Human gene S31 encodes the pharmacologically defined serotonin 5-hydroxytryptamine1E receptor.

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：: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：:Anandamide (AEA) and delta9-tetrahydrocannabinol (THC) are endogenous and exogenous ligands, respectively, for cannabinoid receptors. Whereas most of the pharmacological actions of cannabinoids are mediated by CB1 receptors, there is also evidence that these compounds can produce effects that are not mediated by the a...

journal_title：Molecular pharmacology

authors： Hejazi N,Zhou C,Oz M,Sun H,Ye JH,Zhang L

更新日期：2006-03-01 00:00:00

abstract：:The ubiquitously expressed nitric oxide (NO) receptor soluble guanylate cyclase (sGC) plays a key role in signal transduction. Binding of NO to the N-terminal prosthetic heme moiety of sGC results in approximately 200-fold activation of the enzyme and an increased conversion of GTP into the second messenger cGMP. sGC ...

journal_title：Molecular pharmacology

authors： Rothkegel C,Schmidt PM,Atkins DJ,Hoffmann LS,Schmidt HH,Schröder H,Stasch JP

更新日期：2007-11-01 00:00:00

abstract：:Understanding the molecular basis of ligand binding to receptors provides insights useful for rational drug design. This work describes development of a new antagonist radioligand of the type 1 cholecystokinin receptor (CCK1R), (2-fluorophenyl)-2,3-dihydro-3-[(3-isoquinolinylcarbonyl)amino]-6-methoxy-2-oxo-l-H-indole-...

journal_title：Molecular pharmacology

authors： Dong M,Vattelana AM,Lam PC,Orry AJ,Abagyan R,Christopoulos A,Sexton PM,Haines DR,Miller LJ

更新日期：2015-01-01 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：:The binding of two anthranilic acid derivatives, glafenic and floctafenic acids, to human erythrocytes and plasma proteins has been investigated in vitro by equilibrium dialysis. Despite their close chemical structures it was shown that the binding of the two compounds to serum albumin, lipoproteins, and erythrocytes ...

journal_title：Molecular pharmacology

authors： Albengres E,Urien S,Riant P,Marcel GA,Tillement JP

更新日期：1987-03-01 00:00:00

abstract：:Although both second messenger response systems are fully functional in both cell lines, activation of muscarinic cholinergic receptors only results in inhibition of adenylate cyclase in NG108-15 neuroblastoma X glioma cells and stimulation of phosphoinositide hydrolysis in 1321N1 human astrocytoma cells. Muscarinic r...

journal_title：Molecular pharmacology

authors： Liang M,Martin MW,Harden TK

更新日期：1987-10-01 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：:Direct gastric mucosal cell damage mediated by nonsteroidal anti-inflammatory drugs (NSAIDs) is involved in the formation of NSAID-induced gastric lesions. We recently suggested that this direct cytotoxicity of NSAIDs is caused by their membrane-permeabilization activity. Geranylgeranylacetone (GGA), a clinically used...

journal_title：Molecular pharmacology

authors： Ushijima H,Tanaka K,Takeda M,Katsu T,Mima S,Mizushima T

更新日期：2005-10-01 00:00:00

abstract：:Aldehyde dehydrogenase-2 (ALDH2) catalyzes vascular bioactivation of the antianginal drug nitroglycerin (GTN) to yield nitric oxide (NO) or a related species that activates soluble guanylate cyclase (sGC), resulting in cGMP-mediated vasodilation. Accordingly, established ALDH2 inhibitors attenuate GTN-induced vasorela...

journal_title：Molecular pharmacology

authors： Neubauer R,Neubauer A,Wölkart G,Schwarzenegger C,Lang B,Schmidt K,Russwurm M,Koesling D,Gorren AC,Schrammel A,Mayer B

更新日期：2013-09-01 00:00:00

abstract：:The aptamer mechanism of action involves the direct interaction of oligonucleotide with protein and is responsible for the biological effects of many pharmacologically active oligodeoxynucleotides. In the work reported here, we have determined the effects of aptamers on the secondary, tertiary, and quaternary structur...

journal_title：Molecular pharmacology

authors： Balasubramanian V,Nguyen LT,Balasubramanian SV,Ramanathan M

更新日期：1998-05-01 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：:The activities of phosphorylase kinase and myosin light-chain kinase are regulated by Ca2+ binding to calmodulin. However, differences in the activation properties of the purified enzymes are apparent, since calmodulin binds to phosphorylase kinase in the absence of Ca2+ whereas prior formation of a Ca2+ . calmodulin ...

journal_title：Molecular pharmacology

authors： Silver PJ,Stull JT

更新日期：1983-05-01 00:00:00

abstract：:This study demonstrates the presence of a novel endothelin (ET) receptor subtype that displays high affinity for both ETA- and ETB-selective ligands. This subtype has been identified in canine spleen membranes using ETB-selective agonists ET-3, IRL-1620, sarafotoxin 6c (S6c) as well as ETA-selective antagonists BQ123 ...

journal_title：Molecular pharmacology

authors： Nambi P,Pullen M,Kincaid J,Nuthulaganti P,Aiyar N,Brooks DP,Gellai M,Kumar C

更新日期：1997-10-01 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：:At sites of inflammation, endothelial cells play a major role in defining the types of leukocytes that are recruited to a specific area. This is accomplished, at least in part, through the cytokine induction of cell surface adhesion molecules, including vascular cell adhesion molecule 1 (VCAM-1). We investigated the r...

journal_title：Molecular pharmacology

authors： Cobb RR,Felts KA,Parry GC,Mackman N

更新日期：1996-06-01 00:00:00

abstract：:The induction of human inducible nitric-oxide synthase (iNOS) expression depends (among other factors) on activation of the signal transducer and activator of transcription 1 (STAT1) pathway. Therefore, the STAT1 pathway may be an appropriate target for the development of inhibitors of iNOS expression. HeLa S3 cells t...

journal_title：Molecular pharmacology

authors： Yao Y,Hausding M,Erkel G,Anke T,Förstermann U,Kleinert H

更新日期：2003-02-01 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：:Matrix metalloproteinases (MMPs) are synthesized in response to diverse stimuli, including cytokines, growth factors, hormones, and oxidative stress. Here we show that the nitric oxide (NO) donor 2-(N,N-diethylamino)-diazenolate-2-oxide (DEA-NO) and NO from murine macrophages transcriptionally regulate MMP-13 expressi...

journal_title：Molecular pharmacology

authors： Zaragoza C,Soria E,López E,Browning D,Balbín M,López-Otín C,Lamas S

更新日期：2002-10-01 00:00:00

abstract：:The spatiotemporal dynamics of opioid signaling in the brain remain poorly defined. Photoactivatable opioid ligands provide a means to quantitatively measure these dynamics and their underlying mechanisms in brain tissue. Although activation kinetics can be assessed using caged agonists, deactivation kinetics are obsc...

journal_title：Molecular pharmacology

authors： Banghart MR,Williams JT,Shah RC,Lavis LD,Sabatini BL

更新日期：2013-11-01 00:00:00

abstract：:We have synthesized and characterized a high-affinity alpha 1-adrenergic receptor probe, 4-amino-6,7-dimethoxy-2[4'- [5"(3"'-125I-iodo-4"'-aminophenyl)pentanoyl]-1'-piperazinyl] quinazoline (125I-A55453). This ligand binds reversibly to rat hepatic plasma membranes with high affinity (KD = 77 +/- 6 pM), and it labels ...

journal_title：Molecular pharmacology

authors： Dickinson KE,Leeb-Lundberg LM,Heald SL,Wikberg JE,DeBernardis JF,Caron MG,Lefkowitz RJ

更新日期：1984-09-01 00:00:00

abstract：:Combinations of coimmunoprecipitation, single-cell fluorescence resonance energy transfer, and cell-surface time-resolved fluorescence resonance energy transfer demonstrated protein-protein interactions and quaternary structure for the alpha(1b)-adrenoceptor. Self-association of transmembrane domain 1 and its interact...

journal_title：Molecular pharmacology

authors： Carrillo JJ,López-Giménez JF,Milligan G

更新日期：2004-11-01 00:00:00

abstract：:The dopamine (DA) transporter (DAT) mediates the removal of released DA. DAT is the major molecular target responsible for the rewarding properties and abuse potential of the psychostimulant amphetamine (AMPH). AMPH has been shown to reduce the number of DATs at the cell surface, and this AMPH-induced cell surface DAT...

journal_title：Molecular pharmacology

authors： Kahlig KM,Lute BJ,Wei Y,Loland CJ,Gether U,Javitch JA,Galli A

更新日期：2006-08-01 00:00:00

abstract：:It has been suggested that the teratogenic effects of the antiepileptic drug valproic acid (VPA) is reflected in vitro by the differentiation of F9 cells, activation of peroxisome proliferator-activated receptor delta (PPARdelta), and inhibition of histone deacetylases (HDACs). The aim of this study was to identify ge...

journal_title：Molecular pharmacology

authors： Lampen A,Grimaldi PA,Nau H

更新日期：2005-07-01 00:00:00

abstract：:Herpes simplex virus type 1 (HSV-1) encodes a thymidine kinase (TK) that markedly differs from mammalian nucleoside kinases in terms of substrate specificity. It recognizes both pyrimidine 2'-deoxynucleosides and a variety of purine nucleoside analogs. Based on a computer modeling study and in an attempt to modify thi...

journal_title：Molecular pharmacology

authors： Degrève B,Esnouf R,De Clercq E,Balzarini J

更新日期：2000-12-01 00:00:00

abstract：:Dantrolene was recently identified as a novel inhibitor of the plasmodial surface anion channel (PSAC), an unusual ion channel on Plasmodium falciparum-infected human red blood cells. Because dantrolene is used clinically, has a high therapeutic index, and has desirable chemical synthetic properties, it may be a lead ...

journal_title：Molecular pharmacology

authors： Kang M,Lisk G,Hollingworth S,Baylor SM,Desai SA

更新日期：2005-07-01 00:00:00

abstract：:Our laboratory recently isolated and sequenced cDNAs encoding the microsomal flavin-containing monooxygenases (FMOs) from rabbit liver and rabbit lung. As a first step in understanding the molecular bases for the catalytic and physical differences between these enzymes, we have expressed them in COS-1 cells and compar...

journal_title：Molecular pharmacology

authors： Lawton MP,Kronbach T,Johnson EF,Philpot RM

更新日期：1991-11-01 00:00:00

abstract：:Metabotropic glutamate receptor 5 (mGlu5) is a target for the treatment of central nervous system (CNS) disorders, such as schizophrenia and Alzheimer's disease. Furthermore, mGlu5 has been shown to play an important role in hippocampal synaptic plasticity, specifically in long-term depression (LTD) and long-term pote...

journal_title：Molecular pharmacology

authors： Noetzel MJ,Gregory KJ,Vinson PN,Manka JT,Stauffer SR,Lindsley CW,Niswender CM,Xiang Z,Conn PJ

更新日期：2013-04-01 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