Synergy between coproduced CC and CXC chemokines in monocyte chemotaxis through receptor-mediated events.

abstract：:The human dopamine and norepinephrine transporters (hDAT and hNET, respectively) control neurotransmitter levels within the synaptic cleft and are the site of action for amphetamine (AMPH) and cocaine. We investigated the role of a threonine residue within the highly conserved and putative phosphorylation sequence RET...

journal_title：Molecular pharmacology

authors： Guptaroy B,Fraser R,Desai A,Zhang M,Gnegy ME

更新日期：2011-03-01 00:00:00

abstract：:Differential display reverse transcription-polymerase chain reaction was used to identify mRNAs that are differentially expressed in the brain of rats treated chronically with the reference tricyclic antidepressant, imipramine, in comparison with control rats. The gene encoding for a mutation suppressor for Sec4-8 yea...

journal_title：Molecular pharmacology

authors： Andriamampandry C,Muller C,Schmidt-Mutter C,Gobaille S,Spedding M,Aunis D,Maitre M

更新日期：2002-12-01 00:00:00

abstract：:Intermediate-conductance (KCa3.1) and small-conductance (KCa2) calcium-activated K+ channels are gated by calcium binding to calmodulin (CaM) molecules associated with the calmodulin-binding domain (CaM-BD) of these channels. The existing KCa activators, such as naphtho[1,2-d]thiazol-2-ylamine (SKA-31), 6,7-dichloro-1...

journal_title：Molecular pharmacology

authors： Brown BM,Shim H,Zhang M,Yarov-Yarovoy V,Wulff H

更新日期：2017-10-01 00:00:00

abstract：:A site-directed alkylating agent was used to inactivate one or more types of opioid receptor in two bioassay preparations in the presence of type-selective ligands as protectors of other opioid receptor types. Since the pharmacological potency of an agonist is decreased when the receptor type through which it acts has...

journal_title：Molecular pharmacology

authors： Goldstein A,James IF

更新日期：1984-05-01 00:00:00

abstract：:Squamous cell carcinoma of the head and neck (SCCHN) is one of the most common malignancies worldwide, with low 5-year survival rates. Current strategies that block epidermal growth factor receptor (EGFR) have limited effects when administered as single agents. Targeting EGFR via intratumoral administration of phospho...

journal_title：Molecular pharmacology

authors： Thomas SM,Ogagan MJ,Freilino ML,Strychor S,Walsh DR,Gooding WE,Grandis JR,Zamboni WC

更新日期：2008-03-01 00:00:00

abstract：:Inhibition of cathepsin C, a dipeptidyl peptidase that activates many serine proteases, represents an attractive therapeutic strategy for inflammatory diseases with a high neutrophil burden. We recently showed the feasibility of blocking the activation of neutrophil elastase, cathepsin G, and proteinase-3 with a singl...

journal_title：Molecular pharmacology

authors： Méthot N,Guay D,Rubin J,Ethier D,Ortega K,Wong S,Normandin D,Beaulieu C,Reddy TJ,Riendeau D,Percival MD

更新日期：2008-06-01 00:00:00

abstract：:The nonselective cation channel TRPA1 (ANKTM1, p120) is a potential mediator of pain, and selective pharmacological modulation of this channel may be analgesic. Although several TRPA1 activators exist, these tend to be either reactive or of low potency and/or selectivity. The aim of the present study, therefore, was t...

journal_title：Molecular pharmacology

authors： Maher M,Ao H,Banke T,Nasser N,Wu NT,Breitenbucher JG,Chaplan SR,Wickenden AD

更新日期：2008-04-01 00:00:00

abstract：:A high cytoplasmic Na(+) concentration may contribute to N-methyl-D-aspartate (NMDA)-induced excitotoxicity by promoting Ca(2+) influx via reverse operation of the Na(+)/Ca(2+) exchanger (NaCaX), but may simultaneously decrease the electrochemical Ca(2+) driving force by depolarizing the plasma membrane (PM). Digital ...

journal_title：Molecular pharmacology

authors： Kiedrowski L

更新日期：1999-09-01 00:00:00

abstract：:Several lines of evidence suggest that G-protein-coupled receptors can adopt different active conformations, but their direct demonstration in intact cells is still missing. Using a fluorescence resonance energy transfer (FRET)-based approach we studied conformational changes in alpha(2A)-adrenergic receptors in intac...

journal_title：Molecular pharmacology

authors： Zürn A,Zabel U,Vilardaga JP,Schindelin H,Lohse MJ,Hoffmann C

更新日期：2009-03-01 00:00:00

abstract：:Understanding the structures of active and inactive agonist- and antagonist-bound receptor complexes is of great interest. In this work, we focus on position 30 of cholecystokinin (CCK) and its spatial approximation with the type A CCK receptor. For this, we developed two photoaffinity labeling probes, replacing the n...

journal_title：Molecular pharmacology

authors： Dong M,Hadac EM,Pinon DI,Miller LJ

更新日期：2005-06-01 00:00:00

abstract：:We have studied the molecular mechanism by which the nuclear xenobiotic receptors pregnane X receptor (PXR) and constitutive active/androstane receptor (CAR) regulate transcription of the vitamin D(3) 24-hydroxylase (CYP24A1) gene. In the absence of vitamin D(3), PXR activates the CYP24A1 gene by directly binding to a...

journal_title：Molecular pharmacology

authors： Konno Y,Kodama S,Moore R,Kamiya N,Negishi M

更新日期：2009-02-01 00:00:00

abstract：:The effects of ethanol on a number of electrophysiological parameters were examined in 10 different voltage-gated potassium channels expressed in Xenopus oocytes. None of the channels examined was highly sensitive to ethanol, but there was significant variability among the channels tested at concentrations of ethanol ...

journal_title：Molecular pharmacology

authors： Anantharam V,Bayley H,Wilson A,Treistman SN

更新日期：1992-09-01 00:00:00

abstract：:The effect of breast cancer resistance protein (Bcrp/Abcg2) on the disposition of the phytoestrogens daidzein, genistein, and coumestrol was investigated using Bcrp(-/-) mice. Expression of the genes for either mouse Bcrp or human BCRP in MDCK II cells induced apically directed transport of the three phytoestrogens, w...

journal_title：Molecular pharmacology

authors： Enokizono J,Kusuhara H,Sugiyama Y

更新日期：2007-10-01 00:00:00

abstract：:Effects of pimaric acid (PiMA) and eight closely related compounds on large-conductance K(+) (BK) channels were examined using human embryonic kidney (HEK) 293 cells, in which either the alpha subunit of BK channel (HEKBKalpha) or both alpha and beta1 (HEKBKalphabeta1) subunits were heterologously expressed. Effects o...

journal_title：Molecular pharmacology

authors： Imaizumi Y,Sakamoto K,Yamada A,Hotta A,Ohya S,Muraki K,Uchiyama M,Ohwada T

更新日期：2002-10-01 00:00:00

abstract：:alpha 1-Adrenergic receptor (alpha 1-AR) agonists elevate the intracellular calcium concentration ([Ca2+]i) in 60-80% of astroglia in vitro. Likewise, 60-70% of astroglia exhibit specific binding sites for the alpha 1-AR-selective antagonist (+-)-125I-[beta-(4-hydroxyphenyl)-ethylaminomethyl]tetralone. The density of ...

journal_title：Molecular pharmacology

authors： Shao Y,McCarthy KD

更新日期：1993-08-01 00:00:00

abstract：:Guinea pig lung microsomes converted arachidonic acid (AA) to two classes of cytochrome P450 (P450)-dependent metabolites, 16- through 20-hydroxyeicosatetraenoic acids [(16-20)-OH-AA] and epoxyeicosatrienoic acids (EETs). The rate of formation of (16-20)-OH-AA was approximately 3-fold higher in microsomes from beta-na...

journal_title：Molecular pharmacology

authors： Knickle LC,Bend JR

更新日期：1994-06-01 00:00:00

abstract：:The relations between the single high affinity binding sites for azapropazone, phenylbutazone, chlorpropamide, sulfathiazole, and iophenoxate and the binding regions of human serum albumin represented by the marker ligands diazepam, phenol red, salicylate, and warfarin were examined by a series of competition experime...

journal_title：Molecular pharmacology

authors： Kragh-Hansen U

更新日期：1988-08-01 00:00:00

abstract：:The aptamer mechanism of action involves the direct interaction of oligonucleotide with protein and is responsible for the biological effects of many pharmacologically active oligodeoxynucleotides. In the work reported here, we have determined the effects of aptamers on the secondary, tertiary, and quaternary structur...

journal_title：Molecular pharmacology

authors： Balasubramanian V,Nguyen LT,Balasubramanian SV,Ramanathan M

更新日期：1998-05-01 00:00:00

abstract：:Bioassay-guided fractionation was used to isolate the lignan polygamain as the microtubule-active constituent in the crude extract of the Mountain torchwood, Amyris madrensis. Similar to the effects of the crude plant extract, polygamain caused dose-dependent loss of cellular microtubules and the formation of aberrant...

journal_title：Molecular pharmacology

authors： Hartley RM,Peng J,Fest GA,Dakshanamurthy S,Frantz DE,Brown ML,Mooberry SL

更新日期：2012-03-01 00:00:00

abstract：:Transmembrane domain 6 of the muscarinic acetylcholine (ACh) receptors is important in ligand binding and in the conformational transitions of the receptor but the roles of individual residues are poorly understood. We have carried out a systematic alanine-scanning mutagenesis study on residues Tyr381 to Val387 within...

journal_title：Molecular pharmacology

authors： Ward SD,Curtis CA,Hulme EC

更新日期：1999-11-01 00:00:00

abstract：:We demonstrated previously that the nucleoside of fludarabine (F-ara-A), a clinically effective agent against chronic lymphocytic leukemia and low-grade lymphoma, produces synergistic cytotoxicity against cisplatin-resistant CP2.0 human colon tumor cells when administered in combination with cisplatin. The purpose of ...

journal_title：Molecular pharmacology

authors： Li L,Keating MJ,Plunkett W,Yang LY

更新日期：1997-11-01 00:00:00

abstract：:High-throughput screening has led to the identification of small-molecule blockers of the cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel, but the structural basis of blocker binding remains to be defined. We developed molecular models of the CFTR channel on the basis of homology to the bac...

journal_title：Molecular pharmacology

authors： Norimatsu Y,Ivetac A,Alexander C,O'Donnell N,Frye L,Sansom MS,Dawson DC

更新日期：2012-12-01 00:00:00

abstract：:The Gαi/o-coupled dopamine D2-like receptor family comprises three subtypes: the D2 receptor (D2R), with short and long isoform variants (D2SR and D2LR), D3 receptor (D3R), and D4 receptor (D4R), with several polymorphic variants. The common overlap of norepinephrine innervation and D2-like receptor expression pattern...

journal_title：Molecular pharmacology

authors： Sánchez-Soto M,Bonifazi A,Cai NS,Ellenberger MP,Newman AH,Ferré S,Yano H

更新日期：2016-04-01 00:00:00

abstract：:2,3,7,8-Tetrachlorodibenzo-p-dioxin (TCDD), beta-naphthoflavone (beta NF), and phenobarbital (PB) cause marked induction of cytochrome P-450 (P-450)-mediated arachidonic acid metabolism in chick embryo liver. We show here that the P-450 arachidonic acid epoxygenases induced by TCDD and beta NF are immunochemically ind...

journal_title：Molecular pharmacology

authors： Kanetoshi A,Ward AM,May BK,Rifkind AB

更新日期：1992-12-01 00:00:00

abstract：:Activation of muscarinic cholinergic receptors of 1321N1 human astrocytoma cells attenuates cyclic AMP accumulation. This effect results from an activation of phosphodiesterase with no direct inhibition of adenylate cyclase activity. In spite of this lack of coupling of muscarinic receptors to adenylate cyclase, guani...

journal_title：Molecular pharmacology

authors： Evans T,Martin MW,Hughes AR,Harden TK

更新日期：1985-01-01 00:00:00

abstract：:The effect of mercuric acetate on the activities of deoxyuridine triphosphate nucleotidohydrolase (dUTPase), DNA polymerase (alpha, beta), and uracil-DNA glycosylase has been studied in cultured human KB cells. There was a dose- and time-dependent inactivation of both dUTPase and DNA polymerase alpha activities by mer...

journal_title：Molecular pharmacology

authors： Williams MV,Winters T,Waddell KS

更新日期：1987-02-01 00:00:00

abstract：:[3H]Dihydroalprenolol ([3H]DHA) has been used extensively in receptor binding studies to measure beta-adrenergic receptors in the central nervous system. Usually, nonspecific binding has been defined by high concentrations of the beta-adrenergic receptor agonist isoproterenol or antagonists such as alprenolol or propr...

journal_title：Molecular pharmacology

authors： Riva MA,Creese I

更新日期：1989-07-01 00:00:00

abstract：:Multidrug resistance protein (MRP) 4 transports a variety of endogenous and xenobiotic organic anions. MRP4 is widely expressed in the body and specifically localized to the renal apical proximal tubule cell membrane, where it mediates the excretion of these compounds into urine. To characterize the MRP4 substrate-bin...

journal_title：Molecular pharmacology

authors： El-Sheikh AA,van den Heuvel JJ,Krieger E,Russel FG,Koenderink JB

更新日期：2008-10-01 00:00:00

abstract：:Epoxyeicosatrienoic acids (EETs), products of the cytochrome P-450 monooxygenase metabolism of arachidonic acid, can regulate the activity of ion channels. We examined the effects of EETs on cardiac L-type Ca2+ channels that play important roles in regulating cardiac contractility, controlling heart rate, and mediatin...

journal_title：Molecular pharmacology

authors： Chen J,Capdevila JH,Zeldin DC,Rosenberg RL

更新日期：1999-02-01 00:00:00

abstract：:Cytosolic sulfotransferase 1C3 (SULT1C3) is the least characterized of the three human SULT1C subfamily members. Originally identified as an orphan SULT by computational analysis of the human genome, we recently reported that SULT1C3 is expressed in human intestine and LS180 colorectal adenocarcinoma cells and is upre...

journal_title：Molecular pharmacology

authors： Dubaisi S,Fang H,Kocarek TA,Runge-Morris M

更新日期：2016-11-01 00:00:00