Activation of thromboxane and prostacyclin receptors elicits opposing effects on vascular smooth muscle cell growth and mitogen-activated protein kinase signaling cascades.

abstract：:The effect of mercuric acetate on the activities of deoxyuridine triphosphate nucleotidohydrolase (dUTPase), DNA polymerase (alpha, beta), and uracil-DNA glycosylase has been studied in cultured human KB cells. There was a dose- and time-dependent inactivation of both dUTPase and DNA polymerase alpha activities by mer...

journal_title：Molecular pharmacology

authors： Williams MV,Winters T,Waddell KS

更新日期：1987-02-01 00:00:00

abstract：:Activators of G protein signaling (AGS), initially discovered in the search for receptor-independent activators of G protein signaling, define a broad panel of biologic regulators that influence signal transfer from receptor to G-protein, guanine nucleotide binding and hydrolysis, G protein subunit interactions, and/o...

journal_title：Molecular pharmacology

authors： Blumer JB,Lanier SM

更新日期：2014-03-01 00:00:00

abstract：:The 90-kDa heat shock family (HSP90) of protein and two-component histidine kinases, although quite distinct at the primary amino acid sequence level, share a common structural ATP-binding domain known as the Bergerat fold. The Bergerat fold is important for the ATPase activity and associated chaperone function of HSP...

journal_title：Molecular pharmacology

authors： Besant PG,Lasker MV,Bui CD,Turck CW

更新日期：2002-08-01 00:00:00

abstract：:Large conductance, Ca(2+)-activated K+ channels are believed to underlie interburst intervals and, thus, contribute to the control of hormone release from neurohypophysial terminals. Because ethanol inhibits the release of vasopressin and oxytocin, we studied its effects on large conductance, Ca(2+)-activated K+ chann...

journal_title：Molecular pharmacology

authors： Dopico AM,Lemos JR,Treistman SN

更新日期：1996-01-01 00:00:00

abstract：:Sulfation, catalyzed by members of the sulfotransferase (SULT) superfamily, exerts considerable influence over the biological activity of numerous endogenous and xenobiotic chemicals. In humans, catecholamines such as dopamine are extensively sulfated, and a SULT isoform (SULT1A3 or the monoamine-sulfating form of phe...

journal_title：Molecular pharmacology

authors： Dajani R,Hood AM,Coughtrie MW

更新日期：1998-12-01 00:00:00

abstract：:Studies of the biochemical mechanisms evoked by conventional treatments for neoplastic diseases point to apoptosis as a key process for elimination of unwanted cells. Although the pathways through which chemotherapeutics promote cell death remain largely unknown, caspase proteases play a central role in the induction ...

journal_title：Molecular pharmacology

authors： Benjamin CW,Hiebsch RR,Jones DA

更新日期：1998-03-01 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 human caudate and putamen contain two high affinity binding sites for [3H]spiroperidol. Both of these affinity states exhibit dopaminergic selectivity. Ascorbic acid, at 0.1 mM, induces a slow loss of the low affinity component of [3H]spiroperidol binding in these tissues. The addition of guanyl nucleotides to the...

journal_title：Molecular pharmacology

authors： Andorn AC,Bacon BR,Nguyen-Hunh AT,Parlato SJ,Stitts JA

更新日期：1988-02-01 00:00:00

abstract：:alpha 1-Adrenergic receptor (alpha 1-AR) agonists elevate the intracellular calcium concentration ([Ca2+]i) in 60-80% of astroglia in vitro. Likewise, 60-70% of astroglia exhibit specific binding sites for the alpha 1-AR-selective antagonist (+-)-125I-[beta-(4-hydroxyphenyl)-ethylaminomethyl]tetralone. The density of ...

journal_title：Molecular pharmacology

authors： Shao Y,McCarthy KD

更新日期：1993-08-01 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：:We have previously identified allosteric modulators of the cannabinoid CB(1) receptor (Org 27569, PSNCBAM-1) that display a contradictory pharmacological profile: increasing the specific binding of the CB(1) receptor agonist [(3)H]CP55940 but producing a decrease in CB(1) receptor agonist efficacy. Here we investigate...

journal_title：Molecular pharmacology

authors： Baillie GL,Horswill JG,Anavi-Goffer S,Reggio PH,Bolognini D,Abood ME,McAllister S,Strange PG,Stephens GJ,Pertwee RG,Ross RA

更新日期：2013-02-01 00:00:00

abstract：:Voltage-gated sodium channels (Navs) are promising targets for analgesic and antiepileptic therapies. Although specificity between Nav subtypes may be desirable to target specific neural types, such as nociceptors in pain, many broadly acting Nav inhibitors are clinically beneficial in neuropathic pain and epilepsy. H...

journal_title：Molecular pharmacology

authors： Hinckley CA,Kuryshev Y,Sers A,Barre A,Buisson B,Naik H,Hajos M

更新日期：2021-01-01 00:00:00

abstract：:Recent clinical studies reveal that selective agonists of group II metabotropic glutamate (mGlu) receptors have robust efficacy in treating positive and negative symptoms in patients with schizophrenia. Group II mGlu receptor agonists also modulate the in vivo activity of psychotomimetic drugs and reduce the ability o...

journal_title：Molecular pharmacology

authors： Benneyworth MA,Xiang Z,Smith RL,Garcia EE,Conn PJ,Sanders-Bush E

更新日期：2007-08-01 00:00:00

abstract：:NS20Y neuroblastoma cells expressing a homogeneous population of D1-dopamine receptors were used in the present study as a model system to investigate the mechanisms of agonist-induced stimulation and desensitization of D1 receptor-coupled adenylyl cyclase activity. Membrane prepared from NS20Y cells showed a pharmaco...

journal_title：Molecular pharmacology

authors： Barton AC,Sibley DR

更新日期：1990-10-01 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：:A central axiom of ligand-receptor theory is that agonists bind more tightly to active than to inactive receptors. However, measuring agonist affinity in inactive receptors is confounded by concomitant activation. We identified a cysteine substituted mutant γ-aminobutyric acid type A (GABAA) receptor with unique chara...

journal_title：Molecular pharmacology

authors： Stewart DS,Hotta M,Desai R,Forman SA

更新日期：2013-06-01 00:00:00

abstract：:The effects of the insulin-releasing sulfonylurea tolbutamide on the cytoplasmic Ca2+ concentration [( Ca2+]i) in individual pancreatic beta-cells or suspensions of beta-cells were analyzed using the probe fura-2 and dual-wavelength fluorometry. Subsequent additions of 1, 10, and 100 microM tolbutamide induced a grade...

journal_title：Molecular pharmacology

authors： Grapengiesser E,Gylfe E,Hellman B

更新日期：1990-03-01 00:00:00

abstract：:Capsaicin (vanilloid) sensitivity has long served as the functional signature of a subset of nociceptive sensory neurons. Mutagenesis studies have revealed seemingly distinct regions involved in mediating ligand binding and channel activation at the capsaicin binding site. Residue 547 (transmembrane region 4) mediates...

journal_title：Molecular pharmacology

authors： Johnson DM,Garrett EM,Rutter R,Bonnert TP,Gao YD,Middleton RE,Sutton KG

更新日期：2006-09-01 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：: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：:Prostate cancer is a highly heterogenous disease in which a patient-tailored care program is much desired. Central to this goal is the development of novel targeted pharmacological interventions. To develop these treatment strategies, an understanding of the integration of cellular pathways involved in both tumorigene...

journal_title：Molecular pharmacology

authors： Assinder SJ,Dong Q,Mangs H,Richardson DR

更新日期：2009-03-01 00:00:00

abstract：:Magnesium modulates hormone-sensitive adenylate cyclase activation. In the present studies, we have examined the magnesium requirement of beta-adrenergic-stimulated adenylate cyclase activity in permeabilized human lymphocytes. Following isoproterenol pretreatment, under conditions that lead to homologous beta-adrener...

journal_title：Molecular pharmacology

authors： Feldman RD

更新日期：1989-03-01 00:00:00

abstract：:Cocaine use poses a major health problem not only because of the dependence it causes but also because of the generation of life-threatening cardiac arrhythmias following overdose. Elucidating the molecular mechanisms of action of cocaine, therefore, remains a critical step in developing treatment for cocaine addictio...

journal_title：Molecular pharmacology

authors： Premkumar LS

更新日期：1999-12-01 00:00:00

abstract：:The effects of the dihydropyridine calcium channel agonist Bay K 8644 on indo-1-loaded Jurkat human leukemia T lymphocytes was assessed by flow cytometry. Bay K 8644 from 10(-9) to 10(-4) M caused a dose-dependent rise in the intracellular free Ca concentration, an effect that was not mimicked by the dihydropyridine C...

journal_title：Molecular pharmacology

authors： Young W,Chen J,Jung F,Gardner P

更新日期：1988-09-01 00:00:00

abstract：:The orphan nuclear receptor liver receptor homolog 1 (LRH-1; NR5A2) is a potent regulator of cholesterol metabolism and bile acid homeostasis. Recently, LRH-1 has been shown to play an important role in intestinal inflammation and in the progression of estrogen receptor positive and negative breast cancers and pancrea...

journal_title：Molecular pharmacology

authors： Corzo CA,Mari Y,Chang MR,Khan T,Kuruvilla D,Nuhant P,Kumar N,West GM,Duckett DR,Roush WR,Griffin PR

更新日期：2015-02-01 00:00:00

abstract：:An investigation of the conformational profiles of two cyclic delta-selective opioid peptides, [D-Pen2,D-Pen5]-enkephalin and [D-Pen2,L-Pen5]-enkephalin, has been made. The methods and procedures used are more extensive and systematic than those previously reported, involving a combination of nested grid rotations, cy...

journal_title：Molecular pharmacology

authors： Chew C,Villar HO,Loew GH

更新日期：1991-04-01 00:00:00

abstract：:The pharmacological preservation of bone in the ovariectomized rat by estrogen, selective estrogen receptor modulators (SERMs), and bisphosphonates has been well described. However, comprehensive molecular analysis of the effects of these pharmacologically diverse antiresorptive agents on gene expression in bone has n...

journal_title：Molecular pharmacology

authors： Helvering LM,Liu R,Kulkarni NH,Wei T,Chen P,Huang S,Lawrence F,Halladay DL,Miles RR,Ambrose EM,Sato M,Ma YL,Frolik CA,Dow ER,Bryant HU,Onyia JE

更新日期：2005-11-01 00:00:00

abstract：:Previous studies indicated that activation of alpha 1-adrenergic receptors in BC3H-1 muscle cells (S. K. Ambler and P. Taylor, J. Biol. Chem. 261:5866-5871, 1986) and muscarinic receptors in 1321N1 astrocytoma cells (S. B. Masters, T. K. Harden, and J. H. Brown, Mol. Pharmacol. 27:325-332, 1985) resulted in the rapid ...

journal_title：Molecular pharmacology

authors： Ambler SK,Thompson B,Solski PA,Brown JH,Taylor P

更新日期：1987-09-01 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：:The expression and molecular regulation of the cytochrome P450IA (P450IA) gene subfamily have been examined in rat hepatic tissue after treatment with pyridine. The microsomal ethoxyresorufin O-deethylase activity, which has been shown to be specific for the P450IA subfamily, was increased approximately 2- and 3.5-fol...

journal_title：Molecular pharmacology

authors： Kim SG,Reddy SL,States JC,Novak RF

更新日期：1991-07-01 00:00:00