A new 2-pyrone derivative, 5-bromo-3-(3-hydroxyprop-1-ynyl)-2H-pyran-2-one, suppresses stemness in glioma stem-like cells.

abstract：:Anthracyclines are effective anticancer agents. However, their use is limited by cardiotoxicity, an effect linked to their ability to chelate iron and to perturb iron metabolism (Mol Pharmacol 68:261-271, 2005). These effects on iron-trafficking remain poorly understood, but they are important to decipher because trea...

journal_title：Molecular pharmacology

authors： Xu X,Sutak R,Richardson DR

更新日期：2008-03-01 00:00:00

abstract：:To enable the detailed pharmacological characterization of five bombesin (BN) analogs with respect to the human gastrin-releasing peptide (GRP) receptor, we ectopically expressed the receptor in BALB/3T3 cells. In such cells (termed GR1 cells), GRP stimulated DNA synthesis and Ca2+ mobilization. Two of these analogs, ...

journal_title：Molecular pharmacology

authors： Wu JM,Hoang DO,Feldman RI

更新日期：1995-04-01 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：:The carbocyclic analogue of 5-nitro-2'-deoxyuridine (NO2dUrd), in which the sugar moiety is replaced by a cyclopentane ring and which was designated C-NO2dUrd, has been evaluated for its cytostatic, antimetabolic, and antitumor properties. The following findings are noted. C-NO2dUrd is about 500- to 2000-fold less inh...

journal_title：Molecular pharmacology

authors： Balzarini J,De Clercq E,Herdewijn P,Robins MJ

更新日期：1985-05-01 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：:Large-conductance Ca(2+)-activated K(+) (BK(Ca)) channels play an important role in the regulation of cell physiology in a wide variety of excitable and nonexcitable tissues. Filamin A is a conserved and ubiquitous actin-binding protein that forms perpendicular actin cross-links and contributes to changes in cell shap...

journal_title：Molecular pharmacology

authors： Kim EY,Ridgway LD,Dryer SE

更新日期：2007-09-01 00:00:00

abstract：:We show here that arsenite (As(3+)) elicits multiple effects on gene control, such as the interruption of cell cycle control by initiating G(2)/M arrest as well as inhibiting the aryl hydrocarbon (Ah) receptor-mediated 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD)-inducible expression of CYP1A1. This raises the question ...

journal_title：Molecular pharmacology

authors： Bonzo JA,Chen S,Galijatovic A,Tukey RH

更新日期：2005-04-01 00:00:00

abstract：:Monoamine oxidases (MAOs) A and B, flavin-containing enzymes found in the outer mitochondrial membrane, oxidize many important biogenic and xenobiotic amines. The two enzymes are expressed in many tissues, with some tissues containing primarily one form and others containing both. Although MAO in placental mitochondri...

journal_title：Molecular pharmacology

authors： Riley LA,Waguespack MA,Denney RM

更新日期：1989-07-01 00:00:00

abstract：:The highly conserved aspartate residue in the second transmembrane domain of G protein-coupled receptors is present in position 113 in the type 1 neurotensin receptor (NTR1) but is replaced by an Ala residue in position 79 in the type 2 neurotensin receptor (NTR2). NTR1 couples to Galphaq to stimulate phospholipase C ...

journal_title：Molecular pharmacology

authors： Martin S,Botto JM,Vincent JP,Mazella J

更新日期：1999-02-01 00:00:00

abstract：:Thromboxane A2 stimulation of smooth muscle cells contributes to the development of vascular lesions after percutaneous transluminal coronary angioplasty. In view of this, we examined the signaling pathways stimulated by a thromboxane receptor agonist, U-46619, in cultures of rat aortic smooth muscle cells. Treatment ...

journal_title：Molecular pharmacology

authors： Jones DA,Benjamin CW,Linseman DA

更新日期：1995-11-01 00:00:00

abstract：:The L-type amino acid transporter 1 (LAT1) is an Na(+)-independent neutral amino acid transporter subserving the amino acid transport system L. Because of its broad substrate selectivity, system L has been proposed to be responsible for the permeation of amino acid-related drugs through the plasma membrane. To underst...

journal_title：Molecular pharmacology

authors： Uchino H,Kanai Y,Kim DK,Wempe MF,Chairoungdua A,Morimoto E,Anders MW,Endou H

更新日期：2002-04-01 00:00:00

abstract：:The chemokine receptor CCR2 is a G protein-coupled receptor that is activated primarily by the endogenous CC chemokine ligand 2 (CCL2). Many different small-molecule antagonists have been developed to inhibit this receptor, as it is involved in a variety of diseases characterized by chronic inflammation. Unfortunately...

journal_title：Molecular pharmacology

authors： Zweemer AJ,Nederpelt I,Vrieling H,Hafith S,Doornbos ML,de Vries H,Abt J,Gross R,Stamos D,Saunders J,Smit MJ,Ijzerman AP,Heitman LH

更新日期：2013-10-01 00:00:00

abstract：:The cDNA for the rat alpha 1c-adrenergic receptor (AR) has been cloned using a probe derived from the bovine alpha 1c-AR sequence. Clone rB7a has a 2.6-kilobase insert with a 1390-base pair open reading frame and encodes a receptor of 466 amino acids. The cloned receptor has 91% amino acid identity with the bovine alp...

journal_title：Molecular pharmacology

authors： Laz TM,Forray C,Smith KE,Bard JA,Vaysse PJ,Branchek TA,Weinshank RL

更新日期：1994-09-01 00:00:00

abstract：:The glucagon-like peptide-1 receptor (GLP-1R) is a key physiological regulator of insulin secretion and a major therapeutic target for the treatment of type II diabetes. However, regulation of GLP-1R function is complex with multiple endogenous peptides that interact with the receptor, including full-length (1-37) and...

journal_title：Molecular pharmacology

authors： Koole C,Wootten D,Simms J,Valant C,Miller LJ,Christopoulos A,Sexton PM

更新日期：2011-09-01 00:00:00

abstract：:Mitochondrial disorders are devastating genetic diseases for which efficacious therapies are still an unmet need. Recent studies report that increased availability of intracellular NAD obtained by inhibition of the NAD-consuming enzyme poly(ADP-ribose) polymerase (PARP)-1 or supplementation with the NAD-precursor nico...

journal_title：Molecular pharmacology

authors： Felici R,Lapucci A,Cavone L,Pratesi S,Berlinguer-Palmini R,Chiarugi A

更新日期：2015-06-01 00:00:00

abstract：:The cannabinoid analog abnormal cannabidiol [abn-cbd; (-)-4-(3-3,4-trans-p-menthadien-[1,8]-yl)-olivetol] does not bind to CB(1) or CB(2) receptors, yet it acts as a full agonist in relaxing rat isolated mesenteric artery segments. Vasorelaxation by abn-cbd is endothelium-dependent, pertussis toxin-sensitive, and is i...

journal_title：Molecular pharmacology

authors： Offertáler L,Mo FM,Bátkai S,Liu J,Begg M,Razdan RK,Martin BR,Bukoski RD,Kunos G

更新日期：2003-03-01 00:00:00

abstract：:Glutamatergic synaptic transmitters are cleared from the synaptic cleft through excitatory amino acid transporters (EAATs) that are responsible for recycling glutamate and transporting it into neurons and glial cells. To probe the structural role of the TM4b-4c loop of EAAT1 (Rattus norvegicus), each of the 57 amino a...

journal_title：Molecular pharmacology

authors： Zhang W,Zhang X,Qu S

更新日期：2018-07-01 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：:Several 2-amino-3-benzoylthiophenes were found to increase the binding of [3H]N6-cyclohexyladenosine to A1 adenosine receptors in rat brain membranes. Concentration-response curves were bell-shaped, with up to 45% stimulation of binding at 10 microM followed by inhibition at higher concentrations. Because these compou...

journal_title：Molecular pharmacology

authors： Bruns RF,Fergus JH

更新日期：1990-12-01 00:00:00

abstract：:ATP-gated purinergic receptors (P2XRs) are a family of cation-permeable channels that conduct Ca(2+) and facilitate voltage-sensitive Ca(2+) entry in excitable cells. To study Ca(2+) signaling by P2XRs and its dependence on voltage-sensitive Ca(2+) influx, we expressed eight cloned P2XR subtypes individually in gonado...

journal_title：Molecular pharmacology

authors： Koshimizu TA,Van Goor F,Tomić M,Wong AO,Tanoue A,Tsujimoto G,Stojilkovic SS

更新日期：2000-11-01 00:00:00

abstract：:Chronic stimulation of beta-adrenoceptors leads to increased mRNA and protein levels of pertussis toxin (PTX)-sensitive guanine nucleotide-binding proteins (G proteins) in the heart. In the present study the time course is reported of the effect of isoprenaline infusions on myocardial mRNA levels of Gi alpha-2, Gi alp...

journal_title：Molecular pharmacology

authors： Eschenhagen T,Mende U,Diederich M,Nose M,Schmitz W,Scholz H,Schulte am Esch J,Warnholtz A,Schäfer H

更新日期：1992-11-01 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：:An 'epoxygenase' eicosanoid analog, 14, 15-cis-episulfide-eicosatrienoic acid, has several unique pharmacological effects on platelets. These include (i) inhibition of ionophore A23187- but not thrombin-induced activation, (ii) inhibition of thromboxane B2 biosynthesis derived from endogenous but not exogenous arachid...

journal_title：Molecular pharmacology

authors： Bernstrom K,Malcolm K,McGee J,Maclouf J,Levy-Toledano S,Falck JR,Fitzpatrick FA

更新日期：1991-02-01 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：:The use of classic antipsychotic drugs is limited by the occurrence of extrapyramidal motor symptoms, which are caused by dopamine (DA) receptor blockade in the neostriatum. We examined the impact of early-life stress on haloperidol-induced catalepsy using the rat model of prenatal restraint stress (PRS). Adult "PRS r...

journal_title：Molecular pharmacology

authors： Marrocco J,Mairesse J,Bucci D,Lionetto L,Battaglia G,Consolazione M,Ravasi L,Simmaco M,Morley-Fletcher S,Maccari S,Nicoletti F

更新日期：2013-08-01 00:00:00

abstract：:EM-652 (SCH 57068) is a new orally active antiestrogen that demonstrates pure antagonistic effects in the mammary gland and endometrium. In vivo studies have shown that EM-652 is primarily glucuronidated at the 7-hydroxy position in rats and that the metabolite is present in the plasma of female monkeys and human subj...

journal_title：Molecular pharmacology

authors： Barbier O,Albert C,Martineau I,Vallée M,High K,Labrie F,Hum DW,Labrie C,Bélanger A

更新日期：2001-03-01 00:00:00

abstract：:The ability of dopamine agonists and antagonists to compete with [3H]spiperone binding to rat striatal membrane preparations at 4, 15, 26, and 37 degrees varied markedly with temperature. Dopamine and the dopamine agonist 2-amino-6,7-dihydroxy-1,2,3,4-tetrahydronaphthalene hydrobromide (ADTN) were more potent at lower...

journal_title：Molecular pharmacology

authors： Kilpatrick GJ,el Tayar N,Van de Waterbeemd H,Jenner P,Testa B,Marsden CD

更新日期：1986-09-01 00:00:00

abstract：:Up-regulation of fractalkine is involved in vascular and tissue damage in inflammatory conditions. Resveratrol has been shown to have anti-inflammatory, antioxidant, and antitumor activities. Its regulatory effects on expression of fractalkine in vascular endothelial cells and fractalkine receptor CX3CR1 in monocytes ...

journal_title：Molecular pharmacology

authors： Moon SO,Kim W,Sung MJ,Lee S,Kang KP,Kim DH,Lee SY,So JN,Park SK

更新日期：2006-07-01 00:00:00

abstract：:Iron-loading diseases remain an important problem because of the toxicity of iron-catalyzed redox reactions. Iron loading occurs in the mitochondria of Friedreich's ataxia (FA) patients and may play a role in its pathogenesis. This suggests that iron chelation therapy could be useful. We developed previously the lipop...

journal_title：Molecular pharmacology

authors： Lim CK,Kalinowski DS,Richardson DR

更新日期：2008-07-01 00:00:00

abstract：:Several lines of evidence suggest that G-protein-coupled receptors can adopt different active conformations, but their direct demonstration in intact cells is still missing. Using a fluorescence resonance energy transfer (FRET)-based approach we studied conformational changes in alpha(2A)-adrenergic receptors in intac...

journal_title：Molecular pharmacology

authors： Zürn A,Zabel U,Vilardaga JP,Schindelin H,Lohse MJ,Hoffmann C

更新日期：2009-03-01 00:00:00