Ketoconazole and miconazole are antagonists of the human glucocorticoid receptor: consequences on the expression and function of the constitutive androstane receptor and the pregnane X receptor.

abstract：:Vasopressin receptor subtype(s) responsible for stimulation of insulin release from pancreatic beta cells were investigated by using subtype-selective antagonists and mice that were genetically lacking either V1a or V1b receptors. Arginine vasopressin (AVP) increased insulin release from isolated mouse islet cells in ...

journal_title：Molecular pharmacology

authors： Oshikawa S,Tanoue A,Koshimizu TA,Kitagawa Y,Tsujimoto G

更新日期：2004-03-01 00:00:00

abstract：:In the present study we have investigated the capacity of various compounds sterically related to indolo[3,2-b]carbazole to inhibit specific 2,3,7,8-tetrachloro[1,6-3H]dibenzo-p-dioxin binding in rat liver cytosol, as analyzed by electrofocusing in polyacrylamide gels. When the two nitrogen atoms of indolo[3,2-b]carba...

journal_title：Molecular pharmacology

authors： Gillner M,Bergman J,Cambillau C,Alexandersson M,Fernström B,Gustafsson JA

更新日期：1993-08-01 00:00:00

abstract：:GABAA receptors are predominantly composed of alphabetagamma and alphabetadelta isoforms in the brain. It has been proposed that alphabetagamma receptors mediate phasic inhibition, whereas alphabetadelta receptors mediate tonic inhibition. Propofol (2,6-di-isopropylphenol), a widely used anesthetic drug, exerts its ef...

journal_title：Molecular pharmacology

authors： Feng HJ,Macdonald RL

更新日期：2004-12-01 00:00:00

abstract：:Activation of synthesis-modulating dopamine autoreceptors by dopamine or its agonists has been shown to inhibit dopamine synthesis in the rat striatum. However, systemic administration of the direct-acting dopamine agonist apomorphine failed to inhibit dopamine synthesis in striata from rats that had received local un...

journal_title：Molecular pharmacology

authors： Bean AJ,Shepard PD,Bunney BS,Nestler EJ,Roth RH

更新日期：1988-12-01 00:00:00

abstract：:Although G protein-coupled receptors are often categorized in terms of their primary coupling to a given type of Gα protein subunit, it is now well established that many show promiscuous coupling and activate multiple signaling pathways. Furthermore, some agonists selectively activate signaling pathways by promoting i...

journal_title：Molecular pharmacology

authors： Evans BA,Broxton N,Merlin J,Sato M,Hutchinson DS,Christopoulos A,Summers RJ

更新日期：2011-02-01 00:00:00

abstract：:The anti-arrhythmic quinidine has been reported to be a competitive inhibitor of the catalytic activities of human liver P-450DB, including sparteine delta 2-oxidation and bufuralol 1'-hydroxylation, and we confirmed the observation that submicromolar concentrations are strongly inhibitory. Human liver microsomes oxid...

journal_title：Molecular pharmacology

authors： Guengerich FP,Müller-Enoch D,Blair IA

更新日期：1986-09-01 00:00:00

abstract：:Autophagy is a response of cancer cells to various anticancer therapies. It is designated as programmed cell death type II and characterized by the formation of autophagic vacuoles in the cytoplasm. The Akt/mammalian target of rapamycin (mTOR)/p70 ribosomal protein S6 kinase (p70S6K) and the extracellular signal-regul...

journal_title：Molecular pharmacology

authors： Aoki H,Takada Y,Kondo S,Sawaya R,Aggarwal BB,Kondo Y

更新日期：2007-07-01 00:00:00

abstract：:Interleukin 6 (IL-6), which is elevated in patients with congestive heart failure and acts as both a chronic marker of inflammation and an acute-phase reactant, is associated with myocardial damage. Circulating levels of arginine vasopressin (AVP) are elevated during cardiac stress and could be a factor for cardiac in...

journal_title：Molecular pharmacology

authors： Xu F,Sun S,Wang X,Ni E,Zhao L,Zhu W

更新日期：2017-09-01 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：: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：:The present study characterizes the methanethiosulfonate (MTS) inhibition profiles of 26 consecutive cysteine-substituted mutants comprising transmembrane (TM) helix 6 of the human apical Na(+)-dependent bile acid transporter (SLC10A2). TM6 is linked exofacially to TM7 via extracellular loop 3. TM7 was identified prev...

journal_title：Molecular pharmacology

authors： Hussainzada N,Khandewal A,Swaan PW

更新日期：2008-02-01 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：:Ca-dependent, K-stimulated 86Rb efflux, a measure of Ca-activated K conductance in rat brain synaptosomes, was blocked by phenothiazines and haloperidol. Micromolar concentrations of the phenothiazines, fluphenazine and trifluoperazine, and haloperidol, a non-phenothiazine antipsychotic and calmodulin antagonist, sele...

journal_title：Molecular pharmacology

authors： Benishin CG,Krueger BK,Blaustein MP

更新日期：1988-02-01 00:00:00

abstract：:Previous studies showed that lapatinib and obatoclax interact in a greater-than-additive fashion to cause cell death and do so through a toxic form of autophagy. The present studies sought to extend our analyses. Lapatinib and obatoclax killed multiple tumor cell types, and cells lacking phosphatase and tensin homolog...

journal_title：Molecular pharmacology

authors： Cruickshanks N,Tang Y,Booth L,Hamed H,Grant S,Dent P

更新日期：2012-12-01 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：:Histone deacetylase inhibitors (HDACis) are currently in trial or are in clinical use for the treatment of a number of tumor types. The clinical efficacy of HDACis can be partly attributed to the modulation of the cell cycle by the HDACis. Here, we have examined the effects of N-(2-aminophenyl)-4-((4-pyridin-3-ylpyrim...

journal_title：Molecular pharmacology

authors： Chia K,Beamish H,Jafferi K,Gabrielli B

更新日期：2010-09-01 00:00:00

abstract：:Nitric oxide (NO) binds with high affinity to the heme of soluble guanylyl cyclase (sGC), resulting in accumulation of the second messenger cGMP in many biological systems. 1H-[1,2,4]Oxadiazolo[4,3-a]quinoxalin-1-one (ODQ) was recently described as potent and selective inhibitor of sGC, providing an invaluable tool wi...

journal_title：Molecular pharmacology

authors： Schrammel A,Behrends S,Schmidt K,Koesling D,Mayer B

更新日期：1996-07-01 00:00:00

abstract：:The retinoid (visual) cycle consists of a series of biochemical reactions needed to regenerate the visual chromophore 11-cis-retinal and sustain vision. Genetic or environmental factors affecting chromophore production can lead to blindness. Using animal models that mimic human retinal diseases, we previously demonstr...

journal_title：Molecular pharmacology

authors： Gao S,Kahremany S,Zhang J,Jastrzebska B,Querubin J,Petersen-Jones SM,Palczewski K

更新日期：2018-05-01 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：: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 total CYP3A5 mRNA level is significantly greater in carriers of the CYP3A5*1 allele than in CYP3A5*3 homozygotes. Most of the CYP3A5*3 mRNA includes an intronic sequence (exon 3B) containing premature termination codons (PTCs) between exons 3 and 4. Two models were used to investigate the degradation of CYP3A5 mRN...

journal_title：Molecular pharmacology

authors： Busi F,Cresteil T

更新日期：2005-09-01 00:00:00

abstract：:Potassium channels play fundamental roles in physiology. Chemically diverse drugs bind in the pore region of K+ channels. Here, we homology-modeled voltage- and Ca2+-gated K+ channel BK and voltage-gated Kv1.3 using the X-ray structures of MthK and Kv1.2, respectively, and simulated the binding of d-tubocurarine in th...

journal_title：Molecular pharmacology

authors： Rossokhin A,Teodorescu G,Grissmer S,Zhorov BS

更新日期：2006-04-01 00:00:00

abstract：:Many Gi-coupled receptors are known to interact with the pertussis toxin (PTX)-insensitive Gz protein. Given that the alpha subunits of Gi and Gz share only 60% identity in their amino acid sequences, their receptor-interacting domains must be highly similar. By swapping the carboxyl termini of alpha i2 and alpha z wi...

journal_title：Molecular pharmacology

authors： Tsu RC,Ho MK,Yung LY,Joshi S,Wong YH

更新日期：1997-07-01 00:00:00

abstract：:K-252b, a member of the staurosporine family of protein kinase inhibitors, selectively potentiates the activation of the nerve growth factor receptor, TrkA, by a nonpreferred ligand, neurotrophin-3 (NT-3), in a variety of cell types. At higher (micromolar) concentrations of K-252b, an inhibitory effect occurs because ...

journal_title：Molecular pharmacology

authors： Pollack S,Young L,Bilsland J,Wilkie N,Ellis S,Hefti F,Broughton H,Harper S

更新日期：1999-07-01 00:00:00

abstract：:The effect of halothane on synthesis of retained and secreted proteins was investigated using isolated perfused rat livers. Anesthetic exposure rapidly inhibited synthesis of total liver proteins in a dose-dependent manner by a mechanism which appeared to involve reduced rates of both peptide chain initiation and elon...

journal_title：Molecular pharmacology

authors： Flaim KE,Jefferson LS,McGwire JB,Rannels DE

更新日期：1983-09-01 00:00:00

abstract：:Melanocortins (MCs) have various physiological actions on the brain. The recent cloning of neural MC receptors opened new avenues to study the effects of these neuropeptides on the nervous system. Here we investigated the structure-activity relationships (SARs) of peptides derived from adrenocorticotropic hormone (ACT...

journal_title：Molecular pharmacology

authors： Adan RA,Cone RD,Burbach JP,Gispen WH

更新日期：1994-12-01 00:00:00

abstract：:Recently, several classes of compounds have been shown to be potent, selective, and specific inhibitors of human immunodeficiency virus type 1 replication in vitro. These include the tetrahydroimidazo[4,5,1-jk][1,4]-benzodiazepin-2(1H)-one and -thione (TIBO) and the 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (H...

journal_title：Molecular pharmacology

authors： Debyser Z,Pauwels R,Baba M,Desmyter J,De Clercq E

更新日期：1992-05-01 00:00:00

abstract：:Chick brain mRNA was isolated and injected into Xenopus oocytes. This led to the expression of gamma-aminobutyrate (GABA) channels easily accessible for current measurements using the voltage clamp technique. The effect of the anthelmintic natural product avermectin B1a on the GABA current was studied quantitatively. ...

journal_title：Molecular pharmacology

authors： Sigel E,Baur R

更新日期：1987-12-01 00:00:00

abstract：:Human and bovine dopamine transporters (DAT) demonstrate discrete functional differences in dopamine (DA), 1-methyl-4-phenylpyridium (MPP(+)) transport, and cocaine analog binding. In a previous study, the functional analyses on the chimeras of human and bovine DAT have revealed that the region from residues 133 throu...

journal_title：Molecular pharmacology

authors： Lee SH,Chang MY,Lee KH,Park BS,Lee YS,Chin HR,Lee YS

更新日期：2000-05-01 00:00:00

abstract：:Binding by 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) to the Ah receptor leads to transcriptional activation of several genes and a toxicity syndrome that includes tumor promotion, wasting, hormonal and immune system dysfunction, and death. Recent findings indicate that TCDD may also affect cardiac function. Here, we ...

journal_title：Molecular pharmacology

authors： Canga L,Paroli L,Blanck TJ,Silver RB,Rifkind AB

更新日期：1993-12-01 00:00:00