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：:Multidrug resistance-associated protein 2 (Mrp2) is an ATP-dependent export pump that mediates the formation of bile-salt-independent bile flow. Disruption of the canalicular localization of Mrp2, without changes in its expression, is observed in chronic liver failure and is accompanied by oxidative stress. We reporte...

journal_title：Biochemical pharmacology

authors： Saeki J,Sekine S,Horie T

更新日期：2011-01-01 00:00:00

abstract：:Cardiac steroids are used to treat various diseases including congestive heart failure and cancer. The aim of this study was to investigate the anti-leukemic activity of UNBS1450, a hemi-synthetic cardenolide belonging to the cardiac steroid glycoside family. Here, we report that, at low nanomolar concentrations, UNBS...

journal_title：Biochemical pharmacology

authors： Juncker T,Cerella C,Teiten MH,Morceau F,Schumacher M,Ghelfi J,Gaascht F,Schnekenburger M,Henry E,Dicato M,Diederich M

更新日期：2011-01-01 00:00:00

abstract：:For almost 10 years, Nod2 has been known as a cytosolic innate receptor able to sense peptidoglycan from Gram-positive and -negative bacteria and to trigger RIP2- and NF-κB-mediated pro-inflammatory and antibacterial response. Mutations in the gene encoding Nod2 in humans have been associated with Crohn's disease (CD)...

journal_title：Biochemical pharmacology

authors： Lecat A,Piette J,Legrand-Poels S

更新日期：2010-12-15 00:00:00

abstract：:Poly(ADP-ribosylation) consists in the conversion of β-NAD(+) into ADP-ribose, which is then bound to acceptor proteins and further used to form polymers of variable length and structure. The correct turnover of poly(ADP-ribose) is ensured by the concerted action of poly(ADP-ribose) polymerase (PARP) and poly(ADP-ribo...

journal_title：Biochemical pharmacology

authors： Giansanti V,Donà F,Tillhon M,Scovassi AI

更新日期：2010-12-15 00:00:00

abstract：:Nitric oxide sensitive guanylyl cyclase (NOsGC) is a heterodimeric enzyme consisting of an α and a β subunit. Two heterodimeric enzymes are known to be important for NO-signalling in humans: α(1)/β(1) and α(2)/β(1). No difference had so far been detected with respect to their pharmacological properties, but as we show...

journal_title：Biochemical pharmacology

authors： Haase N,Haase T,Kraehling JR,Behrends S

更新日期：2010-12-01 00:00:00

abstract：:Induction of the breast cancer resistance protein (BCRP/ABCG2) expression has been found in various tissues and cell-types after exposure to chemicals including 17β-estradiol, rosiglitazone, imatinib, as well as aryl hydrocarbon receptor (AhR) activators such as 2,3,7,8-tetrachlorodibenzodioxin, 3-methylcholanthrene (...

journal_title：Biochemical pharmacology

authors： Tompkins LM,Li H,Li L,Lynch C,Xie Y,Nakanishi T,Ross DD,Wang H

更新日期：2010-12-01 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：:Chlorogenic acid (Chl) has been reported to possess a wide range of biological and pharmacological properties including induction of apoptosis of Bcr-Abl(+) chronic myeloid leukemia (CML) cell lines and clinical leukemia samples via inhibition of Bcr-Abl phosphorylation. Here we studied the mechanisms of action of Chl...

journal_title：Biochemical pharmacology

authors： Rakshit S,Mandal L,Pal BC,Bagchi J,Biswas N,Chaudhuri J,Chowdhury AA,Manna A,Chaudhuri U,Konar A,Mukherjee T,Jaisankar P,Bandyopadhyay S

更新日期：2010-12-01 00:00:00

abstract：:We describe the synthesis and the pharmacological characterization of a new quaternary selective serotonin reuptake inhibitor (SSRI) N-methyl-citalopram (NMC) with periphery restricted action due to its inability to cross the blood brain barrier. NMC recognized and blocked the human platelet serotonin transporter (SER...

journal_title：Biochemical pharmacology

authors： Bismuth-Evenzal Y,Roz N,Gurwitz D,Rehavi M

更新日期：2010-11-15 00:00:00

abstract：:Imaging the pharmacodynamics of anti-cancer drugs may allow early assessment of anti-cancer effects. Increases in 3'-deoxy-3'-[(18)F]fluorothymidine ([(18)F]FLT) uptake early after thymidylate synthase inhibition (TS) inhibition, the so-called flare response, is considered to be largely due to an increase in binding s...

journal_title：Biochemical pharmacology

authors： Lee SJ,Kim SY,Chung JH,Oh SJ,Ryu JS,Hong YS,Kim TW,Moon DH

更新日期：2010-11-15 00:00:00

abstract：:The advent of drugs targeting tumor-associated prosurvival alterations of cancer cells has changed the interest of antitumor drug development from cytotoxic drugs to target-specific agents. Although single-agent therapy with molecularly targeted agents has shown limited success in tumor growth control, a promising str...

journal_title：Biochemical pharmacology

authors： Perego P,Cossa G,Zuco V,Zunino F

更新日期：2010-11-15 00:00:00

abstract：:Aberrant signal transduction by mutant or overexpressed protein kinases has emerged as a promising target for treatment of acute myeloid leukemia (AML). We here present a novel low molecular weight kinase inhibitor, AKN-032, targeting the FMS-like tyrosine kinase 3 (FLT3) and discovered in a new type of screening funn...

journal_title：Biochemical pharmacology

authors： Eriksson A,Höglund M,Lindhagen E,Aleskog A,Hassan SB,Ekholm C,Fhölenhag K,Jensen AJ,Löthgren A,Scobie M,Larsson R,Parrow V

更新日期：2010-11-15 00:00:00

abstract：:Chlamydia pneumoniae is a universal pathogen that has been indicated to play a part in the development of asthma, atherosclerosis and lung cancer. The complete eradication of this intracellular bacterium is in practice impossible with the antibiotics that are currently in use and studies on new antichlamydial compound...

journal_title：Biochemical pharmacology

authors： Salin O,Alakurtti S,Pohjala L,Siiskonen A,Maass V,Maass M,Yli-Kauhaluoma J,Vuorela P

更新日期：2010-10-15 00:00:00

abstract：:The nicotinic acetylcholine receptors (nAChR) assembled from alpha4 and beta2 subunits are the most densely expressed subtype in the brain. Concentration-effect curves for agonist activation of alpha4beta2*-nAChR are biphasic. This biphasic agonist sensitivity is ascribed to differences in subunit stoichiometry. The s...

journal_title：Biochemical pharmacology

authors： Marks MJ,Meinerz NM,Brown RW,Collins AC

更新日期：2010-10-15 00:00:00

abstract：:Oxidant damage from reactive oxygen species (ROS) and reactive nitrogen species (RNS) is a major contributor to the cellular damage seen in numerous types of renal injury. Resveratrol (trans-3,4',5-trihydroxystilbene) is a phytoalexin found naturally in many common food sources. The anti-oxidant properties of resverat...

journal_title：Biochemical pharmacology

authors： Holthoff JH,Woodling KA,Doerge DR,Burns ST,Hinson JA,Mayeux PR

更新日期：2010-10-15 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：:Curcumin, a yellow pigment present in the spice turmeric (Curcuma longa), has been linked with multiple beneficial activities, but its optimum potential is limited by poor bioavailability, in part due to the lack of solubility in aqueous solvents. To overcome the solubility problem, we have recently developed a novel ...

journal_title：Biochemical pharmacology

authors： Yadav VR,Prasad S,Kannappan R,Ravindran J,Chaturvedi MM,Vaahtera L,Parkkinen J,Aggarwal BB

更新日期：2010-10-01 00:00:00

abstract：:From routine in vitro drug-transporter inhibition assays, observed inhibition is typically assumed from direct interaction with the transporter. Other mechanisms that possibly reduce substrate uptake are not frequently fully examined. The objective of this study was to investigate the association of transporter inhibi...

journal_title：Biochemical pharmacology

authors： Zheng X,Diao L,Ekins S,Polli JE

更新日期：2010-10-01 00:00:00

abstract：:The orphan nuclear receptor estrogen-related receptor alpha (ERRalpha) has been implicated in the development of various human malignancies, including breast, prostate, ovary, and colon cancer. ERRalpha, bound to a co-activator protein (e.g., peroxisome proliferator receptor gamma co-activator-1alpha, PGC-1alpha), reg...

journal_title：Biochemical pharmacology

authors： Duellman SJ,Calaoagan JM,Sato BG,Fine R,Klebansky B,Chao WR,Hobbs P,Collins N,Sambucetti L,Laderoute KR

更新日期：2010-09-15 00:00:00

abstract：:Idiopathic pulmonary fibrosis (IPF) involves infiltration of leucocytes, pulmonary injury, fibrosis and resulting pulmonary dysfunction. Myofibroblasts and transforming growth factor (TGF)-beta1 have been suggested to play a major role in the pathology and the myofibroblasts are derived from both lung epithelial cells...

journal_title：Biochemical pharmacology

authors： Tanaka K,Tanaka Y,Namba T,Azuma A,Mizushima T

更新日期：2010-09-15 00:00:00

abstract：:Bcr-abl kinase inhibitors have provided proof of principal that targeted therapy holds great promise for the treatment of cancer. However, despite the success of these agents in treating chronic myelogenous leukemia (CML), the majority of patients continue to present with minimal residual disease contained within the ...

journal_title：Biochemical pharmacology

authors： Nair RR,Tolentino J,Hazlehurst LA

更新日期：2010-09-01 00:00:00

abstract：:Rational approaches to targeted cancer therapy have begun to predominate the pipelines of oncology drug development. Our rapidly increasing understanding of the "wiring" of tumor cells and the vulnerabilities of such cells that can potentially be exploited through targeted treatments has opened up enormous opportuniti...

journal_title：Biochemical pharmacology

authors： Sharma SV,Settleman J

更新日期：2010-09-01 00:00:00

abstract：:ATP-driven efflux pumps such as phosphoglycoprotein-170 (P-gp), multidrug-resistance-associated protein-2 (MRP-2), or breast cancer resistance protein (BCRP) play a crucial role in limiting the efficacy of tumor pharmacotherapy. Selected flavonoids have been suggested to inhibit individual efflux-transporters and to a...

journal_title：Biochemical pharmacology

authors： Schumacher M,Hautzinger A,Rossmann A,Holzhauser S,Popovic D,Hertrampf A,Kuntz S,Boll M,Wenzel U

更新日期：2010-08-15 00:00:00

abstract：:Pyruvate is an important metabolic intermediate, and also is an effective scavenger of hydrogen peroxide and other reactive oxygen species (ROS). Pharmacological administration of pyruvate has been shown to improve organ function in animal models of oxidant-mediated cellular injury. However, pyruvate is relatively uns...

journal_title：Biochemical pharmacology

authors： Kao KK,Fink MP

更新日期：2010-07-15 00:00:00

abstract：:Multivalent dendrimeric conjugates of GPCR ligands may have increased potency or selectivity in comparison to monomeric ligands, a phenomenon that was tested in a model of cytoprotection in mouse HL-1 cardiomyocytes. Quantitative RT-PCR indicated high expression levels of endogenous A(1) and A(2A) adenosine receptors ...

journal_title：Biochemical pharmacology

authors： Keene AM,Balasubramanian R,Lloyd J,Shainberg A,Jacobson KA

更新日期：2010-07-15 00:00:00

abstract：:Osteoarthritis (OA) is a chronic degenerative joint disorder characterized by destruction of the articular cartilage, subchondral bone alterations and synovitis. Current treatments are focused on symptomatic relief but they lack efficacy to control the progression of this disease which is a leading cause of disability...

journal_title：Biochemical pharmacology

authors： Alcaraz MJ,Megías J,García-Arnandis I,Clérigues V,Guillén MI

更新日期：2010-07-01 00:00:00

abstract：:Nobiletin is a polymethoxylated flavone found in certain citrus fruits that exhibits various pharmacological effects including anti-inflammatory, antitumor and neuroprotective properties. The present study investigated the effects of nobiletin on insulin sensitivity in obese diabetic ob/ob mice, and the possible mecha...

journal_title：Biochemical pharmacology

authors： Lee YS,Cha BY,Saito K,Yamakawa H,Choi SS,Yamaguchi K,Yonezawa T,Teruya T,Nagai K,Woo JT

更新日期：2010-06-01 00:00:00

abstract：:Thymoquinone (TQ), derived from the medicinal spice Nigella sativa (also called black cumin), has been shown to exhibit anti-inflammatory and anti-cancer activities. In this report we employed polymer-based nanoparticle approach to improve upon its effectiveness and bioavailability. TQ was encapsulated with 97.5% effi...

journal_title：Biochemical pharmacology

authors： Ravindran J,Nair HB,Sung B,Prasad S,Tekmal RR,Aggarwal BB

更新日期：2010-06-01 00:00:00

abstract：:Smoking during pregnancy is the largest modifiable risk factor for pregnancy-related morbidity and mortality. The success of bupropion for smoking cessation warrants its investigation for the treatment of pregnant patients. Nevertheless, the use of bupropion for the treatment of pregnant smokers requires additional da...

journal_title：Biochemical pharmacology

authors： Wang X,Abdelrahman DR,Zharikova OL,Patrikeeva SL,Hankins GD,Ahmed MS,Nanovskaya TN

更新日期：2010-06-01 00:00:00

abstract：:Inhibitory effects of Delta(9)-tetrahydrocannabinol (Delta(9)-THC), cannabidiol (CBD), and cannabinol (CBN), the three major constituents in marijuana, on catalytic activities of human cytochrome P450 (CYP) 1 enzymes were investigated. These cannabinoids inhibited 7-ethoxyresorufin O-deethylase activity of recombinant...

journal_title：Biochemical pharmacology

authors： Yamaori S,Kushihara M,Yamamoto I,Watanabe K

更新日期：2010-06-01 00:00:00

abstract：:BLT2, a low-affinity leukotriene B4 (LTB4) receptor, is a member of the G-protein coupled receptor (GPCR) family and is involved in the pathogenesis of inflammatory diseases such as asthma. Despite its clinical implications, however, no pharmacological inhibitors are available. In the present study, we screened for sm...

journal_title：Biochemical pharmacology

authors： Kim JY,Lee WK,Yu YG,Kim JH

更新日期：2010-05-15 00:00:00

abstract：:Inflammation-induced microsomal prostaglandin E synthase-1 (mPGES-1) is the terminal enzyme that synthesizes prostaglandin E(2) (PGE(2)) downstream of cyclooxygenase-2 (COX-2). The efficacy of nonsteroidal anti-inflammatory drugs and COX-2 inhibitors in the treatment of the signs and symptoms of osteoarthritis, rheuma...

journal_title：Biochemical pharmacology

authors： Mbalaviele G,Pauley AM,Shaffer AF,Zweifel BS,Mathialagan S,Mnich SJ,Nemirovskiy OV,Carter J,Gierse JK,Wang JL,Vazquez ML,Moore WM,Masferrer JL

更新日期：2010-05-15 00:00:00

abstract：:C-1748 is a DNA-binding agent with potent antitumor activity, especially towards prostate and colon carcinoma xenografts in mice. Here, we elucidated the nature of cellular response of human colon carcinoma HCT8 and HT29 cells to C-1748 treatment, at biologically relevant concentrations (EC(90) and their multiplicity)...

journal_title：Biochemical pharmacology

authors： Augustin E,Moś-Rompa A,Nowak-Ziatyk D,Konopa J

更新日期：2010-05-01 00:00:00

abstract：:Glutathione conjugation and transportation of glutathione conjugates of anticancer drugs out of cells are important for detoxification of many anticancer drugs. Inhibition of this detoxification system has recently been proposed as a strategy to treat drug-resistant solid tumors. Gallbladder carcinoma is resistant to ...

journal_title：Biochemical pharmacology

authors： Wang W,Sun YP,Huang XZ,He M,Chen YY,Shi GY,Li H,Yi J,Wang J

更新日期：2010-04-15 00:00:00

abstract：:We have been studying the requirement for the aryl hydrocarbon receptor nuclear translocator (Arnt)-dependent DNA complex formation, which precedes the activation of gene transcription. Using DEAE chromatography, we have obtained a Sf9 insect fraction F5 that is highly enriched with beta-tubulin. F5 inhibits the forma...

journal_title：Biochemical pharmacology

authors： Zhang T,Wang X,Shinn A,Jin J,Chan WK

更新日期：2010-04-15 00:00:00

abstract：:The antimicrobial peptide human beta-defensin-3 (hBD-3) is produced by epidermal keratinocytes and protects the skin from infections. This peptide induces the release of a lipid mediator, prostaglandin D(2) from dermal mast cells. Prostaglandin D(2) binds to cell-surface G protein-coupled receptors, D prostanoid recep...

journal_title：Biochemical pharmacology

authors： Kanda N,Ishikawa T,Watanabe S

更新日期：2010-04-01 00:00:00

abstract：:Human CYP2E1 is one of the pharmacologically and toxicologically important cytochrome P450 isoforms. Earlier studies have reported that the CYP2E1 expression is extensively regulated by post-transcriptional and post-translational mechanisms, but the molecular basis remains unclear. In the present study, we examined th...

journal_title：Biochemical pharmacology

authors： Mohri T,Nakajima M,Fukami T,Takamiya M,Aoki Y,Yokoi T

更新日期：2010-04-01 00:00:00

abstract：:Multidrug resistance-associated protein (MRP-1/ABCC1) transports a wide range of therapeutic agents and may play a critical role in the development of multidrug resistance (MDR) in tumor cells. However, the regulation of MRP-1 remains controversial. To explore whether miRNAs are involved in the regulation of MRP-1 exp...

journal_title：Biochemical pharmacology

authors： Liang Z,Wu H,Xia J,Li Y,Zhang Y,Huang K,Wagar N,Yoon Y,Cho HT,Scala S,Shim H

更新日期：2010-03-15 00:00:00

abstract：:Inflammation is a multi-staged process whose expansive phase is thought to be driven by acutely released arachidonic acid (AA) and its metabolites. Inhibition of cyclooxygenase (COX), lipoxygenase (LOX), or soluble epoxide hydrolase (sEH) is known to be anti-inflammatory. Inhibition of sEH stabilizes the cytochrome P4...

journal_title：Biochemical pharmacology

authors： Liu JY,Yang J,Inceoglu B,Qiu H,Ulu A,Hwang SH,Chiamvimonvat N,Hammock BD

更新日期：2010-03-15 00:00:00