abstract：:Trypanosoma brucei encodes a relatively high number of genes of the equilibrative nucleoside transporter (ENT) family. We report here the cloning and in-depth characterization of one T. brucei brucei ENT member, TbNT9/AT-D. This transporter was expressed in Saccharomyces cerevisiae and displayed a uniquely high affini...

journal_title：Molecular pharmacology

authors： Al-Salabi MI,Wallace LJ,Lüscher A,Mäser P,Candlish D,Rodenko B,Gould MK,Jabeen I,Ajith SN,de Koning HP

更新日期：2007-03-01 00:00:00

abstract：:Cidofovir [(S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine; (S)-HPMPC] is an antiviral drug that has been approved for the treatment of cytomegalovirus retinitis in patients with AIDS. Cidofovir also possesses potent activity against human papillomavirus-induced tumors in animal models and patients. We have recent...

journal_title：Molecular pharmacology

authors： Liekens S,Gijsbers S,Vanstreels E,Daelemans D,De Clercq E,Hatse S

更新日期：2007-03-01 00:00:00

abstract：:Valproic acid (VPA) is an effective antiepileptic drug with an additional activity for the treatment of bipolar disorder. It has been assumed that both activities arise from a common target. At the molecular level, VPA targets a number of distinct proteins that are involved in signal transduction. VPA inhibition of in...

journal_title：Molecular pharmacology

authors： Shimshoni JA,Dalton EC,Jenkins A,Eyal S,Ewan K,Williams RS,Pessah N,Yagen B,Harwood AJ,Bialer M

更新日期：2007-03-01 00:00:00

abstract：:We have examined alpha1beta2gamma2L GABAA receptor modulation by the endogenous steroids allopregnanolone (3alpha5alphaP), pregnenolone sulfate, and beta-estradiol in the absence and presence of ethanol. Coapplication of 0.1 to 1% (17-170 mM) ethanol influenced receptor modulation by 3alpha5alphaP but not that by preg...

journal_title：Molecular pharmacology

authors： Akk G,Li P,Manion BD,Evers AS,Steinbach JH

更新日期：2007-02-01 00:00:00

abstract：:Airway smooth muscle (ASM) cells can act as effector cells in the initiation and/or perpetuation of airway inflammation in asthma by producing various inflammatory chemokines or cytokines. Previous studies from our laboratory and others showed that the combination of tumor necrosis factor-alpha (TNFalpha) and interfer...

journal_title：Molecular pharmacology

authors： Keslacy S,Tliba O,Baidouri H,Amrani Y

更新日期：2007-02-01 00:00:00

abstract：:Adenine-uridine rich elements (AREs) play an important role in modulating mRNA stability, being the target site of many ARE-binding proteins (AUBPs) that are involved in the decay process. Three 26-mer 2'-O-methyl oligoribonucleotides (ORNs) homologous to the core region of ARE of bcl2 mRNA have been studied for decoy...

journal_title：Molecular pharmacology

authors： Bevilacqua A,Ghisolfi L,Franzi S,Maresca G,Gherzi R,Capaccioli S,Nicolin A,Canti G

更新日期：2007-02-01 00:00:00

abstract：:Upon sustained insult, kinins are released and many kinin responses, such as inflammatory pain, adapt from a B2 receptor (B2R) type in the acute phase to a B1 receptor (B1R) type in the chronic phase. In this study, we show that kinins modulate receptor endocytosis to rapidly decrease B2R and increase B1R on the cell ...

journal_title：Molecular pharmacology

authors： Enquist J,Skröder C,Whistler JL,Leeb-Lundberg LM

更新日期：2007-02-01 00:00:00

abstract：:Regulators of G-protein signaling (RGS) proteins are important components of signal transduction pathways initiated through G-protein-coupled receptors (GPCRs). RGS proteins accelerate the intrinsic GTPase activity of G-protein alpha-subunits (Galpha) and thus shorten the time course and reduce the magnitude of G-prot...

journal_title：Molecular pharmacology

authors： Roman DL,Talbot JN,Roof RA,Sunahara RK,Traynor JR,Neubig RR

更新日期：2007-01-01 00:00:00

abstract：:To determine the role of C-Rel in nitric-oxide synthase-2 (NOS-2) transcriptional activation, we evaluated the effect of lipopolysaccharide and interferon-gamma (LPS/IFNgamma) on C-Rel DNA binding in RAW 264.7. LPS/IFNgamma-stimulated C-Rel binding peaked at 4 to 8 h and declined at 24 h. Transfection of cells with a ...

journal_title：Molecular pharmacology

authors： Cieslik KA,Deng WG,Wu KK

更新日期：2006-12-01 00:00:00

abstract：:There is no approved means to prevent the toxic actions of cocaine. Cocaine esterase (CocE) is found in a rhodococcal strain of bacteria that grows in the rhizosphere soil around the coca plant and has been found to hydrolyze cocaine in vitro. The esteratic activity of CocE (0.1-1.0 mg, i.v.) was characterized and con...

journal_title：Molecular pharmacology

authors： Cooper ZD,Narasimhan D,Sunahara RK,Mierzejewski P,Jutkiewicz EM,Larsen NA,Wilson IA,Landry DW,Woods JH

更新日期：2006-12-01 00:00:00

abstract：:Tissue plasminogen activator (tPA), a serine protease, catalyzes the conversion of plasminogen to plasmin. In the present study, we investigated the role of the tPA-plasmin system in depolarization-evoked dopamine (DA) and acetylcholine (ACh) release in the nucleus accumbens (NAc) and hippocampus, respectively, of mic...

journal_title：Molecular pharmacology

authors： Ito M,Nagai T,Kamei H,Nakamichi N,Nabeshima T,Takuma K,Yamada K

更新日期：2006-11-01 00:00:00

abstract：:In cells expressing both the insulin receptor isoform A (IRA) and the insulin-like growth factor-1 receptor (IGF1R), the presence of hybrid receptors, made up of an alphabeta-IRA chain associated with an alphabeta-IGF1R chain, has been demonstrated. These heterodimers are found in normal cells, and they also seem to p...

journal_title：Molecular pharmacology

authors： Blanquart C,Gonzalez-Yanes C,Issad T

更新日期：2006-11-01 00:00:00

abstract：:Hepatocyte nuclear factor 4alpha (HNF4alpha) is a key transcription factor for the constitutive expression of cytochromes P450 (P450s) in the liver. However, human hepatoma HepG2 cells show a high level of HNF4alpha but express only marginal P450 levels. We found that the HNF4alpha-mediated P450 transcription in HepG2...

journal_title：Molecular pharmacology

authors： Martínez-Jiménez CP,Castell JV,Gómez-Lechón MJ,Jover R

更新日期：2006-11-01 00:00:00

abstract：:The endogenous bronchodilator, S-nitrosoglutathione (GSNO), increases expression, maturation, and function of both the wild-type and the DeltaF508 mutant of the cystic fibrosis transmembrane conductance regulatory protein (CFTR). Though transcriptional mechanisms of action have been identified, GSNO seems also to have...

journal_title：Molecular pharmacology

authors： Zaman K,Carraro S,Doherty J,Henderson EM,Lendermon E,Liu L,Verghese G,Zigler M,Ross M,Park E,Palmer LA,Doctor A,Stamler JS,Gaston B

更新日期：2006-10-01 00:00:00

abstract：:An alteration in the balance between a T-helper type 2 cell (Th2) response and a Th1 response may predispose to the development of bronchial asthma. Interleukin-18 (IL-18) has an ability to promote both Th1 and Th2 responses, depending on the surrounding cytokine environment. Reactive oxygen species (ROS) play a cruci...

journal_title：Molecular pharmacology

authors： Lee KS,Kim SR,Park SJ,Min KH,Lee KY,Jin SM,Yoo WH,Lee YC

更新日期：2006-10-01 00:00:00

abstract：:The insecticide imidacloprid and structurally related neonicotinoids act selectively on insect nicotinic acetylcholine receptors (nAChRs). To investigate the mechanism of neonicotinoid selectivity, we have examined the effects of mutations to basic amino acid residues in loop D of the nAChR acetylcholine (ACh) binding...

journal_title：Molecular pharmacology

authors： Shimomura M,Yokota M,Ihara M,Akamatsu M,Sattelle DB,Matsuda K

更新日期：2006-10-01 00:00:00

abstract：:Exposure to hepatitis C virus (HCV) can lead to the development of cirrhosis and hepatocellular carcinoma. To examine the effects of long-term HCV infection on hepatic cytochrome P450 1A1 (CYP1A1) expression and function, we used a human hepatoma cell line expressing the HCV subgenomic replicon (Huh.8) to evaluate CYP...

journal_title：Molecular pharmacology

authors： Anderson GR,Hasan A,Yin H,Qadri I,Quattrochi LC

更新日期：2006-09-01 00:00:00

abstract：:The CB1 cannabinoid receptor has been implicated in the regulation of bone remodeling and bone mass. A high bone mass (HBM) phenotype was reported in CB1-null mice generated on a CD1 background (CD1(CB1-/-) mice). By contrast, our preliminary studies in cb1-/- mice, backcrossed to C57BL/6J mice (C57(CB1-/-) mice), rev...

journal_title：Molecular pharmacology

authors： Tam J,Ofek O,Fride E,Ledent C,Gabet Y,Müller R,Zimmer A,Mackie K,Mechoulam R,Shohami E,Bab I

更新日期：2006-09-01 00:00:00

abstract：:Obesity is now recognized as a rapidly increasing worldwide threat to health, largely as a result of causing diabetes. Thus, considerable efforts are underway in the pharmaceutical industry to find drugs to treat this condition. Target validation in various academic and industrial laboratories has revealed a number of...

journal_title：Molecular pharmacology

authors： Pilch PF,Bergenhem N

更新日期：2006-09-01 00:00:00

abstract：:Capsaicin (vanilloid) sensitivity has long served as the functional signature of a subset of nociceptive sensory neurons. Mutagenesis studies have revealed seemingly distinct regions involved in mediating ligand binding and channel activation at the capsaicin binding site. Residue 547 (transmembrane region 4) mediates...

journal_title：Molecular pharmacology

authors： Johnson DM,Garrett EM,Rutter R,Bonnert TP,Gao YD,Middleton RE,Sutton KG

更新日期：2006-09-01 00:00:00

abstract：:The dopamine (DA) transporter (DAT) mediates the removal of released DA. DAT is the major molecular target responsible for the rewarding properties and abuse potential of the psychostimulant amphetamine (AMPH). AMPH has been shown to reduce the number of DATs at the cell surface, and this AMPH-induced cell surface DAT...

journal_title：Molecular pharmacology

authors： Kahlig KM,Lute BJ,Wei Y,Loland CJ,Gether U,Javitch JA,Galli A

更新日期：2006-08-01 00:00:00

abstract：:Thymidine phosphorylase (TPase) is one of the key enzymes involved in the pyrimidine nucleoside salvage pathway. However, TPase also stimulates angiogenesis, and its expression correlates well with microvessel density and metastasis in a variety of human tumors. We have shown recently that 5'-O-trityl-inosine (KIN59) ...

journal_title：Molecular pharmacology

authors： Liekens S,Bronckaers A,Hernández AI,Priego EM,Casanova E,Camarasa MJ,Pérez-Pérez MJ,Balzarini J

更新日期：2006-08-01 00:00:00

abstract：:alpha4beta2 nicotinic acetylcholine receptors (nAChRs) are recognized as the principal nicotine binding site in brain. Recombinant alpha4beta2 nAChR demonstrate biphasic concentration-response relationships with low- and high-EC50 components. This study shows that untranslated regions (UTR) can influence expression of...

journal_title：Molecular pharmacology

authors： Briggs CA,Gubbins EJ,Marks MJ,Putman CB,Thimmapaya R,Meyer MD,Surowy CS

更新日期：2006-07-01 00:00:00

abstract：:Up-regulation of fractalkine is involved in vascular and tissue damage in inflammatory conditions. Resveratrol has been shown to have anti-inflammatory, antioxidant, and antitumor activities. Its regulatory effects on expression of fractalkine in vascular endothelial cells and fractalkine receptor CX3CR1 in monocytes ...

journal_title：Molecular pharmacology

authors： Moon SO,Kim W,Sung MJ,Lee S,Kang KP,Kim DH,Lee SY,So JN,Park SK

更新日期：2006-07-01 00:00:00

abstract：:Cadmium is a dangerous metal distributed widely in the environment. Members of our laboratory recently identified the ZIP8 transporter protein, encoded by the mouse Slc39a8 gene, to be responsible for genetic differences in response to cadmium damage of the testis. Stable retroviral infection of the ZIP8 cDNA in mouse...

journal_title：Molecular pharmacology

authors： He L,Girijashanker K,Dalton TP,Reed J,Li H,Soleimani M,Nebert DW

更新日期：2006-07-01 00:00:00

abstract：:The constitutive androstane receptor (CAR) and the pregnane X receptor (PXR) play a major part in the control of drug metabolism and transport. We have previously shown that PXR and CAR expression is controlled by the glucocorticoid receptor (GR) and proposed the existence of a signal transmission cascade GR-(PXR/CAR)...

journal_title：Molecular pharmacology

authors： Duret C,Daujat-Chavanieu M,Pascussi JM,Pichard-Garcia L,Balaguer P,Fabre JM,Vilarem MJ,Maurel P,Gerbal-Chaloin S

更新日期：2006-07-01 00:00:00

abstract：:The NO/cGMP signaling pathway plays a major role in the cardiovascular system, in which it is involved in the regulation of smooth muscle tone and inhibition of platelet aggregation. Under pathophysiological conditions such as endothelial dysfunction, coronary artery disease, and airway hyperreactivity, smooth muscle ...

journal_title：Molecular pharmacology

authors： Mullershausen F,Lange A,Mergia E,Friebe A,Koesling D

更新日期：2006-06-01 00:00:00

abstract：:Beta-L-dioxolane-cytidine (L-OddC, BCH-4556, Troxacitabine), a novel L-configuration deoxycytidine analog, is under phase III clinical trial for cancer treatment. We showed that human apurinic/apyrimidinic endonuclease (APE-1) has exonuclease activity for preferentially removing L-OddC and other L-configuration nucleo...

journal_title：Molecular pharmacology

authors： Lam W,Park SY,Leung CH,Cheng YC

更新日期：2006-05-01 00:00:00

abstract：:Celecoxib (CE) is a nonsteroidal anti-inflammatory drug (NSAID) that is a specific inhibitor of cyclooxygenase 2 (COX2). It is indicated for a variety of chronic inflammatory conditions, including rheumatoid arthritis. Over the last few years, adverse cardiovascular effects and increased risk for heart attacks have be...

journal_title：Molecular pharmacology

authors： Alloza I,Baxter A,Chen Q,Matthiesen R,Vandenbroeck K

更新日期：2006-05-01 00:00:00

abstract：:In light of the potential use of the thiazolidinedione family of peroxisome proliferator-activated receptor-gamma (PPARgamma) agonists in prostate cancer treatment, this study assessed the mechanism by which these agents suppress prostate-specific antigen (PSA) secretion in prostate cancer cells. Two lines of evidence...

journal_title：Molecular pharmacology

authors： Yang CC,Ku CY,Wei S,Shiau CW,Chen CS,Pinzone JJ,Ringel MD,Chen CS

更新日期：2006-05-01 00:00:00

abstract：:Neurotrophins are a family of secreted proteins that play an important role in the development, differentiation, and survival of neurons. Studies also suggest that aberrant neurotrophin signaling may play a role in processes underlying disease states such as schizophrenia, Alzheimer's disease, and depression. Whereas ...

journal_title：Molecular pharmacology

authors： Lewis MA,Hunihan L,Franco D,Robertson B,Palmer J,Laurent DR,Balasubramanian BN,Li Y,Westphal RS

更新日期：2006-04-01 00:00:00

abstract：:The precise mechanism by which the broad-spectrum anti-RNA virus agent ribavirin elicits its in vitro antiviral effect has remained a matter of debate. We have demonstrated that inhibition of cellular inosine monophosphate dehydrogenase (IMPDH) activity, and thus depletion of intracellular GTP pools, is the predominan...

journal_title：Molecular pharmacology

authors： Leyssen P,De Clercq E,Neyts J

更新日期：2006-04-01 00:00:00

abstract：:Potassium channels play fundamental roles in physiology. Chemically diverse drugs bind in the pore region of K+ channels. Here, we homology-modeled voltage- and Ca2+-gated K+ channel BK and voltage-gated Kv1.3 using the X-ray structures of MthK and Kv1.2, respectively, and simulated the binding of d-tubocurarine in th...

journal_title：Molecular pharmacology

authors： Rossokhin A,Teodorescu G,Grissmer S,Zhorov BS

更新日期：2006-04-01 00:00:00

abstract：:Based on the available data, we speculated that changes in brain iron metabolism induced by L-DOPA might be associated with the neurotoxicity of L-DOPA. To investigate this possibility, the effects of L-DOPA on the expression of iron influx proteins [transferrin receptor (TfR) and divalent metal transporter 1 (DMT1)],...

journal_title：Molecular pharmacology

authors： Chang YZ,Ke Y,Du JR,Halpern GM,Ho KP,Zhu L,Gu XS,Xu YJ,Wang Q,Li LZ,Wang CY,Qian ZM

更新日期：2006-03-01 00:00:00

abstract：:The effects of tournefolic acid B (TAB) and two ester derivatives, TAB methyl ester (TABM) and TAB ethyl ester (TABE), on N-methyl-D-aspartate (NMDA)-mediated excitotoxicity and the underlying mechanisms were investigated. Treatment with 50 microM NMDA elicited neuronal death by 48.7 +/- 5.1%, coinciding with the appe...

journal_title：Molecular pharmacology

authors： Wang CN,Pan HC,Lin YL,Chi CW,Shiao YJ

更新日期：2006-03-01 00:00:00

abstract：:Signaling by the insulin-like growth factor (IGF)-1 receptor (IGF-1R) has been implicated in the promotion and aggressiveness of breast, prostate, colorectal, and lung cancers. The IGF binding proteins (IGFBPs) represent a class of natural IGF antagonists that bind to and sequester IGF-1/2 from the IGF-1R, making them...

journal_title：Molecular pharmacology

authors： Kibbey MM,Jameson MJ,Eaton EM,Rosenzweig SA

更新日期：2006-03-01 00:00:00

abstract：:Anandamide (AEA) and delta9-tetrahydrocannabinol (THC) are endogenous and exogenous ligands, respectively, for cannabinoid receptors. Whereas most of the pharmacological actions of cannabinoids are mediated by CB1 receptors, there is also evidence that these compounds can produce effects that are not mediated by the a...

journal_title：Molecular pharmacology

authors： Hejazi N,Zhou C,Oz M,Sun H,Ye JH,Zhang L

更新日期：2006-03-01 00:00:00

abstract：:The members of the Cys-loop ligand-gated ion channel (LGIC) gene family play a major role in fast synaptic transmission, and these receptors represent an important class of targets for therapeutic agents. Each member of this gene family is a pentameric complex containing one or more different subunits, and a large num...

journal_title：Molecular pharmacology

authors： White MM

更新日期：2006-02-01 00:00:00

abstract：:When expressed via an inducible promoter in human embryonic kidney 293 cells, the rat Mas-related gene D (rMrgD) receptor responded to beta-alanine but not L-alanine by elevating intracellular [Ca(2+)], stimulating phosphorylation of the mitogenactivated protein kinases known as extracellular signal-regulated kinase (...

journal_title：Molecular pharmacology

authors： Milasta S,Pediani J,Appelbe S,Trim S,Wyatt M,Cox P,Fidock M,Milligan G

更新日期：2006-02-01 00:00:00

abstract：:Metallothioneins (MTs) are cytoplasmic proteins that sequester certain divalent cations and are considered a primary cellular defense against the toxic transition metal cadmium (Cd(2+)). MT-I/II(-/-) knockout [MT(-/-)] cells are available and serve as an excellent tool to study non-MT-related mechanisms in metal toler...

journal_title：Molecular pharmacology

authors： Leslie EM,Liu J,Klaassen CD,Waalkes MP

更新日期：2006-02-01 00:00:00