A Latin American Perspective on G Protein-Coupled Receptors.

abstract：:Niflumic acid [2-((3-(trifluoromethyl)phenyl)amino)-3-pyridinecarboxylic acid, NFA] is a nonsteroidal anti-inflammatory drug that also blocks or modulates the gating of a wide spectrum of ion channels. Here we investigated the mechanism of channel activation by NFA on ether-a-go-go-related gene (ERG) K(+) channel subt...

journal_title：Molecular pharmacology

authors： Fernandez D,Sargent J,Sachse FB,Sanguinetti MC

更新日期：2008-04-01 00:00:00

abstract：:alpha4beta2 nicotinic acetylcholine receptors (nAChRs) are recognized as the principal nicotine binding site in brain. Recombinant alpha4beta2 nAChR demonstrate biphasic concentration-response relationships with low- and high-EC50 components. This study shows that untranslated regions (UTR) can influence expression of...

journal_title：Molecular pharmacology

authors： Briggs CA,Gubbins EJ,Marks MJ,Putman CB,Thimmapaya R,Meyer MD,Surowy CS

更新日期：2006-07-01 00:00:00

abstract：:Amphetamine congeners [e.g., 3,4-methylenedioxymetamphetamine (MDMA), or "ecstasy"] are substrates for monoamine transporters (i.e., the transporters for serotonin, norepinephrine, and dopamine); however, their in vivo-action relies on their ability to promote monoamine efflux. The mechanistic basis for this counter t...

journal_title：Molecular pharmacology

authors： Seidel S,Singer EA,Just H,Farhan H,Scholze P,Kudlacek O,Holy M,Koppatz K,Krivanek P,Freissmuth M,Sitte HH

更新日期：2005-01-01 00:00:00

abstract：:Peroxisome proliferator-activated receptor δ (PPARδ) has been implicated in vascular pathophysiology. However, its functions in atherogenic changes of the vascular wall have not been fully elucidated. PPARδ activated by GW501516 (2-[2-methyl-4-[[4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl]methylsulfanyl]ph...

journal_title：Molecular pharmacology

authors： Hwang JS,Ham SA,Yoo T,Lee WJ,Paek KS,Lee CH,Seo HG

更新日期：2016-11-01 00:00:00

abstract：:Ethanol (ETOH) can cause apoptotic death of neurons by depleting GSH with an associated increase in oxidative stress. The current study illustrates a means to overcome this ETOH-induced neurotoxicity by enhancing GSH through boosting Nrf2, a transcription factor that controls GSH homeostasis. ETOH treatment caused a s...

journal_title：Molecular pharmacology

authors： Narasimhan M,Mahimainathan L,Rathinam ML,Riar AK,Henderson GI

更新日期：2011-12-01 00:00:00

abstract：:In cells expressing both the insulin receptor isoform A (IRA) and the insulin-like growth factor-1 receptor (IGF1R), the presence of hybrid receptors, made up of an alphabeta-IRA chain associated with an alphabeta-IGF1R chain, has been demonstrated. These heterodimers are found in normal cells, and they also seem to p...

journal_title：Molecular pharmacology

authors： Blanquart C,Gonzalez-Yanes C,Issad T

更新日期：2006-11-01 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：:Recently, several classes of compounds have been shown to be potent, selective, and specific inhibitors of human immunodeficiency virus type 1 replication in vitro. These include the tetrahydroimidazo[4,5,1-jk][1,4]-benzodiazepin-2(1H)-one and -thione (TIBO) and the 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (H...

journal_title：Molecular pharmacology

authors： Debyser Z,Pauwels R,Baba M,Desmyter J,De Clercq E

更新日期：1992-05-01 00:00:00

abstract：:Adenosine receptors of the A1 and A2 subtypes were characterized in membranes from DDT1 MF-2 smooth muscle cells. These cells possess a high density of A1 adenosine receptors (Bmax = 0.8-0.9 pmol/mg of protein), as measured by both agonist and antagonist radioligands. Agonists compete for [125I]N6-[2-(4-amino-3-iodoph...

journal_title：Molecular pharmacology

authors： Ramkumar V,Barrington WW,Jacobson KA,Stiles GL

更新日期：1990-02-01 00:00:00

abstract：:Melanocortins (MCs) have various physiological actions on the brain. The recent cloning of neural MC receptors opened new avenues to study the effects of these neuropeptides on the nervous system. Here we investigated the structure-activity relationships (SARs) of peptides derived from adrenocorticotropic hormone (ACT...

journal_title：Molecular pharmacology

authors： Adan RA,Cone RD,Burbach JP,Gispen WH

更新日期：1994-12-01 00:00:00

abstract：:We examined the influence of the molecular structure of four novel adamantane derivatives on their ability to block the channels of nicotinic acetylcholine (ACh) and N-methyl-D-aspartate (NMDA) receptors. The structure of the drugs is Ad-CH2-N+H2-(CH2)5-R, where Ad is adamantane and R was varied from ammonium (IEM-175...

journal_title：Molecular pharmacology

authors： Antonov SM,Johnson JW,Lukomskaya NY,Potapyeva NN,Gmiro VE,Magazanik LG

更新日期：1995-03-01 00:00:00

abstract：:We examined the block of N-methyl-D-aspartate (NMDA) receptors by n-alkyl (straight chain) diamines and related monoamines and triamines using whole-cell voltage clamp recording of NMDA receptor currents in cultured rat hippocampal neurons and [3H] dizocilpine binding to rat forebrain homogenates. At -60 mV, the diami...

journal_title：Molecular pharmacology

authors： Subramaniam S,Donevan SD,Rogawski MA

更新日期：1994-01-01 00:00:00

abstract：:Cardiac function is regulated by many hormones and neurotransmitters that exert their physiological effects through the activation of G protein-coupled receptors (GPCRs). Identification of new GPCRs that might display a specific pattern of expression within the heart and differentially regulate specific cardiac functi...

journal_title：Molecular pharmacology

authors： Moore-Morris T,Varrault A,Mangoni ME,Le Digarcher A,Negre V,Dantec C,Journot L,Nargeot J,Couette B

更新日期：2009-05-01 00:00:00

abstract：:The peripheral cannabinoid receptor (CB2) is a G protein-coupled receptor that is both positively and negatively coupled to the mitogen-activated protein kinase (MAPK) and cAMP pathways, respectively, through a Bordetella pertussis toxin-sensitive G protein. CB2 receptor-transfected Chinese hamster ovary cells exhibit...

journal_title：Molecular pharmacology

authors： Bouaboula M,Desnoyer N,Carayon P,Combes T,Casellas P

更新日期：1999-03-01 00:00:00

abstract：:Electrical recordings were made in Xenopus oocytes to study the modulatory effects of steroids on gamma-aminobutyric acid (GABA) receptors expressed by RNA from mammalian brain and retina. GABA responses expressed by rat cerebral cortex poly(A)+ RNA were bicuculline-sensitive Cl- currents mediated by GABAA receptors. ...

journal_title：Molecular pharmacology

authors： Woodward RM,Polenzani L,Miledi R

更新日期：1992-01-01 00:00:00

abstract：:Cyclic nucleotide analogs were used to study relaxation of pig coronary arteries and guinea pig tracheal smooth muscle in an attempt to determine the roles of cAMP- and cGMP-dependent protein kinases (cA-K and cG-K). In pig coronary artery strips, cGMP analogs were generally more effective than cAMP analogs in promoti...

journal_title：Molecular pharmacology

authors： Francis SH,Noblett BD,Todd BW,Wells JN,Corbin JD

更新日期：1988-10-01 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：:In light of the potential use of the thiazolidinedione family of peroxisome proliferator-activated receptor-gamma (PPARgamma) agonists in prostate cancer treatment, this study assessed the mechanism by which these agents suppress prostate-specific antigen (PSA) secretion in prostate cancer cells. Two lines of evidence...

journal_title：Molecular pharmacology

authors： Yang CC,Ku CY,Wei S,Shiau CW,Chen CS,Pinzone JJ,Ringel MD,Chen CS

更新日期：2006-05-01 00:00:00

abstract：:The tetrapeptide Arg-Leu-Tyr-Glu (RLYE), a vascular endothelial growth factor (VEGF) receptor-2 antagonist, has been used previously either alone or in combination with chemotherapeutic drugs for treating colorectal cancer in a mouse model. We analyzed the half-life of the peptide and found that because of degradation...

journal_title：Molecular pharmacology

authors： Yun JA,Kim J,Baek YY,Park W,Park M,Kim S,Kim T,Choi S,Jeoung D,Lee H,Won MH,Kim JY,Ha KS,Kwon YG,Kim YM

更新日期：2019-12-01 00:00:00

abstract：:The decrease in mu-opioid receptor activity after chronic agonist exposure (1 microM [D-Ala(2),N-MePhe(4),Gly-ol(5)]-enkephalin) is largely due to kinase-mediated phosphorylation of intracellular receptor domains. We have recently shown that the substitution of two putative Ca(2+)/calmodulin-dependent protein kinase I...

journal_title：Molecular pharmacology

authors： Koch T,Kroslak T,Averbeck M,Mayer P,Schröder H,Raulf E,Höllt V

更新日期：2000-08-01 00:00:00

abstract：:Ro 11-2465 is a cyanide derivative of imipramine. In cerebral cortex homogenates, [3H] Ro 11-2465 displays a binding profile similar to that of [3H]imipramine. Agents compete with binding of [3H]Ro 11-2465 in an order of potency similar to their ability to block serotonin uptake, and raphe lesions greatly decrease the...

journal_title：Molecular pharmacology

authors： Dumbrille-Ross A,Tang SW

更新日期：1983-05-01 00:00:00

abstract：:Although much has been learned about the mechanisms of ligand selectivity between different opioid receptor subtypes, little is known about the common opioid binding pocket shared by all opioid receptors. The recently discovered orphanin system offers a good opportunity to study the mechanisms involved in the binding ...

journal_title：Molecular pharmacology

authors： Meng F,Ueda Y,Hoversten MT,Taylor LP,Reinscheid RK,Monsma FJ,Watson SJ,Civelli O,Akil H

更新日期：1998-04-01 00:00:00

abstract：:The CYP2C genes are extensively regulated at the transcriptional stage. The present study shows for the first time that CYP2Cs are also regulated post-transcriptionally by microRNAs (miRNAs). By using online search engines, we found potential miRNA response elements (MREs) in the 3'-untranslated region (3'-UTR) of the...

journal_title：Molecular pharmacology

authors： Zhang SY,Surapureddi S,Coulter S,Ferguson SS,Goldstein JA

更新日期：2012-09-01 00:00:00

abstract：:The ATP signaling mechanism in neuroblastoma x glioma hybrid NG108-15 cells differentiated by exposure to dibutyryl-cAMP was characterized. In cells loaded with fura-2, ATP rapidly raised the cytosolic Ca2+ concentration ([Ca2+]i); the magnitude of the rise was inversely proportional to the extracellular Na+ concentra...

journal_title：Molecular pharmacology

authors： Chueh SH,Hsu LS,Song SL

更新日期：1994-03-01 00:00:00

abstract：:ORKAMBI, a combination of the corrector, lumacaftor, and the potentiator, ivacaftor, partially rescues the defective processing and anion channel activity conferred by the major cystic fibrosis-causing mutation, F508del, in in vitro studies. Clinically, the improvement in lung function after ORKAMBI treatment is modes...

journal_title：Molecular pharmacology

authors： Wu YS,Jiang J,Ahmadi S,Lew A,Laselva O,Xia S,Bartlett C,Ip W,Wellhauser L,Ouyang H,Gonska T,Moraes TJ,Bear CE

更新日期：2019-10-01 00:00:00

abstract：:The gamma-aminobutyric acid (GABA) receptor type B (GABA(B)R) is constituted of at least two homologous proteins, GABA(B)R1 and GABA(B)R2. These proteins share sequence and structural similarity with metabotropic glutamate and Ca(2+)-sensing receptors, both of which are sensitive to Ca(2+). Using rat brain membranes, ...

journal_title：Molecular pharmacology

authors： Galvez T,Urwyler S,Prézeau L,Mosbacher J,Joly C,Malitschek B,Heid J,Brabet I,Froestl W,Bettler B,Kaupmann K,Pin JP

更新日期：2000-03-01 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：:Glyceryl trinitrate (GTN) is used in the treatment of angina pectoris and cardiac failure, but the rapid onset of GTN tolerance limits its clinical utility. Research suggests that a principal cause of tolerance is inhibition of an enzyme responsible for the production of physiologically active concentrations of NO fro...

journal_title：Molecular pharmacology

authors： DiFabio J,Ji Y,Vasiliou V,Thatcher GR,Bennett BM

更新日期：2003-11-01 00:00:00

abstract：:The response of myeloid leukemia cells to treatment with 1-beta-D-arabinofuranosylcytosine (ara-C) includes activation of the c-Abl protein tyrosine kinase and the stress-activated protein kinase (SAPK). The present studies demonstrate that treatment of human U-937 leukemia cells with ara-C is associated with transloc...

journal_title：Molecular pharmacology

authors： Raina D,Mishra N,Kumar S,Kharbanda S,Saxena S,Kufe D

更新日期：2002-06-01 00:00:00

abstract：:This study describes experiments investigating the mechanism of activation of A1 adenosine receptors. Isolated rat fat cells were used as a cellular model. The A1 receptors of these cells were covalently labeled with the agonist photoaffinity label R-2-azido-N6-p-hydroxyphenylisopropyladenosine. The covalent incorpora...

journal_title：Molecular pharmacology

authors： Lohse MJ,Klotz KN,Schwabe U

更新日期：1986-10-01 00:00:00