Determinants of specificity for alpha-conotoxin MII on alpha3beta2 neuronal nicotinic receptors.

abstract：:Circular RNAs (circRNAs) are a distinct category of single-stranded, covalently closed RNAs formed by backsplicing. The functions of circRNAs are incompletely known and are under active investigation. Here, we report that in addition to traditional linear mRNAs (linRNA), mouse, rat, and human opioid receptor genes gen...

journal_title：Molecular pharmacology

authors： Irie T,Shum R,Deni I,Hunkele A,Le Rouzic V,Xu J,Wilson R,Fischer GW,Pasternak GW,Pan YX

更新日期：2019-08-01 00:00:00

abstract：:We examined the subtype-selective binding site of the beta-adrenergic receptors (betaARs). The beta(1)/beta(2)-chimeric receptors showed the importance of the second and seventh transmembrane domains (TM2 and TM7) of the beta(2)AR for the binding of the beta(2)-selective agonists such as formoterol and procaterol. Ala...

journal_title：Molecular pharmacology

authors： Isogaya M,Sugimoto Y,Tanimura R,Tanaka R,Kikkawa H,Nagao T,Kurose H

更新日期：1999-11-01 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：:The small GTPase Rac1 has been widely implicated in mammary tumorigenesis and metastasis. Previous studies established that stimulation of ErbB receptors in breast cancer cells activates Rac1 and enhances motility via the Rac-guanine nucleotide exchange factor P-Rex1. As the Janus tyrosine kinase 2 (Jak2)/signal trans...

journal_title：Molecular pharmacology

authors： Lopez-Haber C,Kazanietz MG

更新日期：2013-05-01 00:00:00

abstract：:The fluorogenic sulfhydryl probe 7-diethylamino-3-(4'-maleimidylphenyl)-4-methylcoumarin (CPM) (1-50 nM) is used to characterize the functional role and location of highly reactive thiol groups on the ryanodine-sensitive Ca2+ release channel complex [i.e., ryanodine receptors (RyRs)] of skeletal and cardiac junctional...

journal_title：Molecular pharmacology

authors： Liu G,Abramson JJ,Zable AC,Pessah IN

更新日期：1994-02-01 00:00:00

abstract：:Although the thiopurine drugs 6-mercaptopurine (6-MP) and 6-thioguanine (6-TG) are well established agents for the treatment of leukemia, controversies remain regarding their main mode of action. Previous evidence has suggested that although 6-TG exerts a cytotoxic effect through incorporation of 6-thioguanine nucleot...

journal_title：Molecular pharmacology

authors： Coulthard SA,Hogarth LA,Little M,Matheson EC,Redfern CP,Minto L,Hall AG

更新日期：2002-07-01 00:00:00

abstract：:N-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) induces Parkinson-like symptoms in humans, nonhuman primates, and mice. Several studies suggest that MPTP is metabolized by monoamine oxidase (MAO) type B to yield N-methyl-4-phenyl-pyridinium (MPP+), which is responsible for the neurotoxic effects of the drug. In th...

journal_title：Molecular pharmacology

authors： Itzhak Y,Mash D,Zhang SH,Stein I

更新日期：1991-03-01 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：:Using [3H]leukotriene C4 (LTC4) and radioligand-binding techniques, specific leukotriene C4 binding sites have been identified in membranes derived from guinea pig ventricular myocardium. High performance liquid chromatography analyses indicated that, in the presence of the gamma-glutamyl transpeptidase inhibitor L-se...

journal_title：Molecular pharmacology

authors： Hogaboom GK,Mong S,Stadel JM,Crooke ST

更新日期：1985-02-01 00:00:00

abstract：:The dopamine D3 receptor, although structurally similar to the dopamine D2 receptor, has 100-fold higher affinity for agonists such as dopamine and quinpirole, when these receptors are expressed in 293 cells. Additionally, the D3 receptor has generally lower affinity for several antagonists than does the D2 receptor. ...

journal_title：Molecular pharmacology

authors： Robinson SW,Jarvie KR,Caron MG

更新日期：1994-08-01 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：:Chemokine receptors belong to the class A of G protein-coupled receptors (GPCRs) and are implicated in a wide variety of physiologic functions, mostly related to the homeostasis of the immune system. Chemokine receptors are also involved in multiple pathologic processes, including immune and autoimmune diseases, as we...

journal_title：Molecular pharmacology

authors： Arimont M,Hoffmann C,de Graaf C,Leurs R

更新日期：2019-12-01 00:00:00

abstract：:We showed previously that microtubule disassembly by vinblastine induces the proto-oncogene c-myc in epithelial mammary HBL100 cells. In this study, we demonstrate that vinblastine treatment in these cells, in contrast to what was observed with the colon adenocarcinoma cell line HT29-D4, activated the transcription fa...

journal_title：Molecular pharmacology

authors： Bourgarel-Rey V,Vallee S,Rimet O,Champion S,Braguer D,Desobry A,Briand C,Barra Y

更新日期：2001-05-01 00:00:00

abstract：:UDP-glucuronosyltransferase (UGT) 1A1 (UGT1A1) catalyzes the glucuronidation of bilirubin in liver. Among all UGT isoforms identified to date, it is the only relevant bilirubin-glucuronidating enzyme in human. Because glucuronoconjugation is the major route of bilirubin elimination, any genetic alteration that affects...

journal_title：Molecular pharmacology

authors： Bernard P,Goudonnet H,Artur Y,Desvergne B,Wahli W

更新日期：1999-09-01 00:00:00

abstract：:Acetylsalicylic acid (aspirin) is a cyclooxygenase (COX) inhibitor, yet some of its therapeutic effects are thought to derive from mechanisms unrelated to prostaglandin synthesis inhibition. In human intestinal myofibroblasts, aspirin, at therapeutic doses, had the unexpected effect of inducing prolonged COX-2 express...

journal_title：Molecular pharmacology

authors： Mifflin RC,Saada JI,Di Mari JF,Valentich JD,Adegboyega PA,Powell DW

更新日期：2004-02-01 00:00:00

abstract：:It has been demonstrated previously that cannabinol (CBN) differentially modulates interleukin-2 (IL-2) protein secretion by T cells with a corresponding change in extracellular signal-regulated kinase activity. The objective of the present studies was to further investigate the molecular mechanism by which CBN enhanc...

journal_title：Molecular pharmacology

authors： Jan TR,Rao GK,Kaminski NE

更新日期：2002-02-01 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：: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 binding kinetics of [3H]Ro 15-1788, a selective benzodiazepine receptor antagonist, to synaptosomal membranes of rat cerebral cortices was studied. [3H]Ro 15-1788 binds with high affinity (dissociation constant, 0.53 nM) to a single class of binding sites (maximal binding capacity, 1.97 pmoles/mg of protein). Equi...

journal_title：Molecular pharmacology

authors： Chiu TH,Rosenberg HC

更新日期：1983-03-01 00:00:00

abstract：:G protein-coupled receptors (GPCRs) contribute to the regulation of every aspect of human physiology and are therapeutic targets for the treatment of numerous diseases. As a consequence, understanding the myriad of mechanisms controlling GPCR signaling and trafficking is essential for the development of new pharmacolo...

journal_title：Molecular pharmacology

authors： Dunn HA,Ferguson SS

更新日期：2015-10-01 00:00:00

abstract：:The binding of agonists and antagonists to alpha 2-adrenergic receptors of human platelets was studied. The receptors showed homogeneous affinities for antagonists but two affinity states for the agonist (-)-epinephrine, which were modulated by guanine nucleotides. Van't Hoff plots of antagonist binding had a break po...

journal_title：Molecular pharmacology

authors： Lohse MJ,Klotz KN,Schwabe U

更新日期：1986-03-01 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 role of the cGMP-dependent protein kinase (cGK) and one of its major substrates, the vasodilator-stimulated phosphoprotein (VASP), in the regulation of a receptor-evoked calcium response was investigated. The human type I beta cGK was stably transfected in human embryonic kidney 293 cells and Swiss mouse 3T6 fibro...

journal_title：Molecular pharmacology

authors： Meinecke M,Geiger J,Butt E,Sandberg M,Jahnsen T,Chakraborty T,Walter U,Jarchau T,Lohmann SM

更新日期：1994-08-01 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：:Healing of gastrointestinal mucosal lesions occurs through two processes: an early one involving cell migration and a later one in which cell division replaces lost cells. Both processes require the presence of polyamines, but the mechanism of action of these compounds is unknown. In the present study, we examined the...

journal_title：Molecular pharmacology

authors： McCormack SA,Zimmerman BJ,Israel M,Blanner P,Johnson LR

更新日期：1995-10-01 00:00:00

abstract：:Lysophosphatidic acid (LPA) and sphingosine-1-phosphate (S1P) are members of the phospholipid growth factor family. A major limitation in the field to date has been a lack of receptor subtype-specific agonists and antagonists. Here, we report that dioctylglycerol pyrophosphate and dioctylphosphatidic acid are selectiv...

journal_title：Molecular pharmacology

authors： Fischer DJ,Nusser N,Virag T,Yokoyama K,Wang Da,Baker DL,Bautista D,Parrill AL,Tigyi G

更新日期：2001-10-01 00:00:00

abstract：:Nitric oxide (NO) promotes retinal and choroidal neovascularization, although different isoforms of nitric-oxide synthetase (NOS) are critical in each. Deficiency of endothelial NOS (eNOS) suppresses retinal but not choroidal neovascularization, whereas deficiency of neuronal NOS (nNOS) or inducible NOS (iNOS) suppres...

journal_title：Molecular pharmacology

authors： Ando A,Yang A,Nambu H,Campochiaro PA

更新日期：2002-09-01 00:00:00

abstract：:The gonadotropin-releasing hormone receptor (GnRH-R) of the African catfish couples to phospholipase C and belongs to the large family of G protein-coupled receptors. We recently demonstrated that removal of the carboxyl-terminal tail (S331-Q379) from the catfish GnRH-R results in a loss of agonist binding; the curren...

journal_title：Molecular pharmacology

authors： Blomenröhr M,Heding A,Sellar R,Leurs R,Bogerd J,Eidne KA,Willars GB

更新日期：1999-12-01 00:00:00

abstract：:Phosphorylation of G protein-coupled receptors (GPCRs) by GPCR kinases (GRKs) is a major mechanism of desensitization of these receptors. GPCR activation of GRKs involves an allosteric site on GRKs distinct from the catalytic site. Although recent studies have suggested an important role of the N- and C-termini and do...

journal_title：Molecular pharmacology

authors： Baameur F,Morgan DH,Yao H,Tran TM,Hammitt RA,Sabui S,McMurray JS,Lichtarge O,Clark RB

更新日期：2010-03-01 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