Identification and molecular characterization of rat CXCR3: receptor expression and interferon-inducible protein-10 binding are increased in focal stroke.

abstract：:Valproic acid (VPA) is a widely used antiepileptic agent that is undergoing clinical evaluation for anticancer therapy. We assessed the effects of VPA on angiogenesis in vitro and in vivo. In human umbilical vein endothelial cells, therapeutically relevant concentrations of VPA (0.25 to 1 mM) inhibited proliferation, ...

journal_title：Molecular pharmacology

authors： Michaelis M,Michaelis UR,Fleming I,Suhan T,Cinatl J,Blaheta RA,Hoffmann K,Kotchetkov R,Busse R,Nau H,Cinatl J Jr

更新日期：2004-03-01 00:00:00

abstract：:The fluorogenic sulfhydryl probe 7-diethylamino-3-(4'-maleimidylphenyl)-4-methylcoumarin (CPM) (1-50 nM) is used to characterize the functional role and location of highly reactive thiol groups on the ryanodine-sensitive Ca2+ release channel complex [i.e., ryanodine receptors (RyRs)] of skeletal and cardiac junctional...

journal_title：Molecular pharmacology

authors： Liu G,Abramson JJ,Zable AC,Pessah IN

更新日期：1994-02-01 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：:Five separate guanine nucleotide-binding proteins (G proteins) were immunologically identified in membranes from neuroblastoma x glioma NG108-15 hybrid cells. These alpha subunit proteins were Gi2 alpha, two isoforms of Gi3 alpha, and two isoforms of Go alpha. The G proteins that interacted with delta-opioid receptors...

journal_title：Molecular pharmacology

authors： Roerig SC,Loh HH,Law PY

更新日期：1992-05-01 00:00:00

abstract：:Prostaglandin E(2) (PGE(2)), originally discovered as a pro-inflammatory mediator, also inhibits several chemoattractant-elicited neutrophil functions, including adhesion, secretion of cytotoxic enzymes, production of superoxide anions, and chemotaxis. In this study, we have examined the effects of PGE(2) and prostagl...

journal_title：Molecular pharmacology

authors： Burelout C,Thibault N,Levasseur S,Simard S,Naccache PH,Bourgoin SG

更新日期：2004-08-01 00:00:00

abstract：:We used transcript-specific oligonucleotides to examine the localization in the rat nervous system of the corresponding mRNAs for the two P2X purinoceptor genes cloned recently from the rat vas deferens and PC12 cells. PC12 P2X purinoceptor mRNA was labeled in the olfactory tubercle, striatum, hypothalamus, hippocampu...

journal_title：Molecular pharmacology

authors： Kidd EJ,Grahames CB,Simon J,Michel AD,Barnard EA,Humphrey PP

更新日期：1995-10-01 00:00:00

abstract：:NS20Y neuroblastoma cells expressing a homogeneous population of D1-dopamine receptors were used in the present study as a model system to investigate the mechanisms of agonist-induced stimulation and desensitization of D1 receptor-coupled adenylyl cyclase activity. Membrane prepared from NS20Y cells showed a pharmaco...

journal_title：Molecular pharmacology

authors： Barton AC,Sibley DR

更新日期：1990-10-01 00:00:00

abstract：:The induction of human inducible nitric-oxide synthase (iNOS) expression depends (among other factors) on activation of the signal transducer and activator of transcription 1 (STAT1) pathway. Therefore, the STAT1 pathway may be an appropriate target for the development of inhibitors of iNOS expression. HeLa S3 cells t...

journal_title：Molecular pharmacology

authors： Yao Y,Hausding M,Erkel G,Anke T,Förstermann U,Kleinert H

更新日期：2003-02-01 00:00:00

abstract：:Aspartyl aminopeptidase (DNPEP) has been implicated in the control of angiotensin signaling and endosome trafficking, but its precise biologic roles remain incompletely defined. We performed a high-throughput screen of ∼25,000 small molecules to identify inhibitors of DNPEP for use as tools to study its biologic funct...

journal_title：Molecular pharmacology

authors： Chen Y,Tang H,Seibel W,Papoian R,Oh K,Li X,Zhang J,Golczak M,Palczewski K,Kiser PD

更新日期：2014-08-01 00:00:00

abstract：:Inhibitors of the serotonin transporter (SERT) are widely used antidepressant agents, but the structural mechanism for inhibitory activity and selectivity over the closely related norepinephrine transporter (NET) is not well understood. Here we use a combination of chemical, biological, and computational methods to de...

journal_title：Molecular pharmacology

authors： Andersen J,Stuhr-Hansen N,Zachariassen LG,Koldsø H,Schiøtt B,Strømgaard K,Kristensen AS

更新日期：2014-05-01 00:00:00

abstract：:Retina from 1-day-old chicks is a valuable tissue model for studying neuronal nicotinic receptors because it expresses a large number of the developmentally regulated high affinity [(3)H]epibatidine labeled nicotinic receptors. Most of these receptors contain the beta4 subunit associated with different alpha subunits....

journal_title：Molecular pharmacology

authors： Barabino B,Vailati S,Moretti M,McIntosh JM,Longhi R,Clementi F,Gotti C

更新日期：2001-06-01 00:00:00

abstract：:Prolonged ethanol exposure causes central nervous system hyperexcitability that involves a loss of GABAergic inhibition. We previously demonstrated that long-term ethanol exposure enhances the internalization of synaptic GABA(A) receptors composed of alpha1beta2/3gamma2 subunits. However, the mechanisms of ethanol-med...

journal_title：Molecular pharmacology

authors： Kumar S,Suryanarayanan A,Boyd KN,Comerford CE,Lai MA,Ren Q,Morrow AL

更新日期：2010-05-01 00:00:00

abstract：:The therapeutic potential of antitumor drugs is seriously limited by the manifestation of cellular drug resistance. We used the budding yeast Saccharomyces cerevisiae as a model system to identify novel mechanisms of resistance to one of the most active anticancer agents, cisplatin. We pinpointed NPR2 (nitrogen permea...

journal_title：Molecular pharmacology

authors： Schenk PW,Brok M,Boersma AW,Brandsma JA,Den Dulk H,Burger H,Stoter G,Brouwer J,Nooter K

更新日期：2003-08-01 00:00:00

abstract：:A functional interaction between peroxisome proliferator-activated receptor alpha (PPARalpha) and components of the circadian clock has been suggested, but whether these transcriptional factors interact to regulate the expression of their target genes remains obscure. Here we used a PPARalpha ligand, bezafibrate, to s...

journal_title：Molecular pharmacology

authors： Oishi K,Koyanagi S,Matsunaga N,Kadota K,Ikeda E,Hayashida S,Kuramoto Y,Shimeno H,Soeda S,Ohdo S

更新日期：2010-07-01 00:00:00

abstract：:We have previously reported that endocytic sorting of ET(A) endothelin receptors to the recycling pathway is dependent on a signal residing in the cytoplasmic carboxyl-terminal region. The aim of the present work was to characterize the carboxyl-terminal recycling motif of the ET(A) receptor. Assay of truncation mutan...

journal_title：Molecular pharmacology

authors： Paasche JD,Attramadal T,Kristiansen K,Oksvold MP,Johansen HK,Huitfeldt HS,Dahl SG,Attramadal H

更新日期：2005-05-01 00:00:00

abstract：:Several novel phenylaminotetralins (PATs) cause functional changes in brain that are associated with binding to saturable, high affinity sites that are not identical to any known central nervous system receptor. These PATs were tested for their ability to cause receptor-mediated functional effects on tyrosine hydroxyl...

journal_title：Molecular pharmacology

authors： Booth RG,Wyrick SD,Baldessarini RJ,Kula NS,Myers AM,Mailman RB

更新日期：1993-12-01 00:00:00

abstract：:The N-methyl-D-aspartate (NMDA) receptor is believed to play a major role in learning and in excitotoxic neuronal damage associated with stroke and epilepsy. Pregnenolone sulfate, a neurosteroid, specifically enhances NMDA-gated currents in spinal cord neurons, while inhibiting receptors for the inhibitory amino acids...

journal_title：Molecular pharmacology

authors： Wu FS,Gibbs TT,Farb DH

更新日期：1991-09-01 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：:The anticancer agent 2-cyano-3,12-dioxooleana-1,9-dien-28-oic acid (CDDO) and its methyl ester (CDDO-Me) typically induce a broad spectrum of growth-inhibitory, proapoptotic, and antiangiogenic responses. Treatment of Panc1, Panc28, and L3.6pL pancreatic cancer cells with low micromolar concentrations of CDDO or CDDO-...

journal_title：Molecular pharmacology

authors： Jutooru I,Chadalapaka G,Abdelrahim M,Basha MR,Samudio I,Konopleva M,Andreeff M,Safe S

更新日期：2010-08-01 00:00:00

abstract：:Neuroactive steroids are efficacious potentiators of GABA-A receptors. Recent work has identified a site in the alpha1 subunit of the GABA-A receptor, that is essential for potentiation by steroids. However, each receptor contains two copies of the alpha1 subunit. We generated concatemers of subunits so that the alpha...

journal_title：Molecular pharmacology

authors： Bracamontes JR,Steinbach JH

更新日期：2009-04-01 00:00:00

abstract：:Freshly isolated rat hepatocytes rapidly lose their cytochrome P450 (P450) proteins and mRNAs, with no evidence of subsequent restoration, after placement into traditional systems of primary culture on type I collagen. We examined the patterns of expression of 10 constitutively expressed P450 mRNAs in rat hepatocytes ...

journal_title：Molecular pharmacology

authors： Kocarek TA,Schuetz EG,Guzelian PS

更新日期：1993-03-01 00:00:00

abstract：:The local anesthetic-like Na+ channel-blocking drug [3H]PD85639 [alpha-([4-3H]phenyl)-N-[3-(2,6-dimethyl-1-piperizinyl)-alpha-prop yl] [4-3H]benzeneacetamide] binds specifically to receptor sites on Na+ channels in intact synaptosomes and synaptosomal membranes, purified and reconstituted Na+ channels, and type IIA Na...

journal_title：Molecular pharmacology

authors： Thomsen W,Hays SJ,Hicks JL,Schwarz RD,Catterall WA

更新日期：1993-06-01 00:00:00

abstract：:Sazetidine-A has been recently proposed to be a "silent desensitizer" of alpha4beta2 nicotinic acetylcholine receptors (nAChRs), implying that it desensitizes alpha4beta2 nAChRs without first activating them. This unusual pharmacological property of sazetidine-A makes it, potentially, an excellent research tool to dis...

journal_title：Molecular pharmacology

authors： Zwart R,Carbone AL,Moroni M,Bermudez I,Mogg AJ,Folly EA,Broad LM,Williams AC,Zhang D,Ding C,Heinz BA,Sher E

更新日期：2008-06-01 00:00:00

abstract：:Regulator of G protein signaling (RGS) proteins accelerate the endogenous GTPase activity of Galpha(i/o) proteins to increase the rate of deactivation of active Galpha-GTP and Gbetagamma signaling molecules. Previous studies have suggested that RGS proteins are more effective on less efficiently coupled systems such a...

journal_title：Molecular pharmacology

authors： Clark MJ,Linderman JJ,Traynor JR

更新日期：2008-05-01 00:00:00

abstract：:Tetradecyl 2,3-dihydroxybenzoate (ABG-001) is a lead compound derived from neuritogenic gentisides. In the present study, we investigated the mechanism by which ABG-001 induces neurite outgrowth in a rat adrenal pheochromocytoma cell line (PC12). Inhibitors of insulin-like growth factor 1 (IGF-1) receptor, phosphatidy...

journal_title：Molecular pharmacology

authors： Tang R,Gao L,Kawatani M,Chen J,Cao X,Osada H,Xiang L,Qi J

更新日期：2015-08-01 00:00:00

abstract：:Anaplastic thyroid carcinoma (ATC) is among the most aggressive malignancies known and is characterized with rapid growth, early invasion, and complete refractoriness to current therapies. Here we report that triptolide, a small molecule from a Chinese herb, could potently inhibit proliferation in vitro, angiogenesis ...

journal_title：Molecular pharmacology

authors： Zhu W,Ou Y,Li Y,Xiao R,Shu M,Zhou Y,Xie J,He S,Qiu P,Yan G

更新日期：2009-04-01 00:00:00

abstract：:Reversal of the multidrug-resistant (MDR) phenotype is very important for chemotherapy success. In fact, the expression of the MDR1 gene-encoded P-glycoprotein (P-gp) actively expels antitumor agents such as daunomycin (DNM) out of the cells, resulting in drug resistance. We show that upon conjugation to triplex-formi...

journal_title：Molecular pharmacology

authors： Stierlé V,Duca M,Halby L,Senamaud-Beaufort C,Capobianco ML,Laigle A,Jollès B,Arimondo PB

更新日期：2008-05-01 00:00:00

abstract：:The 2,3,7,8-tetrachlorodibenzo-p-dioxin-transformed aryl hydrocarbon receptor (AHR) complex binds to xenobiotic-responsive element (XRE) sequences in the 5' flanking region of the CYP1A1 gene, resulting in initiation of transcription. Both components of the transformed AHR complex [the ligand-binding AHR monomer and t...

journal_title：Molecular pharmacology

authors： Bacsi SG,Reisz-Porszasz S,Hankinson O

更新日期：1995-03-01 00:00:00

abstract：:Novel methods of detecting and quantitating cooperative interactions between an agent and both a tritiated (muscarinic) antagonist and the endogenous agonist (acetylcholine), acting at a common (muscarinic) receptor, have been devised. In a semiquantitative protocol, binding data are transformed into affinity ratios (...

journal_title：Molecular pharmacology

authors： Lazareno S,Birdsall NJ

更新日期：1995-08-01 00:00:00

abstract：:The molecular determinants of high-affinity human ether-a-go-go-related gene (HERG) potassium channel blockade by methanesulfonanilides include two aromatic residues (Phe656 and Tyr652) on the inner helices (S6) and residues on the pore helices that face into the inner cavity, but determinants for lower-affinity HERG ...

journal_title：Molecular pharmacology

authors： Witchel HJ,Dempsey CE,Sessions RB,Perry M,Milnes JT,Hancox JC,Mitcheson JS

更新日期：2004-11-01 00:00:00