Actions of epoxyeicosatrienoic acid on large-conductance Ca(2+)-activated K(+) channels in pituitary GH(3) cells.

abstract：:The peroxisome proliferator activated receptor-γ (PPAR-γ) is involved in the pathogenesis of diabetic retinopathy. Diabetic retinopathy is a preventable microvascular diabetic complication that damages human retinal pigment epithelial cells. Taurine is abundant in the fruit of Lycium barbarum (Goji Berry), and is repo...

journal_title：Biochemical pharmacology

authors： Song MK,Salam NK,Roufogalis BD,Huang TH

更新日期：2011-11-01 00:00:00

abstract：:Petrosaspongiolide M (PT) is a potent secretory phospholipase A(2) inhibitor and anti-inflammatory agent. This marine metabolite reduced the production of nitrite, prostaglandin E(2), and tumor necrosis factor-alpha in the mouse air pouch injected with zymosan. These effects were also observed in mouse peritoneal macr...

journal_title：Biochemical pharmacology

authors： Posadas I,Terencio MC,Randazzo A,Gomez-Paloma L,Payá M,Alcaraz MJ

更新日期：2003-03-01 00:00:00

abstract：:Ribonucleotide reductase (RNR), which consists of R1 and R2 subunits, catalyzes a key step of deoxyribonucleoside triphosphate (dNTP) synthesis for DNA replication and repair. The R2 subunit is controlled in a cell cycle-specific manner for timely DNA synthesis and is negatively regulated by p53 in response to DNA dam...

journal_title：Biochemical pharmacology

authors： Lin ZP,Belcourt MF,Carbone R,Eaton JS,Penketh PG,Shadel GS,Cory JG,Sartorelli AC

更新日期：2007-03-15 00:00:00

abstract：:Post-proline cleaving enzyme (PPCE) was purified from porcine kidney cytosol. The purified enzyme bound [125I-Tyr5]-bradykinin but neither [125I-Tyr1]-kallidin nor [125I-Tyr8]-bradykinin. Scatchard analysis of the data was consistent with a single class of binding sites with a Kassoc = 1.3 +/- 0.1 X 10(8) M-1. The opt...

journal_title：Biochemical pharmacology

authors： Odya CE,Dally RD,Georgiadis KE

更新日期：1987-01-01 00:00:00

abstract：:Membrane damage caused by phospholipase A action is thought to be an important factor in ischemic myocardial injury. Propranolol has been shown previously to have beneficial effects in both animal experiments and clinical trials, and it has membrane-stabilizing properties in vitro. To investigate the possibility that ...

journal_title：Biochemical pharmacology

authors： Trotz M,Jellison EJ,Hostetler KY

更新日期：1987-12-15 00:00:00

abstract：:The response and engagement of host normal tissues in malignant disease are major factors in therapeutic resistance. Physically, solid tumors have regions of hypoxia and acidosis. These physical stresses can lead to a more aggressive malignant phenotype through activation of HIF, GLUT-1, carbonic anhydrase IX, and sub...

journal_title：Biochemical pharmacology

authors： Teicher BA

更新日期：2009-06-01 00:00:00

abstract：:The interaction of the anti-tumor anthraquinones, ametantrone and mitoxantrone, with rat hepatic microsomes has been studied with a fluorescence technique using 7,12-dimethylbenzanthracene as a new fluorescent probe. The two drugs were able to quench the intrinsic fluorescence of microsomal suspension. Mitoxantrone wa...

journal_title：Biochemical pharmacology

authors： al-Gailany KA,Alwan AH

更新日期：1988-10-15 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：:4-S-Cysteaminylphenol (4-S-CAP) and the corresponding catechol 4-S-cysteaminylcatechol (4-S-CAC) have been evaluated for melanocytotoxicity. It was shown recently that tyrosinase oxidation of these substrates produces a violet pigment, dihydro-1,4-benzothiazine-6,7-dione (BQ). In this study we examined whether BQ is t...

journal_title：Biochemical pharmacology

authors： Hasegawa K,Ito S,Inoue S,Wakamatsu K,Ozeki H,Ishiguro I

更新日期：1997-05-15 00:00:00

abstract：:ERCC1 is a critical gene within the nucleotide excision repair pathway. Overexpression of ERCC1 through promoter-mediating transcriptional regulation is associated with repair of cisplatin-induced DNA damage and clinical resistance to platinum-chemotherapy. Several transcriptional repressors and activators within the ...

journal_title：Biochemical pharmacology

authors： Yan QW,Reed E,Zhong XS,Thornton K,Guo Y,Yu JJ

更新日期：2006-03-14 00:00:00

abstract：:Chronic blockade of nitric oxide (NO) synthesis attenuates the eosinophil infiltration into airways of allergic rats. This study was designed to investigate whether the inhibition of eosinophil influx to the lung of allergic rats reflects modifications in the pattern of cell mobilization from the bone marrow to periph...

journal_title：Biochemical pharmacology

authors： Ferreira HH,Costa RA,Jacheta JM,Martins AR,Medeiros MV,Macedo-Soares MF,De Luca IM,Antunes E,De Nucci G

更新日期：2004-08-15 00:00:00

abstract：:The tumor necrosis factor (TNF) superfamily (TNFSF) includes about thirty structurally related receptors (TNFSFRs) and about twenty protein ligands that bind to one or more of these receptors. Receptors of the tumor necrosis factor (TNF) superfamily (TNFSFRs) are pharmacological targets for treatment of inflammatory a...

journal_title：Biochemical pharmacology

authors： Platania CBM,Ronchetti S,Riccardi C,Migliorati G,Marchetti MC,Di Paola L,Lazzara F,Drago F,Salomone S,Bucolo C

更新日期：2020-08-01 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：:Stress, be it from environmental factors or intrinsic to the cell as result of growth and metabolism, can be harmful to cells. Mammalian cells have developed numerous mechanisms to respond to diverse forms of stress. These mechanisms combine signaling cascades and activation of gene expression programs to orchestrate ...

journal_title：Biochemical pharmacology

authors： Aramburu J,Drews-Elger K,Estrada-Gelonch A,Minguillón J,Morancho B,Santiago V,López-Rodríguez C

更新日期：2006-11-30 00:00:00

abstract：:S-Nitrosothiols, a class of NO donors, demonstrate potential benefits for cardiovascular diseases. Drugs for such chronic diseases require long term administration preferentially through the oral route. However, the absorption of S-nitrosothiols by the intestine, which is the first limiting barrier for their vascular ...

journal_title：Biochemical pharmacology

authors： Bonetti J,Zhou Y,Parent M,Clarot I,Yu H,Fries-Raeth I,Leroy P,Lartaud I,Gaucher C

更新日期：2018-09-01 00:00:00

abstract：:The nitroderivative 1-nitro-2-phenylethane (NPE) was recently described as a compound possessing heme-dependent soluble guanylyl cyclase (sGC) stimulating properties in vascular smooth muscle cells. In this study, we tested such pharmacological property of NPE in mice pancreatic acinar cells subjected to the bile salt...

journal_title：Biochemical pharmacology

authors： Cosker F,Lima FJ,Lahlou S,Magalhães PJ

更新日期：2014-09-15 00:00:00

abstract：:The effects of thiamine thiazolone (TT) and thiamine thiazolone pyrophosphate (TTPP) on the in vitro and in vivo inhibition of pyruvate dehydrogenase complex (PDHC) from rat cortex and hippocampus were characterized. TTPP decreased PDHC activity in vitro but had no effect in vivo following its direct chronic administr...

journal_title：Biochemical pharmacology

authors： Kandiko CT,Smith D,Yamamoto BK

更新日期：1988-11-15 00:00:00

abstract：:Cardioprotective effect of a free radical-scavenging compound (HO-3073) was examined during ischaemia-reperfusion (IR) in isolated heart perfusion system and its influence on the pro-survival Akt signalling pathway was addressed. Rat hearts were perfused according to the Langendorff method and subjected to a global 25...

journal_title：Biochemical pharmacology

authors： Toth A,Kovacs K,Deres P,Halmosi R,Czopf L,Hanto K,Kalai T,Hideg K,Sumegi B,Toth K

更新日期：2003-12-01 00:00:00

abstract：:In an effort to identify the human cytochromes P450 involved in the N-demethylation of dextromethorphan, the kinetics of 3-methoxymorphinan formation were studied in microsomal enzyme systems. Under initial rate conditions, 3-methoxymorphinan formation demonstrated single enzyme Michaelis-Menten kinetics using microso...

journal_title：Biochemical pharmacology

authors： Gorski JC,Jones DR,Wrighton SA,Hall SD

更新日期：1994-07-05 00:00:00

abstract：:Sulfasalazine (SF) promotes remyelination and improves the outcome of multiple sclerosis (MS) patients. However, the underlining mechanism remains elusive. Here, we examined whether SF blocks microglia switching to a pro-inflammatory M1-like phenotype through a competing endogenous RNA (ceRNA) effects in cuprizone-ind...

journal_title：Biochemical pharmacology

authors： Duan C,Liu Y,Li Y,Chen H,Liu X,Chen X,Yue J,Zhou X,Yang J

更新日期：2018-09-01 00:00:00

abstract：:Sublines of K562 human leukemia cells were selected for resistance (30- to 80-fold) to etoposide by continuous exposure to 0.5 microM VP-16. Two etoposide-resistant cell lines, K/VP.5 and K/VP.5-1, showed a 5-fold reduction in levels of topoisomerase II alpha protein compared with K562 cells. Northern analysis indicat...

journal_title：Biochemical pharmacology

authors： Ritke MK,Yalowich JC

更新日期：1993-12-03 00:00:00

abstract：:The antitumor, DNA-alkylating agent 1,3-bis[2-chloroethyl]-2-nitrosourea (BCNU; Carmustine), which generates 2-chloroethyl isocyanate upon decomposition in situ, inhibits cellular glutathione reductase (GR; EC 1.8.1.7) activity by up to 90% at pharmacological doses. GR is susceptible to attack from exogenous electroph...

journal_title：Biochemical pharmacology

authors： Rice KP,Penketh PG,Shyam K,Sartorelli AC

更新日期：2005-05-15 00:00:00

abstract：:Phenothiazines (PTZ) are drugs widely used in the treatment of schizophrenia. Trifluoperazine, a piperazinic PTZ derivative, has been described as inhibitor of the mitochondrial permeability transition (MPT). We reported previously the antioxidant activity of thioridazine at relatively low concentrations associated to...

journal_title：Biochemical pharmacology

authors： Cruz TS,Faria PA,Santana DP,Ferreira JC,Oliveira V,Nascimento OR,Cerchiaro G,Curti C,Nantes IL,Rodrigues T

更新日期：2010-10-15 00:00:00

abstract：:The aim of this work is the in vitro and ex vivo assessment of the leishmanicidal activity of camptothecin and three analogues used in cancer therapy: topotecan (Hycantim®), gimatecan (ST1481) and the pro-drug irinotecan (Camptosar®) as well as its active metabolite SN-38 against Leishmania infantum. The activity of c...

journal_title：Biochemical pharmacology

authors： Prada CF,Alvarez-Velilla R,Balaña-Fouce R,Prieto C,Calvo-Álvarez E,Escudero-Martínez JM,Requena JM,Ordóñez C,Desideri A,Pérez-Pertejo Y,Reguera RM

更新日期：2013-05-15 00:00:00

abstract：:Male ddY mice were given one injection of (1) mercury (mercuric chloride) simultaneously with various doses of selenium (sodium selenite), (2) mercury alone, or (3) various doses of selenium alone. The interaction between mercury and selenium in the liver and kidneys at 1, 5, 24, 120, and 240 hr after administration w...

journal_title：Biochemical pharmacology

authors： Yamamoto I

更新日期：1985-08-01 00:00:00

abstract：:Site-specific DNA cleavage in the presence of Cu(II) complexes of podophyllotoxin derivatives was investigated with a modified Sanger sequencing method. Cu(II) complexes of 4'-demethylepipodophyllotoxin (DEPD) and syringic acid (SA) cleaved M13mp18 single-strand DNA site-specifically at both cytosine (C) and guanine (...

journal_title：Biochemical pharmacology

authors： Yamashita A,Tawa R,Imakura Y,Lee KH,Sakurai H

更新日期：1994-05-18 00:00:00

abstract：:The signal transducer and activator of transcription 3 is a constitutively activated oncogenic protein in various human tumors and represents a valid target for anticancer drug design. In this study, we have achieved a new type of STAT3 inhibitors based on structural modifications on shikonin scaffold, guided by compu...

journal_title：Biochemical pharmacology

authors： Qiu HY,Fu JY,Yang MK,Han HW,Wang PF,Zhang YH,Lin HY,Tang CY,Qi JL,Yang RW,Wang XM,Zhu HL,Yang YH

更新日期：2017-12-15 00:00:00

abstract：:5-Substituted-2,2'-anhydrouridines are a new class of competitive inhibitors of uridine phosphorylase. The most potent member of the series is 2,2'-anhydro-5-ethyluridine with an apparent Ki value of 25 nM. These compounds are selective inhibitors of uridine phosphorylase and have no effect on thymidine phosphorylase....

journal_title：Biochemical pharmacology

authors： Veres Z,Szabolcs A,Szinai I,Dénes G,Kajtár-Peredy M,Otvös L

更新日期：1985-05-15 00:00:00

abstract：:Glutathione transferases are believed to play an important protective role in the various tissues of animals and man by catalysing the glutathione conjugation of electrophilic drugs and electrophilic drug metabolites. Many of these compounds have the potential to react with vital cellular macromolecules in the absence...

journal_title：Biochemical pharmacology

authors： Ahokas JT,Davies C,Ravenscroft PJ,Emmerson BT

更新日期：1984-06-15 00:00:00

abstract：:The plasma pharmacokinetics and urinary elimination of the enantiomers of indobufen (2-[p-(1-oxo-2-isoindolinyl)-phenyl]butyric acid), a novel platelet aggregation inhibitor, have been studied in male healthy volunteers given either the racemic compound or the S-enantiomer (200 mg racemate, 100 mg S-enantiomer). Enant...

journal_title：Biochemical pharmacology

authors： Strolm Benedetti M,Frigerio E,Tamassia V,Noseda G,Caldwell J

更新日期：1992-05-08 00:00:00