Caveolins as Regulators of Stress Adaptation.

abstract：:Endothelin-1 (ET) and ATP mobilize Ca2+ in rat C6 glioma cells by stimulating phosphoinositide turnover. Both agents also inhibit adenylyl cyclase (AC) activity in C6 glioma cells. The goal of this study was to characterize the molecular mechanisms responsible for the inhibition of AC activity. The administration of e...

journal_title：Molecular pharmacology

authors： Lin WW,Chuang DM

更新日期：1993-07-01 00:00:00

abstract：:Nuclear receptors play important roles in the maintenance of the endocrine system, regulation of organ differentiation, and fetal development. Endocrine disruptors exert their adverse effects by disrupting the endocrine system via various mechanisms. To assess the effects of endocrine disruptors on nuclear receptors, ...

journal_title：Molecular pharmacology

authors： Kanayama T,Kobayashi N,Mamiya S,Nakanishi T,Nishikawa J

更新日期：2005-03-01 00:00:00

abstract：:In ND8-47 cells, a neuroblastoma x dorsal root ganglion hybrid cell line, activation of delta-opioid receptors induced an increase in the intracellular free calcium concentration ([Ca2+]i) through dihydropyridine-sensitive calcium channels. This effect was mediated by pertussis toxin-sensitive G proteins. The G protei...

journal_title：Molecular pharmacology

authors： Tang T,Kiang JG,Côté TE,Cox BM

更新日期：1995-08-01 00:00:00

abstract：:Several structurally related series of folate analogs were studied as substrates for mouse liver folylpolyglutamate synthetase (FPGS). A comparison of the kinetics of the interaction of this enzyme with folate analogs that contained the quinazoline ring in place of the pteridine ring with those of the analogous pterid...

journal_title：Molecular pharmacology

authors： Moran RG,Colman PD,Jones TR

更新日期：1989-11-01 00:00:00

abstract：:Opioid analgesics are used extensively in the management of pain. Although the clinically effective opioids bind with high affinity to the mu-opioid receptor, studies have suggested that the delta-opioid agonists might represent more ideal analgesic agents, with fewer side effects. A limitation to opiate effectiveness...

journal_title：Molecular pharmacology

authors： Bot G,Blake AD,Li S,Reisine T

更新日期：1997-08-01 00:00:00

abstract：:The nicotinic acetylcholine receptor can be expressed in Xenopus oocytes by injection of in vitro synthesized RNA for the alpha, beta, gamma, and delta mouse muscle subunits. However, detectable responses can also be obtained by injection of alpha, beta, and delta subunit RNA only. The receptors expressed in this case...

journal_title：Molecular pharmacology

authors： Charnet P,Labarca C,Lester HA

更新日期：1992-04-01 00:00:00

abstract：:GPR139 is an orphan G-protein-coupled receptor expressed in the central nervous system. To identify its physiologic ligand, we measured GPR139 receptor activity from recombinant cells after treatment with amino acids, orphan ligands, serum, and tissue extracts. GPR139 activity was measured using guanosine 5'-O-(3-[(35...

journal_title：Molecular pharmacology

authors： Liu C,Bonaventure P,Lee G,Nepomuceno D,Kuei C,Wu J,Li Q,Joseph V,Sutton SW,Eckert W,Yao X,Yieh L,Dvorak C,Carruthers N,Coate H,Yun S,Dugovic C,Harrington A,Lovenberg TW

更新日期：2015-11-01 00:00:00

abstract：:Mouse embryonic spinal cord neurons in culture exhibit spontaneous calcium oscillations from day in vitro (DIV) 6 through DIV 10. Such spontaneous activity in developing spinal cord contributes to maturation of synapses and development of pattern-generating circuits. Here we demonstrate that these calcium oscillations...

journal_title：Molecular pharmacology

authors： Kelamangalath L,Dravid SM,George J,Aldrich JV,Murray TF

更新日期：2011-06-01 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：:Activation of endothelial nitric-oxide synthase (eNOS) has been shown to occur through various pathways involving increases in the cytosolic Ca(2+) concentration, activation of the phosphatidylinositol-3' kinase/Akt pathway, as well as regulation by other kinases and by protein-protein interactions. We have recently r...

journal_title：Molecular pharmacology

authors： Barsacchi R,Perrotta C,Bulotta S,Moncada S,Borgese N,Clementi E

更新日期：2003-04-01 00:00:00

abstract：:We investigated the mechanisms of MDR1 gene activation by CCAAT/enhancer binding protein beta (C/EBPbeta, or nuclear factor for interleukin 6) in human cancer cells. Transfection of the breast cancer cell line MCF-7 and its doxorubicin-selected variant MCF-7/ADR by either C/EBPbeta or C/EBPbeta-LIP (a dominant-negativ...

journal_title：Molecular pharmacology

authors： Chen KG,Sale S,Tan T,Ermoian RP,Sikic BI

更新日期：2004-04-01 00:00:00

abstract：:The therapeutic potential of antitumor drugs is seriously limited by the manifestation of cellular drug resistance. We used the budding yeast Saccharomyces cerevisiae as a model system to identify novel mechanisms of resistance to one of the most active anticancer agents, cisplatin. We pinpointed NPR2 (nitrogen permea...

journal_title：Molecular pharmacology

authors： Schenk PW,Brok M,Boersma AW,Brandsma JA,Den Dulk H,Burger H,Stoter G,Brouwer J,Nooter K

更新日期：2003-08-01 00:00:00

abstract：:The sulfoconjugation of tyrosyl residues is a widespread post-translational modification of biologically active proteins and peptides. The rat liver Golgi enzyme tyrosylprotein sulfotransferase has previously been shown to catalyze the transfer of a sulfate moiety from 5'-phosphoadenosine-3'-phosphosulfate to the synt...

journal_title：Molecular pharmacology

authors： Rens-Domiano S,Hortin GL,Roth JA

更新日期：1989-10-01 00:00:00

abstract：:Melanoma differentiation associated gene-7 (mda-7)/interleukin-24 (IL-24), a member of the IL-10 cytokine gene family, preferentially induces cell death in neoplastic epithelial cells types while sparing their normal counterparts. The effects of mda-7/IL-24 in acute myeloid leukemia (AML) cells have not been extensive...

journal_title：Molecular pharmacology

authors： Rahmani M,Mayo M,Dash R,Sokhi UK,Dmitriev IP,Sarkar D,Dent P,Curiel DT,Fisher PB,Grant S

更新日期：2010-12-01 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：:Small-molecule restoration of wild-type structure and function to mutant p53 (so-called mutant reactivation) is a highly sought-after goal in cancer drug development. We previously discovered that small-molecule zinc chelators called zinc metallochaperones (ZMCs) reactivate mutant p53 by restoring zinc binding to zinc...

journal_title：Molecular pharmacology

authors： Yu X,Blanden A,Tsang AT,Zaman S,Liu Y,Gilleran J,Bencivenga AF,Kimball SD,Loh SN,Carpizo DR

更新日期：2017-06-01 00:00:00

abstract：:ATP-sensitive K(+) channels are closed by the hypoglycemic sulfonylureas like glibenclamide (GBC) and activated by a class of vasorelaxant compounds, the K(+) channel openers. These channels are octamers of Kir6.x and sulfonylurea receptor (SUR) subunits with 4:4 stoichiometry. The properties of the opener-sensitive K...

journal_title：Molecular pharmacology

authors： Russ U,Hambrock A,Artunc F,Löffler-Walz C,Horio Y,Kurachi Y,Quast U

更新日期：1999-11-01 00:00:00

abstract：:(+/-)-6' beta-Fluoroaristeromycin (F-C-Ado) is a potent and competitive inhibitor of purified S-adenosylhomocysteine (AdoHcy) hydrolase isolated from murine L929 cells (Ki = 3.1 nM). It also inhibits vaccinia virus and vesicular stomatitis virus replication in L929 cells, at a 90% inhibitory dose (ID90) of 3.5 and 13 ...

journal_title：Molecular pharmacology

authors： Cools M,Balzarini J,De Clercq E

更新日期：1991-06-01 00:00:00

abstract：:The functional significance of the conserved amino acids within transmembrane regions II and VII of the human 5-hydroxytryptamine (5-HT)1A receptor was analyzed by oligonucleotide-directed mutagenesis followed by transient expression of the mutated receptor genes in COS-1 cells. The substitution of a conserved asparag...

journal_title：Molecular pharmacology

authors： Chanda PK,Minchin MC,Davis AR,Greenberg L,Reilly Y,McGregor WH,Bhat R,Lubeck MD,Mizutani S,Hung PP

更新日期：1993-04-01 00:00:00

abstract：:[3H]Dihydroalprenolol ([3H]DHA) has been used extensively in receptor binding studies to measure beta-adrenergic receptors in the central nervous system. Usually, nonspecific binding has been defined by high concentrations of the beta-adrenergic receptor agonist isoproterenol or antagonists such as alprenolol or propr...

journal_title：Molecular pharmacology

authors： Riva MA,Creese I

更新日期：1989-07-01 00:00:00

abstract：:Pertussis toxin (PTX) ADP-ribosylates alpha subunits of GTP-binding proteins (G proteins) when they are in association with beta gamma dimers, and free alpha subunits are thought not to be substrates under standard assay conditions. We now report the rather unexpected discovery that synthetic peptides encompassing the...

journal_title：Molecular pharmacology

authors： Graf R,Codina J,Birnbaumer L

更新日期：1992-11-01 00:00:00

abstract：:[3H]P1075 binding to membrane preparations of rabbit skeletal muscle were observed in the presence of nucleotide triphosphates or diphosphates but not AMP, cAMP, adenosine, tripolyphosphate, or pyrophosphate. Nonhydrolyzable or poorly hydrolyzable ATP analogs inhibited MgATP-supported binding. The EC50 value for MgATP...

journal_title：Molecular pharmacology

authors： Dickinson KE,Bryson CC,Cohen RB,Rogers L,Green DW,Atwal KS

更新日期：1997-09-01 00:00:00

abstract：:Classical chemoattractant receptors are of fundamental importance to immune responses. The two major roles of such receptors are the modulation of chemotaxis and the generation of reactive oxygen species. The formyl peptide receptor-like 1 (FPRL1) can be stimulated by two different ligands, Trp-Lys-Tyr-Met-Val-Met-CON...

journal_title：Molecular pharmacology

authors： Bae YS,Park JC,He R,Ye RD,Kwak JY,Suh PG,Ho Ryu S

更新日期：2003-09-01 00:00:00

abstract：:We studied the mechanism by which the peptide omega-grammotoxin-SIA inhibits voltage-dependent calcium channels. Grammotoxin at concentrations of > 50 nM completely inhibited inward current carried by 2 mM barium through P-type channels in rat cerebellar Purkinje neurons when current was elicited by depolarizations up...

journal_title：Molecular pharmacology

authors： McDonough SI,Lampe RA,Keith RA,Bean BP

更新日期：1997-12-01 00:00:00

abstract：:Undesired block of human ERG1 potassium channels is the basis for cardiac side effects of many different types of drugs. Therefore, it is important to know exactly why some drugs particularly bind to these channels with high affinity. Upon expression in mammalian cells and Xenopus laevis oocytes, we investigated the i...

journal_title：Molecular pharmacology

authors： Gessner G,Zacharias M,Bechstedt S,Schönherr R,Heinemann SH

更新日期：2004-05-01 00:00:00

abstract：:To determine the role of C-Rel in nitric-oxide synthase-2 (NOS-2) transcriptional activation, we evaluated the effect of lipopolysaccharide and interferon-gamma (LPS/IFNgamma) on C-Rel DNA binding in RAW 264.7. LPS/IFNgamma-stimulated C-Rel binding peaked at 4 to 8 h and declined at 24 h. Transfection of cells with a ...

journal_title：Molecular pharmacology

authors： Cieslik KA,Deng WG,Wu KK

更新日期：2006-12-01 00:00:00

abstract：:Ryanodine receptors (RyRs) are intracellular membrane channels playing key roles in many Ca(2+) signaling pathways and, as such, are emerging novel therapeutic and insecticidal targets. RyRs are so named because they bind the plant alkaloid ryanodine with high affinity and although it is established that ryanodine pro...

journal_title：Molecular pharmacology

authors： Mukherjee S,Thomas NL,Williams AJ

更新日期：2014-09-01 00:00:00

abstract：:Westernization of dietary habits increases lipid intake and is responsible for increased numbers of patients with atherosclerotic diseases. Niemann-Pick C1-Like 1 (NPC1L1)-a cholesterol importer-plays a crucial role in dietary cholesterol absorption in the intestine and is closely associated with several lipid-related...

journal_title：Molecular pharmacology

authors： Yamamoto H,Yamanashi Y,Takada T,Mu S,Tanaka Y,Komine T,Suzuki H

更新日期：2019-07-01 00:00:00

abstract：:Autophagy is the process by which cellular material is delivered to lysosomes for degradation and recycling. There are three different types of autophagy, but macroautophagy, which involves the formation of double membrane vesicles that engulf proteins and organelles that fuse with lysosomes, is by far the most studie...

journal_title：Molecular pharmacology

authors： Thorburn A,Thamm DH,Gustafson DL

更新日期：2014-06-01 00:00:00

abstract：:The effect of breast cancer resistance protein (Bcrp/Abcg2) on the disposition of the phytoestrogens daidzein, genistein, and coumestrol was investigated using Bcrp(-/-) mice. Expression of the genes for either mouse Bcrp or human BCRP in MDCK II cells induced apically directed transport of the three phytoestrogens, w...

journal_title：Molecular pharmacology

authors： Enokizono J,Kusuhara H,Sugiyama Y

更新日期：2007-10-01 00:00:00