Post-transcriptional control of human ether-a-go-go-related gene potassium channel protein by alpha-adrenergic receptor stimulation.

abstract：:We synthesized a novel platinum drug, cis-[PtCl(NH3)2(N7-ACV)]+, in which ACV is the antiviral drug acyclovir [a deoxyriboguanosine analogue, 9-(2-hydroxyethoxymethyl)guanine]. This new compound exhibits antiviral efficacy in vitro and exhibits an antitumor activity profile different from that of cisplatin [Metal-Base...

journal_title：Molecular pharmacology

authors： Balcarová Z,Kaspárková J,Zákovská A,Nováková O,Sivo MF,Natile G,Brabec V

更新日期：1998-05-01 00:00:00

abstract：:Phosphorylation of tau protein promotes stability of the axonal cytoskeleton; aberrant tau phosphorylation is implicated in the biogenesis of paired helical filaments (PHF) seen in Alzheimer's disease. Protein kinases and phosphatases that modulate tau phosphorylation have been identified using in vitro techniques; ho...

journal_title：Molecular pharmacology

authors： Garver TD,Kincaid RL,Conn RA,Billingsley ML

更新日期：1999-04-01 00:00:00

abstract：:Three different cDNA clones, namely DM1-1, Dah1, and Dah2, encoding hepatic cytochrome P-450, were isolated from a cDNA library in lambda gt11 constructed from liver RNA of polychlorinated biphenyl-treated beagle dogs. DM1-1 was 1857 base pairs (bp) long and encoded a polypeptide of 457 residues. Dah1 was 2394 bp long...

journal_title：Molecular pharmacology

authors： Uchida T,Komori M,Kitada M,Kamataki T

更新日期：1990-11-01 00:00:00

abstract：:The heart is richly endowed with K(ATP) channels, which function as biological sensors, regulating membrane potentials and electrical excitability in response to metabolic alterations. We recently reported that the cytochrome P450 metabolites of arachidonic acid, epoxyeicosatrienoic acids (EETs), potently activate car...

journal_title：Molecular pharmacology

authors： Lu T,VanRollins M,Lee HC

更新日期：2002-11-01 00:00:00

abstract：:Organic anion transporting polypeptides (Oatp) mediate the transport of a wide variety of amphipathic organic substrates. Rat Oatp1b2 and human OATP1B3 are members of a liver-specific subfamily of Oatps/OATPs. We investigated whether prolactin (PRL) and growth hormone (GH) regulated Oatp1b2 and OATP1B3 gene expression...

journal_title：Molecular pharmacology

authors： Wood M,Ananthanarayanan M,Jones B,Wooton-Kee R,Hoffman T,Suchy FJ,Vore M

更新日期：2005-07-01 00:00:00

abstract：:Drug-induced plasticity of excitatory synapses has been proposed to be the cellular mechanism underlying the aberrant learning associated with addiction. Exposure to various drugs of abuse causes both morphological plasticity of dendritic spines and functional plasticity of excitatory synaptic transmission. Chronic ac...

journal_title：Molecular pharmacology

authors： Miller EC,Zhang L,Dummer BW,Cariveau DR,Loh H,Law PY,Liao D

更新日期：2012-08-01 00:00:00

abstract：:A substantial body of research implicates L-cysteine sulfinic acid (L-CSA) as a neurotransmitter. However, all physiological actions of L-CSA that have been pharmacologically characterized are mediated by cross-activation of glutamate receptors, and no receptor has been identified that is primarily activated by L-CSA....

journal_title：Molecular pharmacology

authors： Boss V,Nutt KM,Conn PJ

更新日期：1994-06-01 00:00:00

abstract：:Targeted inhibition of oncogenes in tumor cells is a rational approach toward the development of cancer therapies based on RNA interference (RNAi). Tumors caused by human papillomavirus (HPV) infection are an ideal model system for RNAi-based cancer therapies because the oncogenes that cause cervical cancer, E6 and E7...

journal_title：Molecular pharmacology

authors： Putral LN,Bywater MJ,Gu W,Saunders NA,Gabrielli BG,Leggatt GR,McMillan NA

更新日期：2005-11-01 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：:Low-density lipoprotein (LDL) is known to be a mitogenic factor for vascular smooth muscle cells (VSMCs), fibroblasts, and endothelial cells. In the current study, we describe possible intracellular mechanisms by which LDL elicits its mitogenic effects. Stimulation of VSMCs with LDL resulted in a pertussis-toxin (PTX)...

journal_title：Molecular pharmacology

authors： Sachinidis A,Seewald S,Epping P,Seul C,Ko Y,Vetter H

更新日期：1997-09-01 00:00:00

abstract：:As noted previously, in N1E-115 neuroblastoma cells, carbamylcholine, a muscarinic cholinergic agonist, increased cGMP over 15-fold and decreased basal and prostaglandin E1 (PGE1)-stimulated cAMP content. In contrast to the stimulatory effects of PGE1 on cAMP, which were immediate, the carbamylcholine-induced decrease...

journal_title：Molecular pharmacology

authors： Bruni P,Burns DL,Hewlett EL,Moss J

更新日期：1985-08-01 00:00:00

abstract：:We compared the efficiencies with which human alpha 1-adrenergic receptor (AR) subtypes activate inositol phosphate (InsP) formation and increase intracellular Ca2+ in transfected cell lines. Expression of human alpha 1a-, alpha 1b-, and alpha 1d-AR cDNAs under the repressible control of anhydrotetracycline in human e...

journal_title：Molecular pharmacology

authors： Theroux TL,Esbenshade TA,Peavy RD,Minneman KP

更新日期：1996-11-01 00:00:00

abstract：:The new olivacine derivative S16020-2 (NSC-659687) is a DNA topoisomerase II inhibitor endowed with a remarkable antitumor activity against various experimental tumors. In vitro physicochemical properties of this compound, in particular its interaction with DNA and DNA topoisomerase II, were very similar to those of e...

journal_title：Molecular pharmacology

authors： Le Mée S,Chaminade F,Delaporte C,Markovits J,Saucier JM,Jacquemin-Sablon A

更新日期：2000-10-01 00:00:00

abstract：:Controlled inhibition of brain acetyl- and butyrylcholinesterases (AChE and BChE, respectively) and of monoamine oxidase-B (MAO-B) may slow neurodegeneration in Alzheimer's and Parkinson's diseases. It was postulated that certain carbamate esters would inhibit AChE and BChE with the concomitant release in the brain of...

journal_title：Molecular pharmacology

authors： Groner E,Ashani Y,Schorer-Apelbaum D,Sterling J,Herzig Y,Weinstock M

更新日期：2007-06-01 00:00:00

abstract：:The congenital long QT syndrome is an inherited disorder characterized by a delay in cardiac repolarization, leading to lethal cardiac arrhythmias such as torsade de pointes. One form of this disease involves mutations in the voltage-dependent cardiac Na(+) channel, which includes an in-frame deletion of three amino a...

journal_title：Molecular pharmacology

authors： Ono K,Kaku T,Makita N,Kitabatake A,Arita M

更新日期：2000-02-01 00:00:00

abstract：:The effect of the thiol-alkylating agent, N-ethylmaleimide (NEM), on histamine (HA) H1-receptors from guinea pig cerebellum, labeled with [3H]mepyramine, was investigated. The properties of [3H]mepyramine binding (apparent dissociation constant and maximal number of sites) were not modified by prior treatment of the m...

journal_title：Molecular pharmacology

authors： Yeramian E,Garbarg M,Schwartz JC

更新日期：1985-08-01 00:00:00

abstract：:Increasing evidence implicates apoptosis as a major mechanism of cell death in methamphetamine (METH) neurotoxicity. The involvement of a neuroimmune component in apoptotic cell death after injury or chemical damage suggests that cytokines may play a role in METH effects. In the present study, we examined if the absen...

journal_title：Molecular pharmacology

authors： Ladenheim B,Krasnova IN,Deng X,Oyler JM,Polettini A,Moran TH,Huestis MA,Cadet JL

更新日期：2000-12-01 00:00:00

abstract：:G protein-coupled receptor kinases (GRKs) play a key role in the process of receptor homologous desensitization. In the present study, we address the question of whether a variety of receptors coupled to different G protein subtypes and naturally expressed on the same cell are selectively regulated by GRK2. The signal...

journal_title：Molecular pharmacology

authors： Iacovelli L,Franchetti R,Grisolia D,De Blasi A

更新日期：1999-08-01 00:00:00

abstract：:Neuronal cell lines provide a source of pure populations of neurons and allow the properties of many neurotransmitter receptors to be studied. However, none of these cells have been reported to express functional gamma-aminobutyric acid (GABA)A receptors. Indeed, there have been no reports of cell lines expressing fun...

journal_title：Molecular pharmacology

authors： Hales TG,Kim H,Longoni B,Olsen RW,Tobin AJ

更新日期：1992-08-01 00:00:00

abstract：:All five (m1-m5) muscarinic receptors are sensitive to allosteric regulation, but gallamine is considerably more potent in slowing the dissociation of N-[3H]methylscopolamine (NMS) from the m2 subtype than from the m3 or m5 subtypes. To study the structural basis for the preference of gallamine for the m2 subtype, we ...

journal_title：Molecular pharmacology

authors： Ellis J,Seidenberg M,Brann MR

更新日期：1993-09-01 00:00:00

abstract：:In the rat isolated optic nerve, nitric oxide (NO) activates soluble guanylyl cyclase (sGC), resulting in a selective accumulation of cGMP in the axons. The axons are also selectively vulnerable to NO toxicity. The experiments initially aimed to determine any causative link between these two effects. It was shown, usi...

journal_title：Molecular pharmacology

authors： Garthwaite G,Goodwin DA,Neale S,Riddall D,Garthwaite J

更新日期：2002-01-01 00:00:00

abstract：:Inhibition of multidrug resistance protein 1 (MRP1) mediated cytostatic drug efflux might be useful in the treatment of drug resistant tumors. Because the glutathione (GSH) conjugate of ethacrynic acid (EA), GS-EA, is a good substrate of MRP1, GS-EA derivatives are expected to be good inhibitors of MRP1. To study stru...

journal_title：Molecular pharmacology

authors： Burg D,Wielinga P,Zelcer N,Saeki T,Mulder GJ,Borst P

更新日期：2002-11-01 00:00:00

abstract：:Camptothecin (CPT) is an effective chemotherapeutic agent for treatment of patients with cancer. The mechanisms underlying CPT-mediated responses in cancer cells are not fully understood. MicroRNA (miRNA) play important roles in tumorigenesis and drug sensitivity. However, the interaction between camptothecin and miRN...

journal_title：Molecular pharmacology

authors： Zeng CW,Zhang XJ,Lin KY,Ye H,Feng SY,Zhang H,Chen YQ

更新日期：2012-04-01 00:00:00

abstract：:Prior studies indicate that adenosine and the adenosine A2A receptor play a role in hepatic fibrosis by a mechanism that has been proposed to involve direct stimulation of hepatic stellate cells (HSCs). The objective of this study was to determine whether primary hepatic stellate cells produce collagen in response to ...

journal_title：Molecular pharmacology

authors： Che J,Chan ES,Cronstein BN

更新日期：2007-12-01 00:00:00

abstract：:The human histamine H(4)-receptor (hH(4)R) possesses high constitutive activity and, like the human H(1)-receptor (hH(1)R), is involved in the pathogenesis of type-I allergic reactions. The study aims were to explore the value of dual H(1)/H(4)R antagonists as antiallergy drugs and to address the question of whether H...

journal_title：Molecular pharmacology

authors： Deml KF,Beermann S,Neumann D,Strasser A,Seifert R

更新日期：2009-11-01 00:00:00

abstract：:The phosphatidylcholine-using phospholipase D (PLD) isoform PLD2 is widely expressed in mammalian cells and is activated in response to a variety of promitogenic agonists. In this study, active and inactive hemagglutinin-tagged human PLD2 (HA-PLD2) constructs were stably expressed in an EL4 cell line lacking detectabl...

journal_title：Molecular pharmacology

authors： Knoepp SM,Chahal MS,Xie Y,Zhang Z,Brauner DJ,Hallman MA,Robinson SA,Han S,Imai M,Tomlinson S,Meier KE

更新日期：2008-09-01 00:00:00

abstract：:[3H]P1075 binding to membrane preparations of rabbit skeletal muscle were observed in the presence of nucleotide triphosphates or diphosphates but not AMP, cAMP, adenosine, tripolyphosphate, or pyrophosphate. Nonhydrolyzable or poorly hydrolyzable ATP analogs inhibited MgATP-supported binding. The EC50 value for MgATP...

journal_title：Molecular pharmacology

authors： Dickinson KE,Bryson CC,Cohen RB,Rogers L,Green DW,Atwal KS

更新日期：1997-09-01 00:00:00

abstract：:MicroRNAs (miRNAs) have emerged as a novel class of endogenous, small, noncoding RNAs that negatively regulate gene expression via degradation or translational inhibition of their target mRNAs. Over 700 miRNAs have been identified and sequenced in humans, and the number of miRNA genes is estimated at more than 1000. I...

journal_title：Molecular pharmacology

authors： Kukreja RC,Yin C,Salloum FN

更新日期：2011-10-01 00:00:00

abstract：:The two G protein-coupled receptors (GPCRs) C-X-C chemokine receptor type 4 (CXCR4) and atypical chemokine receptor 3 (ACKR3) are part of the class A chemokine GPCR family and represent important drug targets for human immunodeficiency virus (HIV) infection, cancer, and inflammation diseases. CXCR4 is one of only thre...

journal_title：Molecular pharmacology

authors： Adlere I,Caspar B,Arimont M,Dekkers S,Visser K,Stuijt J,de Graaf C,Stocks M,Kellam B,Briddon S,Wijtmans M,de Esch I,Hill S,Leurs R

更新日期：2019-12-01 00:00:00

abstract：:Two different mechanisms leading to increased current have been described for the small-molecule human ether-à-go-go-related gene (herg) activator NS1643 [1,3-bis-(2-hydroxy-5-trifluoromethylphenyl)-urea]. On herg1a channels expressed in Xenopus laevis oocytes, it mainly acts via attenuation of inactivation and for ra...

journal_title：Molecular pharmacology

authors： Schuster AM,Glassmeier G,Bauer CK

更新日期：2011-11-01 00:00:00