Discovery of substituted sulfonamides and thiazolidin-4-one derivatives as agonists of human constitutive androstane receptor.

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：:EM012, a semisynthetic phthalideisoquinoline alkaloid, has been recently found to target microtubules and possess anti-cancer activity. In this study, we evaluated the effects of EM012 in combination with the classic microtubule-targeting agent paclitaxel. Our results demonstrated that EM012 enhanced the anti-prolifer...

journal_title：Biochemical pharmacology

authors： Zhou J,Liu M,Aneja R,Chandra R,Joshi HC

更新日期：2004-12-15 00:00:00

abstract：:The effects of the enantiomers of 2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]-sulfinyl ]- 1H-benzimidazole (lansoprazole, AG-1749) on acid formation in isolated canine parietal cells and (H+ + K+)-ATPase activity in canine gastric microsomes were investigated. Both the (+)-and the (-)-enantiomer of lanso...

journal_title：Biochemical pharmacology

authors： Nagaya H,Inatomi N,Nohara A,Satoh H

更新日期：1991-10-24 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：:The interactions of the anticonvulsant drug milacemide (2-n-pentylaminoacetamide) with rat liver mitochondrial monoamine oxidases-A and -B have been studied. The compound acts as a substrate for the B-form of the enzyme, with an apparent Km value of 49 +/- 4.7 microM and a Vmax value of 1.1 +/- 0.2 nmol/min/mg. It is ...

journal_title：Biochemical pharmacology

authors： O'Brien EM,Tipton KF,McCrodden JM,Youdim MB

更新日期：1994-02-11 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：:Growing evidence suggests that hepatic-insulin resistance is sufficient to promote progression to cardiovascular disease. We have shown previously that liver-specific protein-tyrosine-phosphatase 1B (PTP1B) deficiency improves hepatic-insulin sensitivity and whole-body glucose homeostasis. The aim of this study was to...

journal_title：Biochemical pharmacology

authors： Agouni A,Tual-Chalot S,Chalopin M,Duluc L,Mody N,Martinez MC,Andriantsitohaina R,Delibegović M

更新日期：2014-12-15 00:00:00

abstract：:A large variety of 5-substituted 2'deoxyuridines (dUrds) and 2'-deoxyuridylates (dUMPs) have been evaluated for their inhibitory effects on the thymidine (dThd) kinase or thymidylate (dTMP) synthetase isolated from mouse leukemia L1210 cells. The most potent inhibitors of dThd kinase were 5-chloro-, 5-bromo- and 5-iod...

journal_title：Biochemical pharmacology

authors： Balzarini J,De Clercq E,Mertes MP,Shugar D,Torrence PF

更新日期：1982-11-15 00:00:00

abstract：:The alcohol-avoiding ANA (Alko, Non-Alcohol) and alcohol-preferring AA (Alko, Alcohol) rat lines are known to differ in their acetaldehyde metabolism and were originally found to differ in hepatic alcohol dehydrogenase (ADH) and aldehyde dehydrogenase (ALDH) activities in the 1970s. At the beginning of the 1980s, thes...

journal_title：Biochemical pharmacology

authors： Koivisto T,Eriksson CJ

更新日期：1994-10-18 00:00:00

abstract：:Reactive oxygen species (ROS) attack guanine bases in DNA and form 8-hydroxydeoxyguanosine (8-OHdG), which has been regarded simply as an oxidative mutagenic by-product. On the other hand, our previous report showed paradoxically ROS attenuating action of generated 8-OHdG. In the current study, both in vitro and in vi...

journal_title：Biochemical pharmacology

authors： Ock CY,Hong KS,Choi KS,Chung MH,Kim Ys,Kim JH,Hahm KB

更新日期：2011-01-01 00:00:00

abstract：:The binding of [3H]nitrendipine to rat cortical membranes was reduced by phenytoin, phenobarbital, and pentobarbital. The IC50 values were 0.09, 0.40, and 0.76 mM respectively. The drugs reduced the apparent binding affinity of [3H]nitrendipine with little effect on the maximum number of binding sites. The inhibitory ...

journal_title：Biochemical pharmacology

authors： Harris RA,Jones SB,Bruno P,Bylund DB

更新日期：1985-06-15 00:00:00

abstract：:We have demonstrated earlier that a secreted fibroblast growth factor-binding protein (FGF-BP) can enhance angiogenesis and promote tumor growth in vivo. Furthermore, we found that FGF-BP expression in squamous cell carcinoma (SCC) is reduced by concentrations of retinoids that are effective in the treatment of SCC an...

journal_title：Biochemical pharmacology

authors： Boyle BJ,Harris VK,Liaudet-Coopman ED,Riegel AT,Wellstein A

更新日期：2000-12-01 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：:B-Raf kinase is the key point in a main branch of mitogen-activated protein kinase pathways and some of its mutations, such as the V600E mutation, lead to the persistent activation of ERK signaling and the trigger of severe diseases, including melanoma and other somatic cancers. Several potent drugs have been approved...

journal_title：Biochemical pharmacology

authors： Wang PF,Qiu HY,Wang ZF,Zhang YJ,Wang ZC,Li DD,Zhu HL

更新日期：2017-05-15 00:00:00

abstract：:Milacemide (CP 1552 S, 2-n-pentylaminoacetamide), a drug with anti-epileptic potency, increases the gamma-aminobutyric acid (GABA) content specifically in the substantia nigra of rat brain. The effect is dose-related from 25 to 100 mg/kg p.o. The time course shows that at 100 mg/kg p.o. after 2, 3 and 4 hr the substan...

journal_title：Biochemical pharmacology

authors： de Varebeke PJ,Niebes P,Pauwels G,Roba J,Korf J

更新日期：1983-09-15 00:00:00

abstract：:The study of binding is not an easy task especially because of the difficulty of interpreting the results in terms of binding on specific receptor sites. The problem is not new; what is new is the increasing amount of fanciful interpretation that such a technique has generated. The tendency to interpret anomalous or i...

journal_title：Biochemical pharmacology

authors： Laduron PM

更新日期：1984-03-15 00:00:00

abstract：:Nonsteroidal anti-inflammatory drugs (NSAIDs) are now understood to fall into one of two agent classes in clinical use. Traditional NSAIDs inhibit both cyclooxygenases-1 and 2 (COX-1, 2), which act as key enzymes catalyzing the same reaction in the production of prostaglandins (PGs), while the second class of NSAIDs s...

journal_title：Biochemical pharmacology

authors： Imanishi J,Morita Y,Yoshimi E,Kuroda K,Masunaga T,Yamagami K,Kuno M,Hamachi E,Aoki S,Takahashi F,Nakamura K,Miyata S,Ohkubo Y,Mutoh S

更新日期：2011-10-01 00:00:00

abstract：:The seminal vesicle protein No. 4 (SV-IV) secreted from the rat seminal vesicle epithelium, possesses immunosuppressive and anti-inflammatory properties and it is a potent inhibitor of platelet aggregation both in vivo and in vitro. This research aimed to investigate the possible effect of SV-IV on the process of huma...

journal_title：Biochemical pharmacology

authors： Di Micco B,Colonna G,Porta R,Metafora S

更新日期：1994-07-19 00:00:00

abstract：:Several aspects of the effects of zinc on the metabolism of glutathione were examined in the Chinese hamster cell (line CHO) and in three derived sublines which differ in their resistance to the thiol reactive heavy metal cadmium. In the parental CHO cell, which does not induce the synthesis of metallothionein in resp...

journal_title：Biochemical pharmacology

authors： Seagrave J,Tobey RA,Hildebrand CE

更新日期：1983-10-15 00:00:00

abstract：:The effect of ethanol abuse on the lipid ordering of the human erythrocyte membranes was studied by steady-state and time-resolved fluorescence anisotropy measurements of DPH and its polar analogue TMA-DPH, which probe different membrane regions. Steady-state anisotropy values with DPH as a probe were slightly but sig...

journal_title：Biochemical pharmacology

authors： Beaugé F,Gallay J,Stibler H,Borg S

更新日期：1988-10-15 00:00:00

abstract：:As our knowledge on the mechanisms that control cell function increases, more complex signaling pathways and quite intricate cross-talks among regulatory proteins are discovered. Establishing accurate interactions between cellular networks is essential for a healthy cell and different alterations in signaling are know...

journal_title：Biochemical pharmacology

authors： Gomez-Duran A,Carvajal-Gonzalez JM,Mulero-Navarro S,Santiago-Josefat B,Puga A,Fernandez-Salguero PM

更新日期：2009-02-15 00:00:00

abstract：:This Festschrift contribution summarizes the perspectives of two of David Triggle's graduate students. Both share somewhat parallel scientific and career paths-i.e., enrolling in the Biochemical Pharmacology program at the University of Buffalo, pursuing graduate training under the mentorship of David Triggle and subs...

journal_title：Biochemical pharmacology

authors： Rampe D,Gopalakrishnan M

更新日期：2015-11-15 00:00:00

abstract：:Naturally soluble rat germ cell adenylate cyclase was inhibited by adenosine and the adenosine analogs, 9-beta-D-arabinofuranosyl adenine (AFA) and 2',5'-dideoxyadenosine (DDA), all of which inhibited hormone-sensitive adenylate cyclases at the "P" site. The IC50 values for adenosine and DDA were approximately 0.1 and...

journal_title：Biochemical pharmacology

authors： Onoda JM,Braun T,Wrenn SM Jr

更新日期：1987-06-15 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：: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：:Cytogenetic lesions often alter kinase signaling in acute myeloid leukemia (AML) and the addition of kinase inhibitors to the treatment arsenal is of interest. We have screened a kinase inhibitor library and performed combination testing to find promising drug-combinations for synergistic killing of AML cells. Cytotox...

journal_title：Biochemical pharmacology

authors： Österroos A,Kashif M,Haglund C,Blom K,Höglund M,Andersson C,Gustafsson MG,Eriksson A,Larsson R

更新日期：2016-10-15 00:00:00

abstract：:Salinomycin, a polyether antibiotic, acts as a highly selective potassium ionophore and has anticancer activity on various cancer cell lines. Cisplatin has been proved as chemotherapy drug for advanced human non-small cell lung cancer (NSCLC). Thymidylate synthase (TS) is a key enzyme in the pyrimidine salvage pathway...

journal_title：Biochemical pharmacology

authors： Ko JC,Zheng HY,Chen WC,Peng YS,Wu CH,Wei CL,Chen JC,Lin YW

更新日期：2016-12-15 00:00:00

abstract：:Autophagy is generally regarded as a mechanism to promote cell survival. However, autophagy can occasionally be the mechanism responsible of cell demise. We have found that a concomitant depletion of glucose, nutrients and growth factors provoked cell death in a variety of cell lines. This death process was contingent...

journal_title：Biochemical pharmacology

authors： Mattiolo P,Yuste VJ,Boix J,Ribas J

更新日期：2015-12-15 00:00:00

abstract：:Stimulated mast cells produce and release adenosine, and the release of mast cell mediators is potentiated by adenosine, yet very little is known regarding mast cell purine metabolism. Because 5-amino-4-imidazolecarboxamide riboside (AICA riboside) has been shown to alter adenosine metabolism and accelerate the replet...

journal_title：Biochemical pharmacology

authors： Marquardt DL,Gruber HE

更新日期：1986-12-15 00:00:00

abstract：:The biological effects of 1-methyl-2-nitrosoimidazole (INO), the 2 electron reduction product of biologically active 1-methyl-2-nitroimidazole, were examined in HT-29 human colon cancer cells by clonogenic assay and glutathione (GSH) determination. INO was very toxic towards HT-29 cells and was equally toxic under aer...

journal_title：Biochemical pharmacology

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

更新日期：1989-05-15 00:00:00