The alpha 1C-adrenergic receptor: characterization of signal transduction pathways and mammalian tissue heterogeneity.

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：: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：:In vivo administration of the porphyrogenic agent allylisopropylacetamide (AIA) to phenobarbital-pretreated rats results in marked loss of hepatic cytochrome P-450 content. Using isozyme-selective functional markers, we now show that such loss reflects inactivation of several phenobarbital-inducible and constitutive i...

journal_title：Molecular pharmacology

authors： Bornheim LM,Underwood MC,Caldera P,Rettie AE,Trager WF,Wrighton SA,Correia MA

更新日期：1987-08-01 00:00:00

abstract：:The neuropeptides vasoactive intestinal peptide (VIP) and pituitary adenylate cyclase-activating peptide (PACAP) and their class II G protein-coupled receptors VPAC(1), VPAC(2), and PAC(1) play important roles in human physiology. No small molecule modulator has ever been reported for the VIP/PACAP receptors, and ther...

journal_title：Molecular pharmacology

authors： Chu A,Caldwell JS,Chen YA

更新日期：2010-01-01 00:00:00

abstract：:Cardiac-directed expression of AC6 has pronounced favorable effects on cardiac function possibly not linked with cAMP production. To determine rigorously whether cAMP generation is required for the beneficial effects of increased AC6 expression, we generated a catalytically inactive AC6 mutant (AC6mut) that has marked...

journal_title：Molecular pharmacology

authors： Gao MH,Tang T,Lai NC,Miyanohara A,Guo T,Tang R,Firth AL,Yuan JX,Hammond HK

更新日期：2011-03-01 00:00:00

abstract：:Advances in proteomic methodologies based on quantitative mass spectrometry are now transforming pharmacology and experimental biology more broadly. The present review will discuss several examples, based on work in the author's laboratory that focuses on delineating relationships between GPCR signaling and traffickin...

journal_title：Molecular pharmacology

authors： von Zastrow M

更新日期：2020-12-22 00:00:00

abstract：:The instability of the solubilized/purified form, the lack of catalytic activity of the stabilized, macrolide-complexed form, and the compromised catalytic activity of the decomplexed form of steroid-inducible cytochrome P450IIIA1 motivated further investigations of the substrate specificity of this isozyme. A major c...

journal_title：Molecular pharmacology

authors： Namkung MJ,Yang HL,Hulla JE,Juchau MR

更新日期：1988-11-01 00:00:00

abstract：:The anti-arrhythmic quinidine has been reported to be a competitive inhibitor of the catalytic activities of human liver P-450DB, including sparteine delta 2-oxidation and bufuralol 1'-hydroxylation, and we confirmed the observation that submicromolar concentrations are strongly inhibitory. Human liver microsomes oxid...

journal_title：Molecular pharmacology

authors： Guengerich FP,Müller-Enoch D,Blair IA

更新日期：1986-09-01 00:00:00

abstract：:The aim of this study was to clarify the mechanism by which cytochrome P450 (P450)-mediated catalytic activity is decreased following interferon (IFN) administration. Microsomal steroid hydroxylation was assessed to test the hypothesis that IFN selectively decreases the activities of individual P450 isozymes in male r...

journal_title：Molecular pharmacology

authors： Craig PI,Mehta I,Murray M,McDonald D,Aström A,van der Meide PH,Farrell GC

更新日期：1990-09-01 00:00:00

abstract：:The exchange of tritium into water from saxitoxin molecules that were radiolabeled at the C-11 methylene position was measured at 37 degrees in solution and in suspensions of brain membranes. High concentrations of membrane receptors were used to assure that more than 80% of the total saxitoxin (STX) present was speci...

journal_title：Molecular pharmacology

authors： Strichartz G

更新日期：1982-03-01 00:00:00

abstract：:Iodonium inhibition of the flavoenzymes neutrophil NADPH oxidase and cytochrome P450 reductase has been suggested to require reductive metabolism of the inhibitor to a phenyl radical. Inhibition would ultimately result from covalent attachment of phenyl radicals to either the flavin cofactor or adjacent amino acid sid...

journal_title：Molecular pharmacology

authors： O'Donnell VB,Smith GC,Jones OT

更新日期：1994-10-01 00:00:00

abstract：:Gemcitabine and pemetrexed are effective agents in the treatment of non-small-cell lung cancer (NSCLC), and the present study investigates cellular and genetic aspects of their interaction against A549, Calu-1, and Calu-6 cells. Cells were treated with pemetrexed and gemcitabine, and their interaction was assessed usi...

journal_title：Molecular pharmacology

authors： Giovannetti E,Mey V,Nannizzi S,Pasqualetti G,Marini L,Del Tacca M,Danesi R

更新日期：2005-07-01 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：:The peroxisome proliferator-activated receptors (PPARs) represent pharmacological target molecules to improve insulin resistance in type 2 diabetes mellitus. Here we assessed a functional connection between pharmacological activation of PPAR and vascular endothelial growth factor (VEGF) expression in keratinocytes and...

journal_title：Molecular pharmacology

authors： Schiefelbein D,Seitz O,Goren I,Dissmann JP,Schmidt H,Bachmann M,Sader R,Geisslinger G,Pfeilschifter J,Frank S

更新日期：2008-10-01 00:00:00

abstract：:Molecular cloning of membrane-spanning mammalian adenylyl cyclases (ACs) has led to the discovery of nine different isotypes, making ACs potentially useful therapeutic targets. This study investigated the mechanism by which fungicidal nitroimidazole compounds modulate AC activity. Current evidence indicates that biolo...

journal_title：Molecular pharmacology

authors： Haunsø A,Simpson J,Antoni FA

更新日期：2003-03-01 00:00:00

abstract：:Inhibition of cannabinoid receptor 1 (CB1) has shown efficacy in reducing body weight and improving metabolic parameters, with the effects correlating with target engagement in the brain. The peripheral effects of inhibiting the CB1 receptor has been appreciated through studies in diet-induced obese and liver-specific...

journal_title：Molecular pharmacology

authors： Zhao W,Fong O,Muise ES,Thompson JR,Weingarth D,Qian S,Fong TM

更新日期：2010-09-01 00:00:00

abstract：:Identifying novel mechanisms to enhance glucagon-like peptide-1 (GLP-1) receptor signaling may enable nascent medicinal chemistry strategies with the aim of developing new orally available therapeutic agents for the treatment of type 2 diabetes mellitus. Therefore, we tested the hypothesis that selectively modulating ...

journal_title：Molecular pharmacology

authors： Willard FS,Wootten D,Showalter AD,Savage EE,Ficorilli J,Farb TB,Bokvist K,Alsina-Fernandez J,Furness SG,Christopoulos A,Sexton PM,Sloop KW

更新日期：2012-12-01 00:00:00

abstract：:A novel cloned polymorphism of the human concentrative nucleoside transporter hCNT3 was described and functionally characterized. This variant consists of a T/C transition leading to the substitution of cysteine 602 by an arginine residue in the core of transmembrane domain 13. The resulting hCNT3(C602R) protein has t...

journal_title：Molecular pharmacology

authors： Errasti-Murugarren E,Cano-Soldado P,Pastor-Anglada M,Casado FJ

更新日期：2008-02-01 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：:The vitamin D receptor (VDR) mediates vitamin D signaling in numerous physiological and pharmacological processes, including bone and calcium metabolism, cellular growth and differentiation, immunity, and cardiovascular function. Although transcriptional regulation by VDR has been investigated intensively, an understa...

journal_title：Molecular pharmacology

authors： Choi M,Yamada S,Makishima M

更新日期：2011-12-01 00:00:00

abstract：:Studies in vertebrate neuromuscular synapses have revealed previously that ATP, via P2Y receptors, plays a critical role in regulating postsynaptic gene expressions. An equivalent regulatory role of ATP and its P2Y receptors would not necessarily be expected for the very different situation of the brain synapses, but ...

journal_title：Molecular pharmacology

authors： Siow NL,Choi RC,Xie HQ,Kong LW,Chu GK,Chan GK,Simon J,Barnard EA,Tsim KW

更新日期：2010-12-01 00:00:00

abstract：:In the present study, we have elucidated the functional characteristics and mechanism of action of methaqualone (2-methyl-3-o-tolyl-4(3H)-quinazolinone, Quaalude), an infamous sedative-hypnotic and recreational drug from the 1960s-1970s. Methaqualone was demonstrated to be a positive allosteric modulator at human α1,2...

journal_title：Molecular pharmacology

authors： Hammer H,Bader BM,Ehnert C,Bundgaard C,Bunch L,Hoestgaard-Jensen K,Schroeder OH,Bastlund JF,Gramowski-Voß A,Jensen AA

更新日期：2015-08-01 00:00:00

abstract：:The toxicity of acetaminophen (4'-hydroxyacetanilide), 3,5-dimethylacetaminophen (3'-5'-dimethyl-4'-hydroxyacetanilide), and 2,6-dimethylacetaminophen (2',6'-dimethyl-4'-hydroxyacetanilide) was investigated in hepatocytes isolated from phenobarbital-pretreated rats. At a concentration of 5 mM, acetaminophen was found ...

journal_title：Molecular pharmacology

authors： Porubek DJ,Rundgren M,Harvison PJ,Nelson SD,Moldéus P

更新日期：1987-06-01 00:00:00

abstract：:The effects of interleukin (IL)-1 beta, IL-4, IL-6, tumor necrosis factor (TNF)-alpha, interferon (IFN)-alpha, IFN-gamma, and transforming growth factor (TGF)-beta 1 on cytochrome P-450 (CYP) 1A expression and polycyclic aromatic hydrocarbon (PAH)-mediated induction in primary human hepatocyte cultures were determined...

journal_title：Molecular pharmacology

authors： Abdel-Razzak Z,Corcos L,Fautrel A,Campion JP,Guillouzo A

更新日期：1994-12-01 00:00:00

abstract：:α-Conotoxins are subtype-selective nicotinic acetylcholine receptor (nAChR) antagonists. Although potent α3β2 nAChR-selective α-conotoxins have been identified, currently characterized α-conotoxins show no or only weak affinity for α4β2 nAChRs, which are, besides α7 receptors, the most abundant nAChRs in the mammalian...

journal_title：Molecular pharmacology

authors： Beissner M,Dutertre S,Schemm R,Danker T,Sporning A,Grubmüller H,Nicke A

更新日期：2012-10-01 00:00:00

abstract：:The aim of this study was to create and characterize constitutively active mutant (CAM) histamine H(1) receptors (H(1)R) using random mutagenesis methods to further investigate the activation process of the rhodopsin-like family of G protein-coupled receptors (GPCRs). This approach identified position 6.40 in TM 6 as ...

journal_title：Molecular pharmacology

authors： Bakker RA,Jongejan A,Sansuk K,Hacksell U,Timmerman H,Brann MR,Weiner DM,Pardo L,Leurs R

更新日期：2008-01-01 00:00:00

abstract：:TNP-ATP has become widely recognized as a potent and selective P2X receptor antagonist, and is currently being used to discriminate between subtypes of P2X receptors in a variety of tissues. We have investigated the ability of TNP-ATP to inhibit alpha,beta-methylene ATP (alpha,beta-meATP)-evoked responses in 1321N1 hu...

journal_title：Molecular pharmacology

authors： Burgard EC,Niforatos W,van Biesen T,Lynch KJ,Kage KL,Touma E,Kowaluk EA,Jarvis MF

更新日期：2000-12-01 00:00:00

abstract：:Previous studies showed that lapatinib and obatoclax interact in a greater-than-additive fashion to cause cell death and do so through a toxic form of autophagy. The present studies sought to extend our analyses. Lapatinib and obatoclax killed multiple tumor cell types, and cells lacking phosphatase and tensin homolog...

journal_title：Molecular pharmacology

authors： Cruickshanks N,Tang Y,Booth L,Hamed H,Grant S,Dent P

更新日期：2012-12-01 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：:K-252b, a member of the staurosporine family of protein kinase inhibitors, selectively potentiates the activation of the nerve growth factor receptor, TrkA, by a nonpreferred ligand, neurotrophin-3 (NT-3), in a variety of cell types. At higher (micromolar) concentrations of K-252b, an inhibitory effect occurs because ...

journal_title：Molecular pharmacology

authors： Pollack S,Young L,Bilsland J,Wilkie N,Ellis S,Hefti F,Broughton H,Harper S

更新日期：1999-07-01 00:00:00