Mechanism of action of the nitrosoureas--IV. Synthesis of the 2-haloethylnitrosourea-induced DNA cross-link 1-(3-cytosinyl),2-(1-guanyl)ethane.

abstract：:Rat liver cells were separated into parenchymal cells (PC), Kupffer cells (KC) and endothelial cells (EC). The distribution of carboxylesterases (EC 3.1.1.1) between these cell types was investigated by PAGE and chromatogenic substrate staining, and compared with the results for total liver preparation and individual ...

journal_title：Biochemical pharmacology

authors： Gaustad R,Berg T,Fonnum F

更新日期：1992-08-18 00:00:00

abstract：:Interleukin-2 (IL-2) has been shown to decrease cytochrome P450 (CYP) mRNAs and proteins in cultured rat hepatocytes, and IL-2 administration decreases CYPs in rats. Although high doses of IL-2 are administered to cancer patients, the effect on human CYPs has not yet been determined. Patients with hepatic metastases f...

journal_title：Biochemical pharmacology

authors： Elkahwaji J,Robin MA,Berson A,Tinel M,Lettéron P,Labbe G,Beaune P,Elias D,Rougier P,Escudier B,Duvillard P,Pessayre D

更新日期：1999-04-15 00:00:00

abstract：:An Ehrlich ascites tumour cell line (EHR2) was selected for resistance to etoposide (VP16) by in vivo exposure to this agent. The resulting cell line (EHR2/VP16) was 114.3-, 5.7-, and 4.0-fold resistant to VP16, daunorubicin, and vincristine, respectively. The amount of salt-extractable immunoreactive topoisomerase II...

journal_title：Biochemical pharmacology

authors： Nielsen D,Maare C,Eriksen J,Litman T,Friche E,Skovsgaard T

更新日期：2000-08-01 00:00:00

abstract：:Evasion of cell death by overexpression of anti-apoptotic proteins, such as Bcl-2, is commonly observed in cancer cells leading to a lack of response to chemotherapy. Hence, there is a need to find new chemotherapeutic agents that are able to overcome chemoresistance mediated by Bcl-2 and to understand their mechanism...

journal_title：Biochemical pharmacology

authors： Hoffmann R,von Schwarzenberg K,López-Antón N,Rudy A,Wanner G,Dirsch VM,Vollmar AM

更新日期：2011-09-01 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：:The abilities of the naturally occurring polyamines, putrescine, spermidine and spermine, to affect variables related to the bioenergetic functions of isolated rat liver mitochondria were studied. At concentrations comparable to those present intracellularly, the polyamines inhibited state 4 respiration, but they had ...

journal_title：Biochemical pharmacology

authors： Byczkowski JZ,Zychlinski L,Porter CW

更新日期：1982-12-15 00:00:00

abstract：:"Are new neurons added in the adult mammalian brain?" "Do neural stem cells activate following CNS diseases?" "How can we modulate their activation to promote recovery?" Recent findings in the field provide novel insights for addressing these questions from a new perspective. In this review, we will summarize the curr...

journal_title：Biochemical pharmacology

authors： Pino A,Fumagalli G,Bifari F,Decimo I

更新日期：2017-10-01 00:00:00

abstract：:Ligand-receptor binding kinetics (i.e. association and dissociation rates) are emerging as important parameters for drug efficacy in vivo. Awareness of the kinetic behavior of endogenous ligands is pivotal, as drugs often have to compete with those. The binding kinetics of neurokinin 1 (NK1) receptor antagonists have ...

journal_title：Biochemical pharmacology

authors： Nederpelt I,Bleeker D,Tuijt B,IJzerman AP,Heitman LH

更新日期：2016-10-15 00:00:00

abstract：:L1210 and K562 leukaemic cells have been used to study the relationship between cytotoxicity and free radical production by two aziridinyl benzoquinones, 2,5-bis(carboethoxyamino)3,6-diaziridinyl-1,4-benzoquinone (AZQ) and 2,5-bis(2-hydroxyethylamino)-3,6-diaziridinyl-1,4-benzoquinone (BZQ). BZQ showed a high level of...

journal_title：Biochemical pharmacology

authors： Lea JS,Garner HJ,Butler J,Hoey BM,Ward TH

更新日期：1988-05-15 00:00:00

abstract：:Hep G2 cells, an established cell line derived from a human hepatoma, have retained a number of hepatocytic phase I and II reactions. The influence of picolines (2-, 3- and 4-methylpyridine), related compounds and some classical enzyme inducers on specific glutathione transferase (GST) activity and its subunit composi...

journal_title：Biochemical pharmacology

authors： Dierickx PJ

更新日期：1994-11-16 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：:Although there are a number of well-characterised animal models available for testing and comparing the efficacy of iron chelators, most are expensive to operate and are not capable of providing rapid and reproducible results. The method described herein is based on the labelling of rat liver with 59Fe using rat 59Fe-...

journal_title：Biochemical pharmacology

authors： Liu ZD,Lu SL,Hider RC

更新日期：1999-03-01 00:00:00

abstract：:The tissue distribution of captopril, an antihypertensive drug possessing a free sulfhydryl group, and its sulfur-conjugated metabolites was studied in rats by gas chromatography-mass spectrometry at 15, 30 and 60 min following a single 10 mg/kg oral dose of captopril. It was found that tissue accumulation of captopri...

journal_title：Biochemical pharmacology

authors： Drummer OH,Worland PJ,Jarrott B

更新日期：1983-05-15 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：:The effect of exhaustive exercise on the hepatobiliary transport of organic anions was investigated in rats. Animals were run on a rodent treadmill at 24 m/min up a 12% grade (152 +/- 15 min). Exercise resulted in significant hypoglycaemia (-46%) and increased plasma levels of lactate (+12%), together with a marked re...

journal_title：Biochemical pharmacology

authors： Villa JG,Collado PS,Almar MM,Gonzalez J

更新日期：1990-12-01 00:00:00

abstract：:Gram-negative bacilli have become increasingly resistant to antibiotics over the past 2 decades due to selective pressure from the extensive use of antibiotics in the hospital and community. In addition, these bacteria have made optimum use of their innate genetic capabilities to extensively mutate structural and regu...

journal_title：Biochemical pharmacology

authors： Gootz TD

更新日期：2006-03-30 00:00:00

abstract：:A set of sulfamides designed, synthesized and evaluated against maximal electroshock seizure (MES) and pentilenetetrazol (PTZ) tests with promising results, were tested for their affinity for the benzodiazepine binding site of the GABA(A) receptor. The most active compounds, N,N'-dicyclohexylsulfamide (7) and N,N'-dip...

journal_title：Biochemical pharmacology

authors： Wasowski C,Gavernet L,Barrios IA,Villalba ML,Pastore V,Samaja G,Enrique A,Bruno-Blanch LE,Marder M

更新日期：2012-01-15 00:00:00

abstract：:[[trans-PtCl(NH(3))(2)](2)mu-(trans-Pt(NH(3))(2)(H(2)N(CH(2))(6)-NH(2))(2))](4+) (BBR3464) is a cationic trinuclear platinum drug that is being evaluated in phase II clinical trials for treatment of lung and ovarian cancers. The structure and DNA binding profile of BBR3464 is different from drugs commonly used clinica...

journal_title：Biochemical pharmacology

authors： Kabolizadeh P,Ryan J,Farrell N

更新日期：2007-05-01 00:00:00

abstract：:Our results indicate that sex hormones play an important role in the regulation of brain and hepatic GST protein during maturity. The conjugating factor GSH does not appear to be under the influence of sex hormones. These observations are of great significance in view of the possibility of continued exposure to neurot...

journal_title：Biochemical pharmacology

authors： Das M,Agarwal AK,Seth PK

更新日期：1982-12-01 00:00:00

abstract：:The aim of this review is to summarize current available information about the role of PI3K/AKT/mTOR signaling in head and neck cancer as a potential target for new therapy options. 90% of all head and neck cancers are squamous cell carcinomas (HNSCC). The most common genetic alteration is inactivation of p16 gene whi...

journal_title：Biochemical pharmacology

authors： Marquard FE,Jücker M

更新日期：2020-02-01 00:00:00

abstract：:Dexamethasone and etoposide both induce apoptosis in immature rat thymocytes. We investigated the dependence of apoptosis on the phase of the cell cycle after incubation with these drugs. Cell cycle progression was followed by a combination of pulse labelling with 5-bromo-2'-deoxyuridine (BrdU), labelling fixed cells ...

journal_title：Biochemical pharmacology

authors： Fearnhead HO,Chwalinski M,Snowden RT,Ormerod MG,Cohen GM

更新日期：1994-09-15 00:00:00

abstract：:The present study was undertaken to investigate a mechanism of the inhibitory effect of vitamin E in urethane-induced lung tumorigenesis in mice. We assayed ornithine decarboxylase (ODC) activity and the prostaglandin E2 (PGE2) level in lung at 8 weeks after urethane injection (promotion phase). Excessive vitamin E fe...

journal_title：Biochemical pharmacology

authors： Yano T,Yano Y,Uchida M,Murakami A,Hagiwara K,Otani S,Ichikawa T

更新日期：1997-06-01 00:00:00

abstract：:In addition to the established control of acid secretion of the class of proton pump inhibitors (PPI) reactivity from the pyridyl methyl sulphinyl benzimidazole type a second independent anti-inflammatory reactivity was observed in vitro. This inhibitory reactivity was clearly noticed using three different assays wher...

journal_title：Biochemical pharmacology

authors： Simon WA,Sturm E,Hartmann HJ,Weser U

更新日期：2006-04-28 00:00:00

abstract：:A series of fucoidan [sulfated poly(L-fucopyranose)] derivatives were prepared by chemical sulfation and desulfation, and they were tested for their abilities to stimulate tissue plasminogen activator (t-PA)-catalyzed plasminogen activation, clot lysis, and the inhibition of fibrin polymer formation. The magnitude of ...

journal_title：Biochemical pharmacology

authors： Soeda S,Sakaguchi S,Shimeno H,Nagamatsu A

更新日期：1992-04-15 00:00:00

abstract：:CYP2C19 (formerly known as CYP2C75), highly homologous to human CYP2C19, has been identified in cynomolgus and rhesus macaques, non-human primate species widely used in drug metabolism studies. CYP2C19 is predominantly expressed in liver and encodes a functional drug-metabolizing enzyme. Genetic variants in human CYP2...

journal_title：Biochemical pharmacology

authors： Uno Y,Matsushita A,Shukuya M,Matsumoto Y,Murayama N,Yamazaki H

更新日期：2014-09-15 00:00:00

abstract：:The effects of schisanhenol (Sal) on Adriamycin (ADM)-induced rat heart mitochondrial toxicity in vitro were investigated. Malondialdehyde formation, lysis, disintegration and membrane rigidification in mitochondria treated with ADM were reduced significantly by Sal. In the electron spin resonance studies, Sal did not...

journal_title：Biochemical pharmacology

authors： Lin TJ,Liu GT,Pan Y,Liu Y,Xu GZ

更新日期：1991-10-09 00:00:00

abstract：:Tumor-induced neoangiogenesis is an essential event for solid tumor growth. Therefore, a compound able to block angiogenesis-promoting factors could have antitumor activity. The polysulfonated naphthylurea suramin is hypothesized to have this mode of action. A series of sulfonated distamycin A derivatives have been sy...

journal_title：Biochemical pharmacology

authors： Ciomei M,Pastori W,Mariani M,Sola F,Grandi M,Mongelli N

更新日期：1994-01-20 00:00:00

abstract：:Mastoparan, a polypeptide known to activate heterotrimeric GTP-binding proteins, enhances the transport of Ca2+ and K+ across membranes. In the present study we investigated the influence of mastoparan on transepithelial resistance (TER) and on short circuit current (SCC) of the intestinal cell line T84. Mastoparan de...

journal_title：Biochemical pharmacology

authors： Blumenstein I,Gerhard R,Ries J,Kottra G,Stein J

更新日期：2003-04-01 00:00:00

abstract：:Human ABCG2 is a plasma membrane glycoprotein that provides physiological protection against xenobiotics. ABCG2 also significantly influences biodistribution of drugs through pharmacological tissue barriers and confers multidrug resistance to cancer cells. Moreover, ABCG2 is the molecular determinant of the side popul...

journal_title：Biochemical pharmacology

authors： Hegedüs C,Truta-Feles K,Antalffy G,Várady G,Német K,Ozvegy-Laczka C,Kéri G,Orfi L,Szakács G,Settleman J,Váradi A,Sarkadi B

更新日期：2012-08-01 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