Insulin-like growth factor type-I receptor-dependent phosphorylation of extracellular signal-regulated kinase 1/2 but not Akt (protein kinase B) can be induced by picropodophyllin.

abstract：:Nicotine can enhance working memory and attention. Activation of both alpha7 and beta2(*) nicotinic acetylcholine receptors (nAChRs) in the prefrontal cortex (PFC) has been implicated in these processes. The ability of presynaptic nAChRs to modulate neurotransmitter release, notably glutamate release, is postulated to...

journal_title：Molecular pharmacology

authors： Dickinson JA,Kew JN,Wonnacott S

更新日期：2008-08-01 00:00:00

abstract：:The effect of halothane on synthesis of retained and secreted proteins was investigated using isolated perfused rat livers. Anesthetic exposure rapidly inhibited synthesis of total liver proteins in a dose-dependent manner by a mechanism which appeared to involve reduced rates of both peptide chain initiation and elon...

journal_title：Molecular pharmacology

authors： Flaim KE,Jefferson LS,McGwire JB,Rannels DE

更新日期：1983-09-01 00:00:00

abstract：:Dietary lipids and fat-soluble micronutrients are solubilized in mixed micelles and absorbed in the small intestine. Based on an assumption that cholesterol and other fat-soluble molecules share a number of transport mechanisms and the fact that Niemann-Pick C1-like 1 (NPC1L1) is critical for intestinal cholesterol ab...

journal_title：Molecular pharmacology

authors： Narushima K,Takada T,Yamanashi Y,Suzuki H

更新日期：2008-07-01 00:00:00

abstract：:The ability of four antidepressant drugs, imipramine, alaproclate, norzimelidine, and fluvoxamine, to inhibit serotonin transport into platelet plasma membrane vesicles was tested over a range of external Na+ concentrations. Imipramine affinity, as we previously reported [J. Biol. Chem. 258:6115-6119 (1983)] increases...

journal_title：Molecular pharmacology

authors： Humphreys CJ,Levin J,Rudnick G

更新日期：1988-06-01 00:00:00

abstract：:Voltage-gated sodium channels are inhibited by many local anesthetics, antiarrhythmics, and antiepileptic drugs. The local anesthetic lidocaine appears to be able to access its binding site in the sodium channel only from the membrane phase or from the internal face of the channel. In contrast, the antiepileptic drug ...

journal_title：Molecular pharmacology

authors： Jo S,Bean BP

更新日期：2014-02-01 00:00:00

abstract：:Previous studies have shown that at least two subtypes of somatostatin (SRIF) receptors (SRIF1 and SRIF2) are expressed in mammalian cells. SRIF1 receptors have high affinity for MK 678, whereas SRIF2 receptors have no affinity for MK 678 but selectively bind peptides with structures similar to that of CGP 23996. Rece...

journal_title：Molecular pharmacology

authors： Rens-Domiano S,Law SF,Yamada Y,Seino S,Bell GI,Reisine T

更新日期：1992-07-01 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 chemical reaction of 1,4-benzoquinone with glutathione results in the formation of adducts that exhibit increasing degrees of glutathione substitution. Purification of these adducts and analysis by 1H and 13C nuclear magnetic resonance spectroscopy revealed the products of the reaction to be 2-(glutathion-S-yl)hyd...

journal_title：Molecular pharmacology

authors： Lau SS,Hill BA,Highet RJ,Monks TJ

更新日期：1988-12-01 00:00:00

abstract：:A fusion protein consisting of the endothelin B (ET(B)) receptor and the enhanced green fluorescent protein (EGFP) in conjunction with Cyanin3- or fluorescein-conjugated endothelin 1 (Cy3-ET1, Fluo-ET1) was used to investigate the ligand-mediated internalization of the ET(B) receptor. The ET(B) receptor and the ET(B)/...

journal_title：Molecular pharmacology

authors： Oksche A,Boese G,Horstmeyer A,Furkert J,Beyermann M,Bienert M,Rosenthal W

更新日期：2000-06-01 00:00:00

abstract：:Serotonin [5-hydroxytryptamine (5-HT)] receptors are distinguished pharmacologically by their characteristic affinities for agonists and antagonists. Two serotonin receptors, the 5-HT2 and 5-HT1c, share a number of pharmacologic and structural properties while differing in their affinities for certain agonists and ant...

journal_title：Molecular pharmacology

authors： Choudhary MS,Craigo S,Roth BL

更新日期：1992-10-01 00:00:00

abstract：:Seven transmembrane G protein-coupled receptors (GPCRs) are often phosphorylated at the C terminus and on intracellular loops in response to various extracellular stimuli. Phosphorylation of GPCRs by GPCR kinases and certain other kinases can promote the recruitment of arrestin molecules. The arrestins critically regu...

journal_title：Molecular pharmacology

authors： Yang Z,Yang F,Zhang D,Liu Z,Lin A,Liu C,Xiao P,Yu X,Sun JP

更新日期：2017-09-01 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 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

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：: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 N-methyl-D-aspartate (NMDA)-sensitive glutamate receptors are known to be inhibited by 3-amino-1-hydroxy-2-pyrrolidone (HA-966) and 7-chlorokynurenic acid (Cl-KYN), which act at the glycine-regulated allosteric modulatory center. In this work we show that, in synaptic membranes prepared from rat brain, Cl-KYN and ...

journal_title：Molecular pharmacology

authors： Danysz W,Fadda E,Wroblewski JT,Costa E

更新日期：1989-12-01 00:00:00

abstract：:Reuptake of glutamate in astrocytes, a critical mechanism involved in the maintenance of physiological excitatory amino acid neurotransmission, is inhibited by both arachidonic acid (AA) and reactive oxygen species (ROS), via incompletely defined molecular mechanisms. Because ROS are generated during AA metabolism and...

journal_title：Molecular pharmacology

authors： Volterra A,Trotti D,Racagni G

更新日期：1994-11-01 00:00:00

abstract：:The mechanisms underlying mastoparan-induced elevation of the intracellular free calcium concentration ([Ca2+]i) were investigated in the insulin-secreting cell lines RINm5F and HIT. In both cell types, micromolar concentrations of mastoparan induced a prompt increase of [Ca2+]i, measured as an increase in fura-2 fluo...

journal_title：Molecular pharmacology

authors： Eddlestone GT,Komatsu M,Shen L,Sharp GW

更新日期：1995-04-01 00:00:00

abstract：:Several reports have been published recently demonstrating a beneficial effect of epidermal growth factor receptor (EGFR) inhibitors in improving pathologic and behavioral conditions in neurodegenerative diseases (NDDs) such as Alzheimer's disease and Amyotrophic Lateral Sclerosis (ALS) as well as the brain and spinal...

journal_title：Molecular pharmacology

authors： Tavassoly O,Sato T,Tavassoly I

更新日期：2020-07-01 00:00:00

abstract：:We previously described the development of genetic models to study the in vivo functions of the hepatic cytochrome P450 (P450) system, through the hepatic deletion of either cytochrome P450 oxidoreductase [POR; HRN (hepatic reductase null) line] or cytochrome b(5) [HBN (hepatic cytochrome b(5) null) line]. However, HR...

journal_title：Molecular pharmacology

authors： Henderson CJ,McLaughlin LA,Wolf CR

更新日期：2013-06-01 00:00:00

abstract：:Cytochrome P450 (P450) enzymes are responsible for metabolizing drugs. Expression of P450s can directly affect drug metabolism, resulting in various outcomes in therapeutic efficacy and adverse effects. Several nuclear receptors are transcription factors that can regulate expression of P450s at both basal and drug-ind...

journal_title：Molecular pharmacology

authors： Chen L,Bao Y,Piekos SC,Zhu K,Zhang L,Zhong XB

更新日期：2018-07-01 00:00:00

abstract：:The putative serotonin (5-HT) agonist RU 24969 [5-methoxy-3-1,2,3,6-tetrahydropyridin-4-yl)indole; 5-MeO-THPI] has been extensively used in the study and classification of 5-HT receptors. In order to study molecular determinants for recognition of THPIs at central 5-HT recognition sites, about 25 additional THPI deriv...

journal_title：Molecular pharmacology

authors： Taylor EW,Nikam SS,Lambert G,Martin AR,Nelson DL

更新日期：1988-07-01 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：:Signaling by G-protein-coupled receptors is often considered a uniform process, whereby a homogeneously activated proportion of randomly distributed receptors are activated under equilibrium conditions and produce homogeneous, steady-state intracellular signals. While this may be the case in some biologic systems, the...

journal_title：Molecular pharmacology

authors： Lohse MJ,Hofmann KP

更新日期：2015-09-01 00:00:00

abstract：:The Integrated Stress Response (ISR) is a signaling program that enables cellular adaptation to stressful conditions like hypoxia and nutrient deprivation in the tumor microenvironment. An important effector of the ISR is activating transcription factor 4 (ATF4), a transcription factor that regulates genes involved in...

journal_title：Molecular pharmacology

authors： Sayers CM,Papandreou I,Guttmann DM,Maas NL,Diehl JA,Witze ES,Koong AC,Koumenis C

更新日期：2013-03-01 00:00:00

abstract：:Multidrug resistance-associated protein 2 (MRP2) transports glutathione conjugates, glucuronide conjugates, and sulfated conjugates of bile acids. In the present study, we examined the role of charged amino acids in the transmembrane domains of rat Mrp2, conserved among MRP families, using the isolated membrane vesicl...

journal_title：Molecular pharmacology

authors： Ito K,Suzuki H,Sugiyama Y

更新日期：2001-05-01 00:00:00

abstract：:Modulation of neuronal ion channels by the cloned rat brain CB1 cannabinoid receptor was investigated with the use of a heterologous neuronal expression system. Transient expression of the rat brain CB1 cannabinoid receptor was accomplished through microinjection of in vitro transcribed cRNA into the cytoplasm of enzy...

journal_title：Molecular pharmacology

authors： Pan X,Ikeda SR,Lewis DL

更新日期：1996-04-01 00:00:00

abstract：:Comparative molecular field analysis (CoMFA) predicts that the large electrostatic field around the phosphate groups of ATP plays a crucial role in stabilizing the open state of the cardiac ryanodine receptor (RyR) channel. We therefore investigated the effects of adenosine-5'-(beta,gamma-methylenetriphosphate) (AMP-P...

journal_title：Molecular pharmacology

authors： Chan WM,Welch W,Sitsapesan R

更新日期：2003-01-01 00:00:00

abstract：:Tumors provide an extremely abnormal microenvironment that stimulates neovascularization from surrounding vessels and causes altered gene expression within vascular cells. Up-regulation of vascular endothelial growth factor (VEGF) receptors has allowed selective destruction of tumor vessels by administration of a chim...

journal_title：Molecular pharmacology

authors： Akiyama H,Mohamedali KA,E Silva RL,Kachi S,Shen J,Hatara C,Umeda N,Hackett SF,Aslam S,Krause M,Lai H,Rosenblum MG,Campochiaro PA

更新日期：2005-12-01 00:00:00

abstract：:We examined the subtype-selective binding site of the beta-adrenergic receptors (betaARs). The beta(1)/beta(2)-chimeric receptors showed the importance of the second and seventh transmembrane domains (TM2 and TM7) of the beta(2)AR for the binding of the beta(2)-selective agonists such as formoterol and procaterol. Ala...

journal_title：Molecular pharmacology

authors： Isogaya M,Sugimoto Y,Tanimura R,Tanaka R,Kikkawa H,Nagao T,Kurose H

更新日期：1999-11-01 00:00:00