Diacylglycerol kinase inhibitor, R59022, potentiates neutrophil oxidase activation by Ca2+-dependent stimuli. Evidence for two separate but convergent pathways.

abstract：:DNA-dependent protein kinase (DNA-PK) plays a key role in repair of radiation-induced DNA double strand breaks (DSB) by non-homologous end-joining. DNA-PK inhibitors (DNA-PKi) are therefore efficient radiosensitisers, but normal tissue radiosensitisation represents a risk for their use in radiation oncology. Here we d...

journal_title：Biochemical pharmacology

authors： Wong WW,Jackson RK,Liew LP,Dickson BD,Cheng GJ,Lipert B,Gu Y,Hunter FW,Wilson WR,Hay MP

更新日期：2019-11-01 00:00:00

abstract：:Vindesine biotransformation was investigated using a bank of human liver microsomes. The drug was converted into one major metabolite (M) upon incubation with the microsomes. Large interindividual variations were observed: vindesine biotransformation rates ranged from 1.2 to 12.9 pmol/min/mg protein. Vindesine metabol...

journal_title：Biochemical pharmacology

authors： Zhou XJ,Zhou-Pan XR,Gauthier T,Placidi M,Maurel P,Rahmani R

更新日期：1993-02-24 00:00:00

abstract：:DNA methylation is a mammalian epigenetic mark that participates to define where and when genes are expressed, both in normal cells and in the context of diseases. Like other epigenetic marks, it is reversible and can be modulated by chemical agents. Because it plays an important role in cancer by silencing certain ge...

journal_title：Biochemical pharmacology

authors： Pechalrieu D,Etievant C,Arimondo PB

更新日期：2017-04-01 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：:Chlorzoxazone is mainly metabolized to 6-hydroxychloroxazone (6-OHchlorzoxazone) by the ethanol-inducible cytochrome P450 2E1 (CYP2E1). To evaluate the impact of ethanol consumption on the enzyme induction, the pharmacokinetics of chlorozoxazone and 6-OHchlorzoxazone were studied in alcoholic and control subjects. Fif...

journal_title：Biochemical pharmacology

authors： Girre C,Lucas D,Hispard E,Menez C,Dally S,Menez JF

更新日期：1994-04-29 00:00:00

abstract：:Oxyntomodulin (Oxm) is a hormone which has been shown to exhibit a range of potentially beneficial actions for alleviation of obesity-diabetes. However, exploitation of Oxm-based therapies has been severely restricted due to degradation by the enzyme dipeptidylpeptidase-IV (DPP-IV). Thus, the aim of this study was to ...

journal_title：Biochemical pharmacology

authors： Kerr BD,Flatt PR,Gault VA

更新日期：2010-12-01 00:00:00

abstract：:The homomeric α7 nicotinic acetylcholine receptor is a well-studied therapeutic target, though its characteristically rapid desensitization complicates the development of drugs with specific agonist effects. Moreover, some experimental compounds such as GTS-21 (2,4diMeOBA), a derivative of the α7-selective partial ago...

journal_title：Biochemical pharmacology

authors： Isaacson MD,Horenstein NA,Stokes C,Kem WR,Papke RL

更新日期：2013-03-15 00:00:00

abstract：:The addition of agents, such as tumor necrosis factor-alpha, to human peripheral neutrophils (HPPMN) induces priming, which enhances the receptor-mediated superoxide (O2-) generation and tyrosine phosphorylation of several HPPMN proteins. Lidocaine, a local anesthetic, inhibited both enhanced O2- generation and tyrosi...

journal_title：Biochemical pharmacology

authors： Kanbara T,Tomoda MK,Sato EF,Ueda W,Manabe M

更新日期：1993-04-22 00:00:00

abstract：:Adherence of Plasmodium falciparum-infected erythrocytes (IE) to the venular endothelium in brain and other organs is characteristic of cerebral malaria, an often fatal complication in infected individuals. It has been shown that cytoadherence may be mediated through interaction of IE with glycoproteins on host target...

journal_title：Biochemical pharmacology

authors： Wright PS,Cross-Doersen DE,Schroeder KK,Bowlin TL,McCann PP,Bitonti AJ

更新日期：1991-06-15 00:00:00

abstract：:The microsomal brush-border fraction of rat renal tissue contains enzymatic activity, optimally active at pH 9, that is capable of degrading human myelin basic protein (BP) peptide 43-88. In the present study, this degradation and the effect on it of selected drugs and hormones were examined further. Of the substances...

journal_title：Biochemical pharmacology

authors： Trestman RL,Heinemann MA,Whitaker JN,Seyer JM

更新日期：1985-04-15 00:00:00

abstract：:Phosphodiesterase inhibitors were used as a tool to manipulate cellular nucleotide levels in vitro and in vivo. The lipopolysaccharide (LPS)-induced release of tumor necrosis factor alpha (TNF-alpha) from mouse peritoneal macrophages was inhibited by prostaglandin E2 with an IC50 of 0.05 microM and by dibutyryl-cAMP w...

journal_title：Biochemical pharmacology

authors： Fischer W,Schudt C,Wendel A

更新日期：1993-06-22 00:00:00

abstract：:We tested the influence of IFNgamma on proteasome activity in parental Hep G2 cells that do not metabolize ethanol, as well as in recombinant Hep G2-derived cells that express either or both alcohol dehydrogenase (ADH) and cytochrome P4502E1 (CYP2E1). IFNgamma treatment increased proteasome activity in VL-17A (ADH(+),...

journal_title：Biochemical pharmacology

authors： Osna NA,Clemens DL,Donohue TM Jr

更新日期：2003-09-01 00:00:00

abstract：:Tenofovir alafenamide (TAF) can be considered a new prodrug of tenofovir (TFV), as successor of tenofovir disoproxil fumarate (TDF). It is in vivo as potent against human immunodeficiency virus (HIV) at a 30-fold lower dose (10mg) than TDF (300mg). TAF has been approved in November 2015 (in the US and EU), as a single...

journal_title：Biochemical pharmacology

authors： De Clercq E

更新日期：2016-11-01 00:00:00

abstract：:Son of Sevenless (SOS) was discovered in Drosophila melanogaster. Essential for normal eye development in Drosophila, SOS has two human homologues, SOS1 and SOS2. The SOS1 gene encodes the Son of Sevenless 1 protein, a Ras and Rac guanine nucleotide exchange factor. This protein is composed of several important domain...

journal_title：Biochemical pharmacology

authors： Pierre S,Bats AS,Coumoul X

更新日期：2011-11-01 00:00:00

abstract：:MRP1 overexpression in multidrug-resistant cancer cells has been shown to be responsible for collateral sensitivity to some flavonoids that stimulate a huge MRP1-mediated GSH efflux. This massive GSH depletion triggers the death of these cancer cells. We describe here that bivalent flavonoid dimers strikingly stimulat...

journal_title：Biochemical pharmacology

authors： Dury L,Nasr R,Lorendeau D,Comsa E,Wong I,Zhu X,Chan KF,Chan TH,Chow L,Falson P,Di Pietro A,Baubichon-Cortay H

更新日期：2017-01-15 00:00:00

abstract：:Anticholinesterases (anti-ChE) have some effects on biological properties including behavior, vision, and electroencephalograms, which are often long lasting and which do not appear to be due to cholinesterase (ChE; EC 3.1.1.7) inhibition, but which may be due to alterations in the organization and/or functioning of t...

journal_title：Biochemical pharmacology

authors： Schupper H,Rosenberg P

更新日期：1991-09-12 00:00:00

abstract：:Continuous in vitro cultivation of human lymphoid H9 cells in the presence of 0.5microM arabinosyl-cytosine (araC) resulted in cell variant, H9-araC cells, that was >600-fold resistant to the drug and cross resistant to its analogs and other unrelated nucleosides, e.g. dideoxycytidine (5-fold), thiacytidine (2-fold), ...

journal_title：Biochemical pharmacology

authors： Sarkar M,Han T,Damaraju V,Carpenter P,Cass CE,Agarwal RP

更新日期：2005-08-01 00:00:00

abstract：:It was shown previously that three 1,5-diazabicyclo[3.1.0]hexane-2,4-diones selectively inhibited human Type II IMP dehydrogenase (IMPDH) from Tmolt4 cell leukemia [Barnes et al., Biochemistry 2000;39:13641-50]. The agents acted as competitive inhibitors of this isoform, yet when tested against human Type I at concent...

journal_title：Biochemical pharmacology

authors： Barnes BJ,Eakin AE,Izydore RA,Hall IH

更新日期：2001-07-01 00:00:00

abstract：:Bradykinin (BK) induces inflammation in rheumatoid arthritis (RA). Resveratrol is a potent activator of Sirt1 which could modulate inflammation through deacetylating histones of transcription factors. Here, we investigated the mechanisms underlying BK-induced COX-2 expression which is modulated by resveratrol/Sirt1 in...

journal_title：Biochemical pharmacology

authors： Yang CM,Chen YW,Chi PL,Lin CC,Hsiao LD

更新日期：2017-05-15 00:00:00

abstract：:A series of N-hydroxy-N'-aminoguanidine derivatives was studied for their effects on L1210 cell growth and ribonucleotide reductase activity. With the twelve compounds studied, there was a good correlation between the inhibition of L1210 cell growth and the inhibition of ribonucleotide reductase activity. The most pot...

journal_title：Biochemical pharmacology

authors： Cory JG,Carter GL,Bacon PE,T'ang A,Lien EJ

更新日期：1985-08-01 00:00:00

abstract：:Lipoxygenase products, which are formed in great amounts in platelets during their activation, have been prepared from arachidonic acid (20:4n-6), the main polyunsaturated fatty acid (PUFA) esterified in platelet phospholipids, and from two major PUFAs of fish fat, eicosapentaenoic (20:5n-3) and docosahexaenoic (22:6n...

journal_title：Biochemical pharmacology

authors： Croset M,Sala A,Folco G,Lagarde M

更新日期：1988-04-01 00:00:00

abstract：:Duration of gene silencing due to the short-term silencing effects induced by exogenous siRNA have limited the therapeutic applications of RNAi and the development of RNAi-based therapeutics. We here generated Eg5 shRNA-expressing plasmids using the inverted terminal repeats (ITRs) sequences to produce Eg5 hairpin RNA...

journal_title：Biochemical pharmacology

authors： Seraj S,Lee J,Ahn HJ

更新日期：2019-08-01 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：:Adenosine (Ado, 10 microM) did not inhibit ADP-induced human platelet aggregation in whole blood. However, if the blood was preincubated with dipyridamole (10 microM), a potent inhibitor of the erythrocytic nucleoside transport system (NTS), Ado acted as a strong inhibitor of platelet aggregation. Similarly, Ado inhib...

journal_title：Biochemical pharmacology

authors： Dawicki DD,Agarwal KC,Parks RE Jr

更新日期：1985-11-15 00:00:00

abstract：:Chemosensitization of bifunctional alkylators by misonidazole (MISO) and related nitroimidazoles in vitro has been shown to require hypoxic exposures. Presumably, reductive metabolism of the nitroimidazole under hypoxic conditions results in generation of a chemosensitizing intermediate(s) in a manner analogous to tha...

journal_title：Biochemical pharmacology

authors： Mulcahy RT,Gipp JJ,Ublacker GA,McClelland RA

更新日期：1990-12-15 00:00:00

abstract：:The effects on metabolism of the fluorinated dicarboxylic acid, perfluorosuccinate, were examined in hepatocytes from fasted rats. Perfluorosuccinate (5 mM) inhibited gluconeogenesis from lactate by 80% and from pyruvate by 40%. Significant inhibition (up to 30%) occurred at a concentration of perfluorosuccinate of 50...

journal_title：Biochemical pharmacology

authors： Gregory RB,Berry MN

更新日期：1989-09-01 00:00:00

abstract：:Vinca alkaloids are clinically used to inhibit the growth of malignancy by interfering with microtubule polymerization. The purpose of this study was to identify the molecular mechanisms underlying growth inhibition as well as apoptosis in vinca alkaloid-treated lung adenocarcinoma cells. Consistent with nocodazole, t...

journal_title：Biochemical pharmacology

authors： Chiu WH,Luo SJ,Chen CL,Cheng JH,Hsieh CY,Wang CY,Huang WC,Su WC,Lin CF

更新日期：2012-05-01 00:00:00

abstract：:This study reports an investigation on the effect of the seleno-organic compound ebselen on rat liver mitochondria. We show that low concentrations of ebselen induced an increase in rat liver mitochondrial membrane permeability, resulting in swelling and loss of membrane potential. These effects were mediated by the o...

journal_title：Biochemical pharmacology

authors： Morin D,Zini R,Ligeret H,Neckameyer W,Labidalle S,Tillement JP

更新日期：2003-05-15 00:00:00

abstract：:Pretreatment of NG108-15 cells with 0.03-25 microM prostaglandin E1 (PGE1) produced decreases in the maximal stimulation of adenylate cyclase activity produced by iloprost, N-ethylcarboxamidoadenosine and sodium fluoride. The rate of desensitization to all three agents was dependent on the concentration of PGE1 used, ...

journal_title：Biochemical pharmacology

authors： Krane A,MacDermot J,Keen M

更新日期：1994-03-15 00:00:00

abstract：:The metabolism of mitozantrone, a chemotherapeutic agent used in the treatment of breast cancer, has been studied in vitro using rat liver subcellular fractions. This compound would appear to be metabolized by two interesting pathways. One involves conjugation with glucuronic acid, catalyzed most effectively by a 3-me...

journal_title：Biochemical pharmacology

authors： Wolf CR,Macpherson JS,Smyth JF

更新日期：1986-05-01 00:00:00