abstract：:Increasing evidence is accumulating that zoledronic acid (ZOL), a nitrogen-containing bisphosphonate (N-BP), is able to affect tumor cells by inhibiting the enzyme farnesyl pyrophosphate synthase (FPPS) in the mevalonate pathway (MVP). The consequent accumulation of unprenylated proteins is believed to largely account...

journal_title：Biochemical pharmacology

authors： Räikkönen J,Mönkkönen H,Auriola S,Mönkkönen J

更新日期：2010-03-01 00:00:00

abstract：:We have investigated the ability of certain dietary flavonoids, known to exert beneficial effects on the central nervous system, to affect neuronal apoptosis. We used cerebellar granule cells undergoing apoptosis due to potassium deprivation in a serum-free medium in either the absence or presence of the flavonoids ge...

journal_title：Biochemical pharmacology

authors： Atlante A,Bobba A,Paventi G,Pizzuto R,Passarella S

更新日期：2010-03-01 00:00:00

abstract：:Macrophages are key inflammatory cells in chronic obstructive pulmonary disease (COPD). The pathophysiology of cigarette smoke-induced lung emphysema is complex but there is a clear role for reactive oxygen species (ROS, such as peroxynitrite), tumor necrosis factor (TNF-alpha) and interleukin (IL)-8. We investigated ...

journal_title：Biochemical pharmacology

authors： Sarir H,Mortaz E,Janse WT,Givi ME,Nijkamp FP,Folkerts G

更新日期：2010-03-01 00:00:00

abstract：:To investigate the potential interactions between the angiotensin II (Ang II) and insulin signaling systems, regulation of IRS-1 phosphorylation and insulin-induced Akt activation by Ang II were examined in clone 9 (C9) hepatocytes. In these cells, Ang II specifically inhibited activation of insulin-induced Akt Thr(30...

journal_title：Biochemical pharmacology

authors： Arellano-Plancarte A,Hernandez-Aranda J,Catt KJ,Olivares-Reyes JA

更新日期：2010-03-01 00:00:00

abstract：BACKGROUND/AIMS:Carnitine palmitoyl-transferase I (CPT I) catalyses the synthesis of long-chain (LC)-acylcarnitines from LC-acyl-CoA esters. It is the rate-limiting enzyme of mitochondrial fatty acid beta-oxidation (FAO) pathway and its activity is regulated by malonyl-CoA. The antiepileptic drug valproic acid (VPA) is...

journal_title：Biochemical pharmacology

authors： Aires CC,Ijlst L,Stet F,Prip-Buus C,de Almeida IT,Duran M,Wanders RJ,Silva MF

更新日期：2010-03-01 00:00:00

abstract：:The aspirin esterase activity of human plasma is due to butyrylcholinesterase and albumin. Our goal was to identify the amino acid residues involved in the aspirin esterase activity of albumin. Fatty acid-free human albumin and human plasma were treated with aspirin for 5 min-24 h. Acetylated residues were identified ...

journal_title：Biochemical pharmacology

authors： Liyasova MS,Schopfer LM,Lockridge O

更新日期：2010-03-01 00:00:00

abstract：:Nephrotoxicity due to renal proximal tubule accumulation of aminoglycoside (AG) antibiotics, such as gentamicin, represents a major clinical problem. Receptor-mediated endocytosis via the multi-ligand receptor megalin is thought to be a key mechanism in the cellular uptake of AGs and nephrotoxicity. This process can b...

journal_title：Biochemical pharmacology

authors： Antoine DJ,Srivastava A,Pirmohamed M,Park BK

更新日期：2010-02-15 00:00:00

abstract：:The abundance of human equilibrative nucleoside transporter 1 (hENT1) has recently been shown to be a predictive marker of benefit from gemcitabine therapy in patients with pancreatic cancer. Since hENT1 is also important for the uptake of positron emission tomography (PET) tracer 3'-deoxy-3'-fluorothymidine (FLT) in ...

journal_title：Biochemical pharmacology

authors： Paproski RJ,Young JD,Cass CE

更新日期：2010-02-15 00:00:00

abstract：:Despite the substantial progress made in understanding initiation expression of the MOR gene in lymphocytes, the signal pathway associated with MOR gene transcription remains to be better defined. As the phosphatidylinositol 3-kinase (PI3K)/AKT pathway can mediate diverse biological responses and is crucial for optima...

journal_title：Biochemical pharmacology

authors： Liu H,Li H,Guo L,Li M,Li C,Wang S,Jiang W,Liu X,McNutt MA,Li G

更新日期：2010-02-01 00:00:00

abstract：:The thermodynamic parameters DeltaG degrees , DeltaH degrees and DeltaS degrees of the binding equilibrium of agonists and antagonists at cannabinoid CB(1) and CB(2) receptors were determined by means of affinity measurements at different temperatures and van't Hoff plots were constructed. Affinity constants were meas...

journal_title：Biochemical pharmacology

authors： Merighi S,Simioni C,Gessi S,Varani K,Borea PA

更新日期：2010-02-01 00:00:00

abstract：:CYP3A4 is the most important drug-metabolizing enzyme that is involved in biotransformation of more than 50% of drugs. Pregnane X receptor (PXR) dominantly controls CYP3A4 inducibility in the liver, whereas vitamin D receptor (VDR) transactivates CYP3A4 in the intestine by secondary bile acids. Four major functional P...

journal_title：Biochemical pharmacology

authors： Pavek P,Pospechova K,Svecova L,Syrova Z,Stejskalova L,Blazkova J,Dvorak Z,Blahos J

更新日期：2010-01-15 00:00:00

abstract：:Prodrug activation gene therapy for cancer involves expressing prodrug-activating enzymes in tumour cells, so they can be selectively killed by systemically administered prodrug. For example, Escherichia colinfsB nitroreductase (E.C. 1.6.99.7)(NTR), sensitises cells to the prodrug CB1954 (5-[aziridin-1-yl]-2,4-dinitro...

journal_title：Biochemical pharmacology

authors： Jaberipour M,Vass SO,Guise CP,Grove JI,Knox RJ,Hu L,Hyde EI,Searle PF

更新日期：2010-01-15 00:00:00

abstract：:It is increasingly clear that some of the effects of both free and derivatised long chain fatty acids in pancreatic beta-cells are mediated by a group of G-protein coupled receptors. Some of these display close structural homology while others are more divergent. This Commentary reviews the expression and functional r...

journal_title：Biochemical pharmacology

authors： Morgan NG,Dhayal S

更新日期：2009-12-15 00:00:00

abstract：:In this study, we showed that oligogalacturonic acid (OGA) purified from flax pectin inhibit in vitro osteoclastic bone resorption in a dose-dependent manner. The OGA inhibitory effect was neither linked to an effect on osteoclast apoptosis, nor to an inhibition of cathepsin K activity. By means of an in vitro collage...

journal_title：Biochemical pharmacology

authors： Lion JM,Mentaverri R,Rossard S,Jullian N,Courtois B,Courtois J,Brazier M,Mazière JC,Kamel S

更新日期：2009-12-15 00:00:00

abstract：:The identification of proliferation/survival pathways constitutively activated by genetic alterations in multiple myeloma (MM), or sustained by the bone marrow (BM) microenvironment, provides novel opportunities for the development of targeted therapies. The deregulated function of protein tyrosine kinases plays a cri...

journal_title：Biochemical pharmacology

authors： Cassinelli G,Ronchetti D,Laccabue D,Mattioli M,Cuccuru G,Favini E,Nicolini V,Greco A,Neri A,Zunino F,Lanzi C

更新日期：2009-11-01 00:00:00

abstract：:The use of either methadone or buprenorphine for treatment of the pregnant opiate-dependent patient improves maternal and neonatal outcome. However, patient outcomes are often complicated by neonatal abstinence syndrome (NAS). The incidence and severity of NAS should depend on opiate concentration in the fetal circula...

journal_title：Biochemical pharmacology

authors： Hemauer SJ,Patrikeeva SL,Nanovskaya TN,Hankins GD,Ahmed MS

更新日期：2009-11-01 00:00:00

abstract：:Serotonin plays a critical role in the regulation of intestinal physiology. The serotonin transporter (SERT) expressed in the intestinal epithelium determines 5-HT availability and activity. The serotoninergic system and SERT activity have been described as being altered in chronic intestinal pathologies such as infla...

journal_title：Biochemical pharmacology

authors： Matheus N,Mendoza C,Iceta R,Mesonero JE,Alcalde AI

更新日期：2009-11-01 00:00:00

abstract：:Dimebolin (Dimebon), is a non-selective antihistamine approved in Russia for the treatment of allergy. Recently, this drug has been shown to be neuroprotective in cellular models of Alzheimer's disease and Huntington's disease, and to preserve cognitive function when chronically administered to AF64A lesioned rats. In...

journal_title：Biochemical pharmacology

authors： Schaffhauser H,Mathiasen JR,Dicamillo A,Huffman MJ,Lu LD,McKenna BA,Qian J,Marino MJ

更新日期：2009-10-15 00:00:00

abstract：:Nicotinic acetylcholine receptors (nAChRs) are members of the Cys-loop family of neurotransmitter-gated ion channels, a family that also includes receptors for gamma-aminobutyric acid, glycine and 5-hydroxytryptamine. In humans, nAChRs have been implicated in several neurological and psychiatric disorders and are majo...

journal_title：Biochemical pharmacology

authors： Millar NS

更新日期：2009-10-01 00:00:00

abstract：:Despite tobacco being highly addictive, it is unclear if nicotine has significant affective properties. To address this, we studied taste reactions to gustatory stimuli, palatable sucrose and unpalatable quinine, which are believed to reflect ongoing affective state. Taste reactivity was assessed during chronic nicoti...

journal_title：Biochemical pharmacology

authors： Wing VC,Cagniard B,Murphy NP,Shoaib M

更新日期：2009-10-01 00:00:00

abstract：:Brain penetration of drugs which are subject to P-glycoprotein (Pgp)-mediated efflux is attenuated, as manifested by the fact that the cerebrospinal fluid concentration (C(CSF)), a good surrogate of the unbound brain concentration (C(ub)), is lower than the unbound plasma concentration (C(up)) for Pgp substrates. In r...

journal_title：Biochemical pharmacology

authors： Tang C,Kuo Y,Pudvah NT,Ellis JD,Michener MS,Egbertson M,Graham SL,Cook JJ,Hochman JH,Prueksaritanont T

更新日期：2009-09-15 00:00:00

abstract：:The deregulated activation of NF-kappaB is associated with cancer development and inflammatory diseases. With an aim to find new NF-kappaB inhibitors, we purified and characterized compounds from extracts of the Fijian sponge Rhabdastrella globostellata, the crinoid Comanthus parvicirrus, the soft corals Sarcophyton s...

journal_title：Biochemical pharmacology

authors： Folmer F,Jaspars M,Solano G,Cristofanon S,Henry E,Tabudravu J,Black K,Green DH,Küpper FC,Aalbersberg W,Feussner K,Dicato M,Diederich M

更新日期：2009-09-15 00:00:00

abstract：:Accumulating evidence indicates that dysfunction in amino acid neurotransmission contributes to the pathophysiology of depression. Consequently, the modulation of amino acid neurotransmission represents a new strategy for antidepressant development. While glutamate receptor ligands are known to have antidepressant eff...

journal_title：Biochemical pharmacology

authors： Valentine GW,Sanacora G

更新日期：2009-09-01 00:00:00

abstract：:Chlorpyrifos (CPF) is a pesticide that causes tens of thousands of deaths per year worldwide. Chlorpyrifos oxon (CPO) is the active metabolite of CPF that inhibits acetylcholinesterase. However, this presumed metabolite has escaped detection in human samples by conventional methods (HPLC, GC-MS, LC-MS) until now. A re...

journal_title：Biochemical pharmacology

authors： Eyer F,Roberts DM,Buckley NA,Eddleston M,Thiermann H,Worek F,Eyer P

更新日期：2009-09-01 00:00:00

abstract：:Novel therapies for the treatment of solid tumors have generally failed to improve patient overall survival. These therapeutic approaches are typically focused on targeting signaling pathways implicated in cell growth and/or survival in order to shrink the malignant mass and achieve an objective clinical response; how...

journal_title：Biochemical pharmacology

authors： Winquist RJ,Boucher DM,Wood M,Furey BF

更新日期：2009-08-15 00:00:00

abstract：:Compounds of the mevalonate pathway containing a terminal di- or triphosphate (mev-PP or mev-PPP) were tested as substrates of several enzyme ligases (T4 RNA ligase, T4 DNA ligase, firefly luciferase and other ligases) for the synthesis of ATP derivatives of the mev-pppA or mev-ppppA type. T4 RNA ligase, in the presen...

journal_title：Biochemical pharmacology

authors： Sillero MA,de Diego A,Tavares JE,Silva JA,Pérez-Zúñiga FJ,Sillero A

更新日期：2009-08-15 00:00:00

abstract：:Cholangiocarcinoma is the second most common primary hepatic neoplasia and the only curative therapy is surgical resection or liver transplantation. Biphosphonates (BPs) are an emerging class of drugs widely used to treat bone diseases and also appear to possess direct antitumor activity. In two human cholangiocarcino...

journal_title：Biochemical pharmacology

authors： Romani AA,Desenzani S,Morganti MM,La Monica S,Borghetti AF,Soliani P

更新日期：2009-07-15 00:00:00

abstract：:Many tumors are resistant to drug-induced cell-cycle arrest and apoptosis. We have reported that apoptosis can be restored in human multidrug-resistant (MDR) hepatocellular carcinoma cell lines by celecoxib. Here we show that P-glycoprotein (P-gp) mediates cell-cycle arrest and autophagy induced by celecoxib in human ...

journal_title：Biochemical pharmacology

authors： Mazzanti R,Platini F,Bottini C,Fantappiè O,Solazzo M,Tessitore L

更新日期：2009-07-01 00:00:00

abstract：:Restoration of dysregulated bone homeostasis is a therapeutic goal in many diseases including osteoporosis, rheumatoid arthritis and metastatic cancer. The molecular pathways regulating bone remodeling are major therapeutic targets, and studies continue to reveal endogenous factors that may be pathologically up- or do...

journal_title：Biochemical pharmacology

authors： Abraham AK,Ramanathan M,Weinstock-Guttman B,Mager DE

更新日期：2009-06-15 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 aim of this study was to document the in vivo transport of everolimus (inhibitor of mTOR) by P-glycoprotein (P-gp), and to investigate the influence of lapatinib (inhibitor of P-gp) on everolimus disposition. Pharmacokinetics of everolimus (0.25mg/kg) has been investigated after oral administration in mdr1a-/1b- m...

journal_title：Biochemical pharmacology

authors： Chu C,Abbara C,Noël-Hudson MS,Thomas-Bourgneuf L,Gonin P,Farinotti R,Bonhomme-Faivre L

更新日期：2009-05-15 00:00:00

abstract：:Tachykinin NK receptors (NKRs) differ to a large degree among species with respect to their affinities for small molecule antagonists. The aims of the present study were to clone NKRs from gerbil (NK2R and NK3R) and dog (NK1R, NK2R and NK3R) in which the sequence was previously unknown and to investigate the potency o...

journal_title：Biochemical pharmacology

authors： Leffler A,Ahlstedt I,Engberg S,Svensson A,Billger M,Oberg L,Bjursell MK,Lindström E,von Mentzer B

更新日期：2009-05-01 00:00:00

abstract：:In vitro treatment of human T-cell leukemia cells with 7-hydroxymethotrexate, the major metabolite of methotrexate resulted in acquired resistance as a result of the complete loss of folypolyglutamate synthetase (FPGS) activity. This was in contradistinction to the major modality of antifolate resistance of impaired d...

journal_title：Biochemical pharmacology

authors： Fotoohi AK,Assaraf YG,Moshfegh A,Hashemi J,Jansen G,Peters GJ,Larsson C,Albertioni F

更新日期：2009-04-15 00:00:00

abstract：:In the combat against inflammation, glucocorticoids (GCs) are a widespread therapeutic. These ligands of the glucocorticoid receptor (GR) inhibit the transactivation of various transcription factors, including nuclear factor-kappaB (NF-kappaB), and alter the composition of the pro-inflammatory enhanceosome, culminatin...

journal_title：Biochemical pharmacology

authors： Beck IM,Vanden Berghe W,Gerlo S,Bougarne N,Vermeulen L,De Bosscher K,Haegeman G

更新日期：2009-04-01 00:00:00

abstract：:Protocatechuic acid (PA), a structurally typical phenolic acid in danshen, shows anti-angina efficacy. But until now, besides scavenging of oxygen free radicals, the understanding of its anti-angina mechanism has been limited. In our study, based on a novel metabolic route of PA identified in rat heart and its influen...

journal_title：Biochemical pharmacology

authors： Cao YG,Zhang L,Ma C,Chang BB,Chen YC,Tang YQ,Liu XD,Liu XQ

更新日期：2009-03-15 00:00:00

abstract：:Neutrophil accumulation response to cigarette smoke (CS) in humans and animal models is believed to play an important role in pathogenesis of many tobacco-related lung diseases. Here we evaluated the lung anti-inflammatory effect of aspirin and indomethacin in mice exposed to CS. C57BL/6 mice were exposed to four ciga...

journal_title：Biochemical pharmacology

authors： Castro P,Nasser H,Abrahão A,Dos Reis LC,Riça I,Valença SS,Rezende DC,Quintas LE,Cavalcante MC,Porto LC,Koatz VL

更新日期：2009-03-15 00:00:00

abstract：:The proteasome inhibitor bortezomib is currently an important drug for treatment of relapsed and refractory multiple myeloma (MM) and for elderly patients. However, cells from some patients show resistance to bortezomib. We have evaluated the possibility of improving bortezomib therapy with Apo2L/TRAIL, a death ligand...

journal_title：Biochemical pharmacology

authors： Balsas P,López-Royuela N,Galán-Malo P,Anel A,Marzo I,Naval J

更新日期：2009-03-01 00:00:00

abstract：:Platelet secretion is an important physiological event in hemostasis. The protease-activated receptors, PAR 1 and PAR 4, and the thromboxane receptor activate the G(12/13) pathways, in addition to the G(q) pathways. Here, we investigated the contribution of G(12/13) pathways to platelet dense granule release. 2MeSADP,...

journal_title：Biochemical pharmacology

authors： Jin J,Mao Y,Thomas D,Kim S,Daniel JL,Kunapuli SP

更新日期：2009-03-01 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：:2,3,7,8-Tetrachlorodibenzo-p-dioxin (TCDD) is a widespread environmental pollutant, which causes a variety of severe health effects, e.g. immunosuppression, hepatotoxicity, and carcinogenesis. The main mediator of TCDD toxicity is the arylhydrocarbon receptor (AhR), which, upon activation, translocates into the nucleu...

journal_title：Biochemical pharmacology

authors： Haarmann-Stemmann T,Bothe H,Abel J

更新日期：2009-02-15 00:00:00