to account fotr the systemic carnitine deficiency in juvenile visceral steatosis (JVS) mice. We have conducted a kinetic analysis using embryonic fibroblasts derived from normal, heterozygous, and homozygous jvs mice and found that the high-...

journal_title：Biochemical pharmacology

authors： Hashimoto N,Suzuki F,Tamai I,Nikaido H,Kuwajima M,Hayakawa J,Tsuji A

更新日期：1998-05-15 00:00:00

abstract：:The uptake of iron by the liver and cerebellum was measured in rats using [59Fe]transferrin. An acute ethanol load (50 mmol/kg body wt., i.p.) elicited a significant increase in the hepatic and cerebellar non-heme iron concentration. The uptake of 59Fe by the liver and the cerebellum was significantly greater in the e...

journal_title：Biochemical pharmacology

authors： Rouach H,Houze P,Gentil M,Orfanelli MT,Nordmann R

更新日期：1994-05-18 00:00:00

abstract：:Peroxidase (EC 1.11.1.7)/H2O2, ceruloplasmin (human type X)/O2, and tyrosinase (EC 1.14.18.1)/O2 all oxidized the indolic neurotransmitter 5-hydroxytryptamine (5-HT) in the physiological pH domain. Peroxidase/H2O2 oxidized 5-HT at pH values down to about 2.5. All oxidation reactions generated complex mixtures of produ...

journal_title：Biochemical pharmacology

authors： Wrona MZ,Dryhurst G

更新日期：1991-04-15 00:00:00

abstract：:Monocrotaline is a pyrrolizidine alkaloid obtained from the seeds of Crotalaria spectabilis. When perfused through an isolated liver, monocrotaline is metabolized to Ehrlich reactive (E+) metabolites. Metabolism of monocrotaline was faster in livers from male rats than female rats, was inducible with phenobarbital pre...

journal_title：Biochemical pharmacology

authors： Lafranconi WM,Huxtable RJ

更新日期：1984-08-01 00:00:00

abstract：:Administration to hamsters of a highly purified human leukocyte interferon subtype, IFN-alpha A, obtained by recombinant DNA methods, abolished the efficacy of high doses of cyclophosphamide (2.5 mg/hamster) against the TBD 932 lymphosarcoma. The effect was more pronounced with concomitant than with sequential treatme...

journal_title：Biochemical pharmacology

authors： Lee SH,Chiu H,Renton KW,Stebbing N

更新日期：1984-11-01 00:00:00

abstract：:The effects of propranolol or phentolamine on the metabolism of phospholipids, diacylglycerol, and triacylglycerol were studied in the bovine retina in vitro. Lipid labeling was followed during short-term incubation of intact bovine retinas with [U-14C]glycerol and [1-14C]palmitic acid. Each of these precursors was re...

journal_title：Biochemical pharmacology

authors： de Boschero MG,Bazan NG

更新日期：1982-03-15 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：:Extrahepatic cytochrome P450 enzymes (CYP450) are pivotal in the metabolism of endogenous substrates and xenobiotics. CYP2J2 is a major cardiac CYP450 and primarily metabolizes polyunsaturated fatty acids such as arachidonic acid to cardioactive epoxyeicosatrienoic acids. Due to its role in endobiotic metabolism, CYP2...

journal_title：Biochemical pharmacology

authors： Karkhanis A,Hong Y,Chan ECY

更新日期：2017-07-01 00:00:00

abstract：:Lipids play a complex role in prostate cancer (PCa). Increased de novo synthesis of fatty acids and/or cholesterol is associated with the development of prostate tumors. Liver X Receptors (LXRs) are members of the nuclear receptor family that regulates intracellular lipid homeostasis. Targeting the transcriptional act...

journal_title：Biochemical pharmacology

authors： Hoang JJ,Baron S,Volle DH,Lobaccaro JM,Trousson A

更新日期：2013-07-01 00:00:00

abstract：:Histamine H-1 receptors in human peripheral lung were characterized by radioligand and biochemical assays employing binding of the H-1 receptor antagonist [3H]pyrilamine to plasma membrane preparations. Simultaneous computerized analyses of the data from fourteen separate equilibrium-binding assays indicated the prese...

journal_title：Biochemical pharmacology

authors： Casale TB,Rodbard D,Kaliner M

更新日期：1985-09-15 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：:Pregnancy is associated with uteroplacental and vascular remodeling in order to adapt for the growing fetus and the hemodynamic changes in the maternal circulation. We have previously shown upregulation of uterine matrix metalloproteinases (MMPs) during pregnancy. Whether pregnancy-associated changes in MMPs are local...

journal_title：Biochemical pharmacology

authors： Dang Y,Li W,Tran V,Khalil RA

更新日期：2013-09-15 00:00:00

abstract：:Rats fed 1% paracetamol in the diet failed to grow and a dose-dependent inhibition of growth was observed and found to be independent of hepatoxicity. Addition of 0.5% D- or L-methionine, or L-cysteine to a diet containing 1% paracetamol restored growth. Addition of L-methionine to the drinking water was equally effec...

journal_title：Biochemical pharmacology

authors： McLean AE,Armstrong GR,Beales D

更新日期：1989-01-15 00:00:00

abstract：:Phenylbutyrate has been shown recently to induce fetal hemoglobin (HbF) production in patients with sickle cell anemia and beta thalassemia. We have now examined related aromatic fatty acids in order to define the range of active structures and identify plausible mechanisms of action. Structure-function analysis revea...

journal_title：Biochemical pharmacology

authors： Hudgins WR,Fibach E,Safaya S,Rieder RF,Miller AC,Samid D

更新日期：1996-10-25 00:00:00

abstract：:The International Diabetes Federation predicts that by 2045 the number of individuals afflicted with diabetes will increase to 629 million. Furthermore, ∼352 million individuals with impaired glucose tolerance are at increased risk for developing diabetes. Several mechanisms have been proposed for the onset of metabol...

journal_title：Biochemical pharmacology

authors： Kowluru A,Kowluru RA

更新日期：2018-08-01 00:00:00

abstract：:Cytosolic sulfotransferases (SULTs), which mediate the conjugation of drugs with 3'-phosphoadenosine-5'-phosphosulfate, have been characterized in humans and cynomolgus monkeys. However, SULTs remain to be evaluated in common marmosets, a species of non-human primate often employed in drug metabolism and pharmacokinet...

journal_title：Biochemical pharmacology

authors： Uno Y,Uehara S,Murayama N,Shimizu M,Yamazaki H

更新日期：2020-10-01 00:00:00

abstract：:Nicotine has been shown in a variety of studies to improve cognitive function including learning, memory and attention. Nicotine both stimulates and desensitizes nicotinic receptors, thus acting both as an agonist and a net antagonist. The relative roles of these two actions for nicotine-induced cognitive improvement ...

journal_title：Biochemical pharmacology

authors： Levin ED

更新日期：2013-10-15 00:00:00

abstract：:We have examined chromosome damage caused by a wide range of bleomycin (BLM) concentrations in Chinese hamster ovary (CHO-K1) cells reversibly porated by the bacterial cytotoxin streptolysin-O (SLO). Chromosome damage was measured using the micronucleus cytokinesis block technique (employing cytochalasin-B). Treatment...

journal_title：Biochemical pharmacology

authors： Johnston PJ,Bryant PE

更新日期：1993-02-09 00:00:00

abstract：:Two antitumor antibiotics doxorubicin and daunorubicin were tested for their ability to influence the activation of protein kinase C in human platelets. Daunorubicin was found to inhibit the phosphorylation of the 40 K PKC substrate induced by thrombin and 12-O-tetradecanoyl-phorbol-13-acetate as well as the phosphory...

journal_title：Biochemical pharmacology

authors： Lanzi C,Banfi P,Ravagnani F,Gambetta RA

更新日期：1988-09-15 00:00:00

abstract：:The characteristics of the muscarinic receptor in isolated gastric fundic cells from rabbit were determined by radioligand binding techniques and functional tests. The dissociation constants (KDS) of selective (hexahydrosiladifenidol and pirenzepine) and non-selective (N-methylscopolamine and atropine) muscarinic rece...

journal_title：Biochemical pharmacology

authors： Baudiere B,Monferini E,Giraldo E,Ladinsky H,Bali JP

更新日期：1987-09-15 00:00:00

abstract：:Nuclear factor-E2-related factor 2 (Nrf2) is a master transcription factor in antioxidant response, protecting against oxidative damage and various diseases. Previous studies suggest that Nrf2 is suppressed in fibrotic skin and Nrf2 agonists represent a therapeutic strategy, which is mainly attributed to Nrf2 function...

journal_title：Biochemical pharmacology

authors： Wu R,Zhang H,Zhao M,Li J,Hu Y,Fu J,Pi J,Wang H,Xu Y

更新日期：2020-04-01 00:00:00

abstract：:We examined the effects of pyrazoloacridine (PZA), an investigational anticancer agent in clinical trials, on cytotoxicity, DNA synthesis, and DNA damage in MCF-7 human breast carcinoma cells. With PZA concentrations ranging from 0.5 to 50 microM for durations of 3-72 hr, cytotoxicity increased in proportion to the to...

journal_title：Biochemical pharmacology

authors： Grem JL,Politi PM,Berg SL,Benchekroun NM,Patel M,Balis FM,Sinha BK,Dahut W,Allegra CJ

更新日期：1996-06-28 00:00:00

abstract：:Alcoholic ketoacidosis and diabetic ketoacidosis are life-threatening complications that share the characteristic features of high anion gap metabolic acidosis. Ketoacidosis is attributed in part to the massive release of ketone bodies (e.g., β-hydroxybutyrate; βOHB) from the liver into the systemic circulation. To da...

journal_title：Biochemical pharmacology

authors： Srinivasan MP,Shawky NM,Kaphalia BS,Thangaraju M,Segar L

更新日期：2019-02-01 00:00:00

abstract：:During attempts to isolate and identify an endogenous ligand for the glycoside binding sites on Na+,K+-ATPase, bovine adrenal glands were found to contain a potent inhibitor of isolated Na+,K+-ATPase. The inhibitory principle was extracted from adrenal cortex, following homogenization in NaHCO3 solution and separation...

journal_title：Biochemical pharmacology

authors： Ng YC,Akera T,Han CS,Braselton WE,Kennedy RH,Temma K,Brody TM,Sato PH

更新日期：1985-07-15 00:00:00

abstract：:To investigate the importance of NAD(P)H:quinone oxidoreductase 1 (or DT-diaphorase; NQO1) in the bioactivation of antitumor quinones, we established a series of stably transfected cell lines derived from BE human colon adenocarcinoma cells. BE cells have no NQO1 activity due to a genetic polymorphism. The new cell li...

journal_title：Biochemical pharmacology

authors： Winski SL,Swann E,Hargreaves RH,Dehn DL,Butler J,Moody CJ,Ross D

更新日期：2001-06-15 00:00:00

abstract：:A new analogue of methotrexate was synthesized from 4-amino-4-deoxy-N10-methylpteroic acid and D,L-homocysteic acid. The product (mAPA-HCysA) was bound tightly to L1210 mouse leukemia dihydrofolate reductase (IC50 = 1 nM), inhibited L1210 cell proliferation in culture (IC50 = 0.3 microM), and prolonged the survival of...

journal_title：Biochemical pharmacology

authors： Rosowsky A,Moran RG,Forsch R,Colman P,Uren J,Wick M

更新日期：1984-01-01 00:00:00

abstract：:We recently found that simvastatin can modulate the nuclear factor-kappaB (NF-kappaB) activation pathway, but whether other statins have similar effects to those of simvastatin is unknown. Therefore, we evaluated the effect six different statins on TNF-induced NF-kappaB activation in human myeloid leukemia cells. We t...

journal_title：Biochemical pharmacology

authors： Ahn KS,Sethi G,Aggarwal BB

更新日期：2008-02-15 00:00:00

abstract：:The murine Cyp2a-4 and Cyp2a-5 genes encode P450 isoforms catalysing testosterone 15 alpha-hydroxylase and coumarin 7-hydroxylase (COH) activities, respectively. Two days after the administration of a hepatotoxic dose of cerium chloride (2 mg/kg i.v.), COH activity was increased 3.2-fold in the liver of DBA/2 mice. Th...

journal_title：Biochemical pharmacology

authors： Salonpää P,Iscan M,Pasanen M,Arvela P,Pelkonen O,Raunio H

更新日期：1992-10-06 00:00:00

abstract：:BLT2, a low-affinity leukotriene B4 (LTB4) receptor, is a member of the G-protein coupled receptor (GPCR) family and is involved in the pathogenesis of inflammatory diseases such as asthma. Despite its clinical implications, however, no pharmacological inhibitors are available. In the present study, we screened for sm...

journal_title：Biochemical pharmacology

authors： Kim JY,Lee WK,Yu YG,Kim JH

更新日期：2010-05-15 00:00:00