A novel EPAC-specific inhibitor suppresses pancreatic cancer cell migration and invasion.

abstract：:Cannabinoids have been implicated in the reduction of glioma growth. The present study investigated a possible relationship between the recently shown induction of cyclooxygenase (COX)-2 expression by the endocannabinoid analog R(+)methanandamide [R(+)-MA] and its effect on the viability of H4 human neuroglioma cells....

journal_title：Molecular pharmacology

authors： Hinz B,Ramer R,Eichele K,Weinzierl U,Brune K

更新日期：2004-12-01 00:00:00

abstract：:The anticancer agent 2-cyano-3,12-dioxooleana-1,9-dien-28-oic acid (CDDO) and its methyl ester (CDDO-Me) typically induce a broad spectrum of growth-inhibitory, proapoptotic, and antiangiogenic responses. Treatment of Panc1, Panc28, and L3.6pL pancreatic cancer cells with low micromolar concentrations of CDDO or CDDO-...

journal_title：Molecular pharmacology

authors： Jutooru I,Chadalapaka G,Abdelrahim M,Basha MR,Samudio I,Konopleva M,Andreeff M,Safe S

更新日期：2010-08-01 00:00:00

abstract：:Studies investigating the effects of beta-naphthoflavone (beta NF) on insulin receptor binding and its intrinsic protein kinase activity in rat liver and placenta were performed. Membranes were prepared from maternal liver and placenta on gestation day 11 and used for [125I]insulin radioreceptor assay. Scatchard analy...

journal_title：Molecular pharmacology

authors： Wang SL,Raizada MK,Shiverick KT

更新日期：1988-03-01 00:00:00

abstract：:The selective inactivation by 17 beta-substituted steroids of rabbit and rat liver cytochromes P-450 involved in the 21-hydroxylation of progesterone has been investigated. Five derivatives each of pregnenolone and progesterone were prepared, in which the methylketo substituent of the 17 beta-position was replaced by ...

journal_title：Molecular pharmacology

authors： Halpert J,Jaw JY,Balfour C

更新日期：1989-01-01 00:00:00

abstract：:The carbonic anhydrase (CA) isozyme (IV) in microsomes is thought to have a dominant role in secretory processes. Using microsomes from bovine kidney and lung (which had the same activity), we have measured the Km and kcat for CO2 hydration and compared these numbers with those for CA I (red blood cells and gut), CA I...

journal_title：Molecular pharmacology

authors： Maren TH,Wynns GC,Wistrand PJ

更新日期：1993-10-01 00:00:00

abstract：:The binding of [3H]Hspiroperidol to D2 dopaminergic receptors in rat striatum was compared to the binding of [3H]dopamine to its binding sites. Both radioligands labeled apparently homogeneous populations of high affinity, stereoselective, saturable sites, determined from analysis of saturation isotherms. [3H]Spiroper...

journal_title：Molecular pharmacology

authors： Hancock AA,Marsh CL

更新日期：1984-11-01 00:00:00

abstract：:C57BL/6J (C57) and DBA/JBOMf (DBA) mice were used to study the role of adipose tissue as a modifier of tissue distribution, biological effects, and elimination of a lipophilic foreign chemical, 2,4,5,2',4',5'-hexachlorobiphenyl (HCB). As an indication of biological potency of the model compound, the activities of hepa...

journal_title：Molecular pharmacology

authors： Ahotupa M,Mäntylä E

更新日期：1983-11-01 00:00:00

abstract：:Nitric oxide (NO) possesses potent anti-inflammatory properties; however, an over-production of NO will promote inflammation and induce cell and tissue dysfunction. Thus, the ability to precisely regulate NO production could prove beneficial in controlling damage. In this study, advantage was taken of the well charact...

journal_title：Molecular pharmacology

authors： Bian K,Harari Y,Zhong M,Lai M,Castro G,Weisbrodt N,Murad F

更新日期：2001-04-01 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：:Identifying novel mechanisms to enhance glucagon-like peptide-1 (GLP-1) receptor signaling may enable nascent medicinal chemistry strategies with the aim of developing new orally available therapeutic agents for the treatment of type 2 diabetes mellitus. Therefore, we tested the hypothesis that selectively modulating ...

journal_title：Molecular pharmacology

authors： Willard FS,Wootten D,Showalter AD,Savage EE,Ficorilli J,Farb TB,Bokvist K,Alsina-Fernandez J,Furness SG,Christopoulos A,Sexton PM,Sloop KW

更新日期：2012-12-01 00:00:00

abstract：:Hepatic very-low-density lipoprotein particles (VLDL) containing full-length apolipoprotein B100 are metabolized in the blood stream to low-density lipoprotein (LDL) particles, whose elevated levels increase the risk of atherosclerosis. Statins and bile-acid sequestrants are effective LDL-lowering therapies for many p...

journal_title：Molecular pharmacology

authors： Yang Y,Ballatori N,Smith HC

更新日期：2002-02-01 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：:Trypanosoma brucei encodes a relatively high number of genes of the equilibrative nucleoside transporter (ENT) family. We report here the cloning and in-depth characterization of one T. brucei brucei ENT member, TbNT9/AT-D. This transporter was expressed in Saccharomyces cerevisiae and displayed a uniquely high affini...

journal_title：Molecular pharmacology

authors： Al-Salabi MI,Wallace LJ,Lüscher A,Mäser P,Candlish D,Rodenko B,Gould MK,Jabeen I,Ajith SN,de Koning HP

更新日期：2007-03-01 00:00:00

abstract：:15-Deoxy delta(12,14)-prostaglandin J(2) (15d-PGJ(2)), an activator of peroxisome proliferator-activated receptor (PPAR)-gamma and -delta, is a prostanoid metabolite with anti-inflammatory actions. In intrauterine tissues, proinflammatory cytokines and prostaglandins have been identified as playing key roles in the ma...

journal_title：Molecular pharmacology

authors： Berry EB,Keelan JA,Helliwell RJ,Gilmour RS,Mitchell MD

更新日期：2005-07-01 00:00:00

abstract：:The aliphatic adenine analogues, D-eritadenine, L-eritadenine, L-threoeritadenine, and 9-(S)-(2,3-dihydroxypropyl)adenine [(S)DHPA] function as inhibitors/inactivators of purified S-adenosylhomocysteine (AdoHcy) hydrolase, but these compounds did not induce reduction of enzyme-bound NAD+. D-Eritadenine, L-eritadenine,...

journal_title：Molecular pharmacology

authors： Schanche JS,Schanche T,Ueland PM,Holý A,Votruba I

更新日期：1984-11-01 00:00:00

abstract：:The vitamin D receptor (VDR) mediates vitamin D signaling in numerous physiological and pharmacological processes, including bone and calcium metabolism, cellular growth and differentiation, immunity, and cardiovascular function. Although transcriptional regulation by VDR has been investigated intensively, an understa...

journal_title：Molecular pharmacology

authors： Choi M,Yamada S,Makishima M

更新日期：2011-12-01 00:00:00

abstract：:The midbrain periaqueductal gray (PAG) is involved in organizing behavioral responses to threat, stress, and pain. These PAG functions are modulated by cholinergic agents. In the present study, we examined the cholinergic modulation of synaptic transmission in the PAG using whole-cell voltage-clamp recordings from rat...

journal_title：Molecular pharmacology

authors： Lau BK,Vaughan CW

更新日期：2008-11-01 00:00:00

abstract：:The precise mechanism by which the cellular uptake of the endocannabinoid anandamide (AEA) occurs has been the source of much debate. In the current study, we show that neuronal differentiated CAD (dCAD) cells accumulate anandamide by a process that is inhibited in a dose-dependent manner by N-(4-hydroxyphenyl)arachid...

journal_title：Molecular pharmacology

authors： McFarland MJ,Bardell TK,Yates ML,Placzek EA,Barker EL

更新日期：2008-07-01 00:00:00

abstract：:Rat and human lung microsomal cytochrome P-450 (P-450) enzymes have been characterized with regard to their catalytic activities towards several xenobiotic chemicals, including procarcinogens, in different microsomal preparations. Rat lung microsomal P-450s were more active than the human P-450s in catalyzing most of ...

journal_title：Molecular pharmacology

authors： Shimada T,Yun CH,Yamazaki H,Gautier JC,Beaune PH,Guengerich FP

更新日期：1992-05-01 00:00:00

abstract：:Cultured murine hepatoma 1c1c7 cells were treated with either the actin filament-disrupting drug cytochalasin D or the microtubule inhibitors colchicine and nocadazole (NOC) to assess the role of the cytoskeleton in the process of cytochrome P450 Cyp1a-1 induction. Indirect fluorescence analyses demonstrated that micr...

journal_title：Molecular pharmacology

authors： Schöller A,Hong NJ,Bischer P,Reiners JJ Jr

更新日期：1994-05-01 00:00:00

abstract：:Several structural subclasses of ligands bind to the benzodiazepine (BZD) binding site of the GABA(A) receptor. Previous studies from this laboratory have suggested that imidazobenzodiazepines (i-BZDs, e.g., Ro 15-1788) require domains in the BZD binding site for high-affinity binding that are distinct from the requir...

journal_title：Molecular pharmacology

authors： Kucken AM,Teissére JA,Seffinga-Clark J,Wagner DA,Czajkowski C

更新日期：2003-02-01 00:00:00

abstract：:alpha4beta2 nicotinic acetylcholine receptors (nAChRs) are recognized as the principal nicotine binding site in brain. Recombinant alpha4beta2 nAChR demonstrate biphasic concentration-response relationships with low- and high-EC50 components. This study shows that untranslated regions (UTR) can influence expression of...

journal_title：Molecular pharmacology

authors： Briggs CA,Gubbins EJ,Marks MJ,Putman CB,Thimmapaya R,Meyer MD,Surowy CS

更新日期：2006-07-01 00:00:00

abstract：:The initial event upon binding of insulin-like growth factor 1 to the insulin-like growth factor type-I receptor (IGF-1R) is auto-phosphorylation of tyrosine residues within the activation loop of the kinase domain followed by phosphorylation of other receptor tyrosine residues and the subsequent activation of the int...

journal_title：Molecular pharmacology

authors： Vasilcanu R,Vasilcanu D,Sehat B,Yin S,Girnita A,Axelson M,Girnita L

更新日期：2008-03-01 00:00:00

abstract：:Previous studies have shown that neural stimulation of brown adipose tissue (BAT) reorganizes the expression and activity of signaling proteins in the beta-adrenergic adenylyl cyclase pathway. Cold stress increases neural stimulation of BAT and increases alpha1-adrenergic receptor number; however, the alpha1 receptor ...

journal_title：Molecular pharmacology

authors： Granneman JG,Zhai Y,Lahners KN

更新日期：1997-04-01 00:00:00

abstract：:We reported previously that protein associated with Myc (PAM) interacts with the C2 domain of type V adenylyl cyclase (ACV-C2) and that purified PAM is a potent inhibitor of Galphas-stimulated ACV activity (J Biol Chem 276:47583-47589, 2001). The present study was conducted to identify the region in PAM that inhibits ...

journal_title：Molecular pharmacology

authors： Gao X,Patel TB

更新日期：2005-01-01 00:00:00

abstract：:The phosphatidylcholine-using phospholipase D (PLD) isoform PLD2 is widely expressed in mammalian cells and is activated in response to a variety of promitogenic agonists. In this study, active and inactive hemagglutinin-tagged human PLD2 (HA-PLD2) constructs were stably expressed in an EL4 cell line lacking detectabl...

journal_title：Molecular pharmacology

authors： Knoepp SM,Chahal MS,Xie Y,Zhang Z,Brauner DJ,Hallman MA,Robinson SA,Han S,Imai M,Tomlinson S,Meier KE

更新日期：2008-09-01 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：: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：:Nicotine can enhance working memory and attention. Activation of both alpha7 and beta2(*) nicotinic acetylcholine receptors (nAChRs) in the prefrontal cortex (PFC) has been implicated in these processes. The ability of presynaptic nAChRs to modulate neurotransmitter release, notably glutamate release, is postulated to...

journal_title：Molecular pharmacology

authors： Dickinson JA,Kew JN,Wonnacott S

更新日期：2008-08-01 00:00:00

abstract：:1-Deoxynojirimycin (DNM) is a saccharide decoy that inhibits cellular alpha-glucosidase I-II activity. Treatment by DNM of human immunodeficiency virus (HIV)-infected lymphocyte cultures inhibits virus spread. The functional properties of the membrane-associated Env glycoprotein (Env) modified in the presence of DNM r...

journal_title：Molecular pharmacology

authors： Papandréou MJ,Barbouche R,Guieu R,Kieny MP,Fenouillet E

更新日期：2002-01-01 00:00:00