Strong activation of ether-à-go-go-related gene 1 K+ channel isoforms by NS1643 in human embryonic kidney 293 and Chinese hamster ovary cells.

abstract：:Bovine pulmonary artery endothelial (CPAE) cells respond to bradykinin, and it has been suggested that the receptors on these cells do not fall into the normal B1/B2 classification of bradykinin receptors [J. Pharmacol. Exp. Ther. 244:646-649 (1988)]. The present study describes a detailed characterization of the subt...

journal_title：Molecular pharmacology

authors： Smith JA,Webb C,Holford J,Burgess GM

更新日期：1995-03-01 00:00:00

abstract：:Ovarian cancer is the leading cause of death from gynecological malignancy and has the worst prognosis of all gynecological cancers. Vascular endothelial growth factor (VEGF) plays an important role in ovarian cancer development. 9-beta-D-Arabinofuranosyl-2-fluoroadenine (Fara-A), a nucleotide analog, is frequently us...

journal_title：Molecular pharmacology

authors： Fang J,Cao Z,Chen YC,Reed E,Jiang BH

更新日期：2004-07-01 00:00:00

abstract：:Pregnanolone [5 beta-pregnan-3 alpha-ol-20-one (5 beta 3 alpha)] and allopregnanolone [5 alpha-pregnan-3 alpha-ol-20-one (5 alpha 3 alpha)] are neuroactive steroids that are reduced metabolites of progesterone. Both 5 beta 3 alpha and 5 alpha 3 alpha are potent positive modulators of the gamma-aminobutyric acid respon...

journal_title：Molecular pharmacology

authors： Friedman L,Gibbs TT,Farb DH

更新日期：1993-07-01 00:00:00

abstract：:The human monoamine oxidase (MAO) B plays a major role in the degradation of biogenic and dietary amines such as phenylethylamine, benzylamine, dopamine, and tyramine. We previously showed that the -246/-99 MAO B promoter region exhibited the highest activity and contained two clusters of overlapping Sp1 sites, a CACC...

journal_title：Molecular pharmacology

authors： Wong WK,Chen K,Shih JC

更新日期：2001-04-01 00:00:00

abstract：:Recent reports regarding the significance of chemokine receptors in disease have put a spotlight on atypical chemokine receptor 3 (ACKR3). This atypical chemokine receptor is overexpressed in numerous cancer types and has been involved in the modulation of tumor cell proliferation and migration, tumor angiogenesis, or...

journal_title：Molecular pharmacology

authors： Neves M,Fumagalli A,van den Bor J,Marin P,Smit MJ,Mayor F

更新日期：2019-12-01 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：: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：:We have found that stypoldione, a bright red o-quinone isolated from the brown alga Stypopodium zonale, inhibits the division of sea urchin embryos in a concentration-dependent manner (IC50 approximately 2.5 X 10(-6) M). Although previous studies have shown this marine natural product to inhibit beef brain microtubule...

journal_title：Molecular pharmacology

authors： White SJ,Jacobs RS

更新日期：1983-11-01 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

abstract：:Dysregulation of the chemokine system is implicated in a number of autoimmune and inflammatory diseases, as well as cancer. Modulation of chemokine receptor function is a very promising approach for therapeutic intervention. Despite interest from academic groups and pharmaceutical companies, there are currently few ap...

journal_title：Molecular pharmacology

authors： Bobkov V,Arimont M,Zarca A,De Groof TWM,van der Woning B,de Haard H,Smit MJ

更新日期：2019-12-01 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：:Autophagy is the process by which cellular material is delivered to lysosomes for degradation and recycling. There are three different types of autophagy, but macroautophagy, which involves the formation of double membrane vesicles that engulf proteins and organelles that fuse with lysosomes, is by far the most studie...

journal_title：Molecular pharmacology

authors： Thorburn A,Thamm DH,Gustafson DL

更新日期：2014-06-01 00:00:00

abstract：:Sazetidine-A has been recently proposed to be a "silent desensitizer" of alpha4beta2 nicotinic acetylcholine receptors (nAChRs), implying that it desensitizes alpha4beta2 nAChRs without first activating them. This unusual pharmacological property of sazetidine-A makes it, potentially, an excellent research tool to dis...

journal_title：Molecular pharmacology

authors： Zwart R,Carbone AL,Moroni M,Bermudez I,Mogg AJ,Folly EA,Broad LM,Williams AC,Zhang D,Ding C,Heinz BA,Sher E

更新日期：2008-06-01 00:00:00

abstract：:1-[6-[[(17beta)-3-methoxyestra-1,3,5(10)-trien-17-yl]amino]hexyl]-1H-pyrrole-2,5-dione (U73122) is widely used to inhibit phospholipase C (PLC)-mediated signaling, but we and others have also reported a PLC-independent block of Kir3 channels in native cells. To elaborate on this major side effect, we examined the acti...

journal_title：Molecular pharmacology

authors： Klose A,Huth T,Alzheimer C

更新日期：2008-11-01 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：:Valproic acid (VPA) is an effective antiepileptic drug with an additional activity for the treatment of bipolar disorder. It has been assumed that both activities arise from a common target. At the molecular level, VPA targets a number of distinct proteins that are involved in signal transduction. VPA inhibition of in...

journal_title：Molecular pharmacology

authors： Shimshoni JA,Dalton EC,Jenkins A,Eyal S,Ewan K,Williams RS,Pessah N,Yagen B,Harwood AJ,Bialer M

更新日期：2007-03-01 00:00:00

abstract：:A human recombinant L-type Ca2+ channel (alpha1C,77) was coexpressed with the rat angiotensin AT1A receptor in Xenopus laevis oocytes. In oocytes expressing only alpha1C,77 channels, application of human angiotensin II (1-10 microM) did not affect the amplitude or kinetics of Ba2+ currents (IBa). In sharp contrast, in...

journal_title：Molecular pharmacology

authors： Oz M,Melia MT,Soldatov NM,Abernethy DR,Morad M

更新日期：1998-12-01 00:00:00

abstract：:Recent years have witnessed the discovery of novel selective agonists of the M(1) muscarinic acetylcholine (ACh) receptor (mAChR). One mechanism invoked to account for the selectivity of such agents is that they interact with allosteric sites. We investigated the molecular pharmacology of two such agonists, 1-[3-(4-bu...

journal_title：Molecular pharmacology

authors： Avlani VA,Langmead CJ,Guida E,Wood MD,Tehan BG,Herdon HJ,Watson JM,Sexton PM,Christopoulos A

更新日期：2010-07-01 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：:The ability of chemically distinct ligands to produce different effects on the same G protein-coupled receptor (GPCR) has interesting therapeutic implications, but, if excessively propagated downstream, would introduce biologic noise compromising cognate ligand detection. We asked whether cells have the ability to lim...

journal_title：Molecular pharmacology

authors： Tsvetanova NG,Trester-Zedlitz M,Newton BW,Riordan DP,Sundaram AB,Johnson JR,Krogan NJ,von Zastrow M

更新日期：2017-02-01 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：: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：:Serotonin 5-HT(2B) receptors are often coexpressed with 5-HT(1B) receptors, and cross-talk between the two receptors has been reported in various cell types. However, many mechanistic details underlying 5-HT(1B) and 5-HT(2B) receptor cross-talk have not been elucidated. We hypothesized that 5-HT(2B) and 5-HT(1B) recep...

journal_title：Molecular pharmacology

authors： Janoshazi A,Deraet M,Callebert J,Setola V,Guenther S,Saubamea B,Manivet P,Launay JM,Maroteaux L

更新日期：2007-06-01 00:00:00

abstract：:Bitopic binding properties apply to a variety of muscarinic compounds that span and simultaneously bind to both the orthosteric and allosteric receptor sites. We provide evidence that fluorescent pirenzepine derivatives, with the M1 antagonist fused to the boron-dipyrromethene [Bodipy (558/568)] fluorophore via spacer...

journal_title：Molecular pharmacology

authors： Daval SB,Kellenberger E,Bonnet D,Utard V,Galzi JL,Ilien B

更新日期：2013-07-01 00:00:00

abstract：:Binding by 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) to the Ah receptor leads to transcriptional activation of several genes and a toxicity syndrome that includes tumor promotion, wasting, hormonal and immune system dysfunction, and death. Recent findings indicate that TCDD may also affect cardiac function. Here, we ...

journal_title：Molecular pharmacology

authors： Canga L,Paroli L,Blanck TJ,Silver RB,Rifkind AB

更新日期：1993-12-01 00:00:00

abstract：:Prostaglandin E(2) (PGE(2)), originally discovered as a pro-inflammatory mediator, also inhibits several chemoattractant-elicited neutrophil functions, including adhesion, secretion of cytotoxic enzymes, production of superoxide anions, and chemotaxis. In this study, we have examined the effects of PGE(2) and prostagl...

journal_title：Molecular pharmacology

authors： Burelout C,Thibault N,Levasseur S,Simard S,Naccache PH,Bourgoin SG

更新日期：2004-08-01 00:00:00

abstract：:Cu/Zn-superoxide dismutase (SOD)-accelerated oxidation of the benzene metabolite 1,4-hydroquinone (HQ) results in the enhanced formation of semiquinone anion radicals, electrophilic 1,4-benzoquinone (BQ), and H202. We selected bone marrow stromal cells and phiX-174 double stranded plasmid DNA as model systems to inves...

journal_title：Molecular pharmacology

authors： Li Y,Kuppusamy P,Zweir JL,Trush MA

更新日期：1996-03-01 00:00:00

abstract：:The in vivo bioavailability of exogenous fibroblast growth factor 2 (FGF2) was studied after i.v. injection of uniformly 14C-labeled FGF2 into young rats. 14C-FGF2 was rapidly accumulated in almost all solid organs within 5 min. After 30 min, more than 65% of FGF2 was retained in liver, 4.5% in kidneys, 1.2% in spleen...

journal_title：Molecular pharmacology

authors： Colin S,Jeanny JC,Mascarelli F,Vienet R,Al-Mahmood S,Courtois Y,Labarre J

更新日期：1999-01-01 00:00:00

abstract：:Adenine-uridine rich elements (AREs) play an important role in modulating mRNA stability, being the target site of many ARE-binding proteins (AUBPs) that are involved in the decay process. Three 26-mer 2'-O-methyl oligoribonucleotides (ORNs) homologous to the core region of ARE of bcl2 mRNA have been studied for decoy...

journal_title：Molecular pharmacology

authors： Bevilacqua A,Ghisolfi L,Franzi S,Maresca G,Gherzi R,Capaccioli S,Nicolin A,Canti G

更新日期：2007-02-01 00:00:00

abstract：:The efficacy of antineoplastic compounds can depend heavily on the genetic background of the cells exposed to the drugs. This becomes evident by the fact that HT-29 human colon cancer cells but not primary murine nontransformed colonocytes are efficiently submitted to apoptosis by the flavonoid flavone. By determining...

journal_title：Molecular pharmacology

authors： Wenzel U,Kuntz S,Daniel H

更新日期：2003-12-01 00:00:00