D1-like dopaminergic activation of phosphoinositide hydrolysis is independent of D1A dopamine receptors: evidence from D1A knockout mice.

abstract：:The liver is the only solid organ that can respond to major tissue loss or damage by regeneration to restore liver biomass. The aryl hydrocarbon receptor (AhR) agonist 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) can disrupt the regenerative process, as evidenced by suppression of DNA synthesis in rat primary hepatocyte...

journal_title：Molecular pharmacology

authors： Huang G,Elferink CJ

更新日期：2005-01-01 00:00:00

abstract：:Direct gastric mucosal cell damage mediated by nonsteroidal anti-inflammatory drugs (NSAIDs) is involved in the formation of NSAID-induced gastric lesions. We recently suggested that this direct cytotoxicity of NSAIDs is caused by their membrane-permeabilization activity. Geranylgeranylacetone (GGA), a clinically used...

journal_title：Molecular pharmacology

authors： Ushijima H,Tanaka K,Takeda M,Katsu T,Mima S,Mizushima T

更新日期：2005-10-01 00:00:00

abstract：:The induction of human inducible nitric-oxide synthase (iNOS) expression depends (among other factors) on activation of the signal transducer and activator of transcription 1 (STAT1) pathway. Therefore, the STAT1 pathway may be an appropriate target for the development of inhibitors of iNOS expression. HeLa S3 cells t...

journal_title：Molecular pharmacology

authors： Yao Y,Hausding M,Erkel G,Anke T,Förstermann U,Kleinert H

更新日期：2003-02-01 00:00:00

abstract：:Thyrotropin-releasing hormone (TRH) receptors were solubilized from a rat pituitary tumor cell line, GH4C1, with digitonin. Convenient assays were developed based on the ability of hydroxylapatite and polyethyleneimine-soaked glass fiber filters to adsorb the solubilized [3H]methyl-TRH-receptor complex but not free [3...

journal_title：Molecular pharmacology

authors： Phillips WJ,Hinkle PM

更新日期：1989-04-01 00:00:00

abstract：:Peroxisome proliferator-activated receptor δ (PPARδ) has been implicated in vascular pathophysiology. However, its functions in atherogenic changes of the vascular wall have not been fully elucidated. PPARδ activated by GW501516 (2-[2-methyl-4-[[4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl]methylsulfanyl]ph...

journal_title：Molecular pharmacology

authors： Hwang JS,Ham SA,Yoo T,Lee WJ,Paek KS,Lee CH,Seo HG

更新日期：2016-11-01 00:00:00

abstract：:The clinical abuse of methamphetamine (METH) is a major concern because it can cause long-lasting neurodegenerative effects in humans. Current concepts of the molecular mechanisms underlying these complications have centered on the formation of reactive oxygen species. Herein, we provide cDNA microarray evidence that ...

journal_title：Molecular pharmacology

authors： Jayanthi S,McCoy MT,Ladenheim B,Cadet JL

更新日期：2002-05-01 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：: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：:The 2,3,7,8-tetrachlorodibenzo-p-dioxin-transformed aryl hydrocarbon receptor (AHR) complex binds to xenobiotic-responsive element (XRE) sequences in the 5' flanking region of the CYP1A1 gene, resulting in initiation of transcription. Both components of the transformed AHR complex [the ligand-binding AHR monomer and t...

journal_title：Molecular pharmacology

authors： Bacsi SG,Reisz-Porszasz S,Hankinson O

更新日期：1995-03-01 00:00:00

abstract：:The availability of high-affinity agonists for peroxisome proliferator-activated receptor-beta/delta (PPARbeta/delta) has led to significant advances in our understanding of the functional role of PPARbeta/delta. In this study, a new PPARbeta/delta antagonist, 4-chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethy...

journal_title：Molecular pharmacology

authors： Palkar PS,Borland MG,Naruhn S,Ferry CH,Lee C,Sk UH,Sharma AK,Amin S,Murray IA,Anderson CR,Perdew GH,Gonzalez FJ,Müller R,Peters JM

更新日期：2010-09-01 00:00:00

abstract：:G protein-coupled receptors (GPCRs) and receptor tyrosine kinases (RTKs) act in concert to regulate cell growth, proliferation, survival, and migration. Metabotropic GABAB receptor (GABABR) is the GPCR for the main inhibitory neurotransmitter GABA in the central nervous system. Increased expression of GABABR has been ...

journal_title：Molecular pharmacology

authors： Xia S,He C,Zhu Y,Wang S,Li H,Zhang Z,Jiang X,Liu J

更新日期：2017-09-01 00:00:00

abstract：:Recombinant interferon-alpha (IFN) enhances the cytotoxic effects of the fluorinated pyrimidine, 5-fluorouracil (5FU), against two human colon cancer cell lines. The aspartate transcarbamylase (ATCase) inhibitor, N-(phosphonacetyl)-L-aspartate (PALA), was studied in combination with 5FU/IFN to determine whether furthe...

journal_title：Molecular pharmacology

authors： Wadler S,Mao X,Bajaj R,Hallam S,Schwartz EL

更新日期：1993-11-01 00:00:00

abstract：:Propofol, etomidate, and barbiturate anesthetics are allosteric coagonists at pentameric α1β3γ2 GABAA receptors, modulating channel activation via four biochemically established intersubunit transmembrane pockets. Etomidate selectively occupies the two β+/α- pockets, the barbiturate photolabel R-5-allyl-1-methyl-5-(m-...

journal_title：Molecular pharmacology

authors： Szabo A,Nourmahnad A,Halpin E,Forman SA

更新日期：2019-04-01 00:00:00

abstract：:The growth of Plasmodium falciparum, a human malaria parasite, is sensitive to inhibition by chelators of several types. The alkylthiocarbamates and 8-hydroxyquinoline at pharmacologic doses selectively inhibit glycolysis within 6 hr in parasitized erythrocytes. The mechanism attributed to these agents is through the ...

journal_title：Molecular pharmacology

authors： Scheibel LW,Stanton GG

更新日期：1986-10-01 00:00:00

abstract：:Adult guinea pig hippocampal membranes contain two 5-hydroxytryptamine (5-HT) receptors positively coupled with an adenylate cyclase. One is a typical 5-HT1A receptor and the second is a nonclassical 5-HT receptor that we previously proposed to call 5-HT4. Here, we show that 4-amino-5-chlor-2-methoxy-benzamide derivat...

journal_title：Molecular pharmacology

authors： Bockaert J,Sebben M,Dumuis A

更新日期：1990-03-01 00:00:00

abstract：:The activities of phosphorylase kinase and myosin light-chain kinase are regulated by Ca2+ binding to calmodulin. However, differences in the activation properties of the purified enzymes are apparent, since calmodulin binds to phosphorylase kinase in the absence of Ca2+ whereas prior formation of a Ca2+ . calmodulin ...

journal_title：Molecular pharmacology

authors： Silver PJ,Stull JT

更新日期：1983-05-01 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：:Amitriptyline is a classic tricyclic antidepressant (TCA) and has been used to treat the depression and anxiety of patients with cancer, but its relevance to cancer cell apoptosis is not known. In the present study, we demonstrated that amitriptyline inhibited cyclin D2 transactivation and displayed potential antimyel...

journal_title：Molecular pharmacology

authors： Mao X,Hou T,Cao B,Wang W,Li Z,Chen S,Fei M,Hurren R,Gronda M,Wu D,Trudel S,Schimmer AD

更新日期：2011-04-01 00:00:00

abstract：:This article describes the expected phenotypic behavior of all types of ligands in constitutively active receptor systems and, in particular, the molecular mechanisms of inverse agonism. The possible physiological relevance of inverse agonism also is discussed. Competitive antagonists with the molecular property of ne...

journal_title：Molecular pharmacology

authors： Kenakin T

更新日期：2004-01-01 00:00:00

abstract：:Previous studies have demonstrated that the quinone group may play an important role in modulating the alkylating activity of quinone alkylating agents. Introduction of a quinone moiety markedly increased the alkylating activity and cytotoxic activity of the model quinone alkylating agents benzoquinone mustard and ben...

journal_title：Molecular pharmacology

authors： Begleiter A,Leith MK,Pan SS

更新日期：1991-09-01 00:00:00

abstract：:Upon sustained insult, kinins are released and many kinin responses, such as inflammatory pain, adapt from a B2 receptor (B2R) type in the acute phase to a B1 receptor (B1R) type in the chronic phase. In this study, we show that kinins modulate receptor endocytosis to rapidly decrease B2R and increase B1R on the cell ...

journal_title：Molecular pharmacology

authors： Enquist J,Skröder C,Whistler JL,Leeb-Lundberg LM

更新日期：2007-02-01 00:00:00

abstract：:Atropine, the classic muscarinic receptor antagonist, inhibits ion currents mediated by neuronal nicotinic acetylcholine receptors expressed in Xenopus laevis oocytes. At the holding potential of -80 mV, 1 microM atropine inhibits 1 mM acetylcholine-induced inward currents mediated by rat alpha2beta2, alpha2beta4, alp...

journal_title：Molecular pharmacology

authors： Zwart R,Vijverberg HP

更新日期：1997-11-01 00:00:00

abstract：:Retina from 1-day-old chicks is a valuable tissue model for studying neuronal nicotinic receptors because it expresses a large number of the developmentally regulated high affinity [(3)H]epibatidine labeled nicotinic receptors. Most of these receptors contain the beta4 subunit associated with different alpha subunits....

journal_title：Molecular pharmacology

authors： Barabino B,Vailati S,Moretti M,McIntosh JM,Longhi R,Clementi F,Gotti C

更新日期：2001-06-01 00:00:00

abstract：:Styrylquinoline derivatives (SQ) efficiently inhibit the 3'-processing activity of integrase (IN) with IC50 values of between 0.5 and 5 microM. We studied the mechanism of action of these compounds in vitro. First, we used steady-state fluorescence anisotropy to assay the effects of the SQ derivatives on the formation...

journal_title：Molecular pharmacology

authors： Deprez E,Barbe S,Kolaski M,Leh H,Zouhiri F,Auclair C,Brochon JC,Le Bret M,Mouscadet JF

更新日期：2004-01-01 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：: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 effects of ethanol on a number of electrophysiological parameters were examined in 10 different voltage-gated potassium channels expressed in Xenopus oocytes. None of the channels examined was highly sensitive to ethanol, but there was significant variability among the channels tested at concentrations of ethanol ...

journal_title：Molecular pharmacology

authors： Anantharam V,Bayley H,Wilson A,Treistman SN

更新日期：1992-09-01 00:00:00

abstract：:A recently isolated monoclonal antibody was found to be a potent and powerful inhibitor of the catalytic activity of rabbit brain acetylcholinesterase (AChE; acetylcholine acetylhydrolase, EC 3.1.1.7), with an IC50 of about 1 nM and a maximal inhibition of at least 90%. The antibody increased the optimal concentration...

journal_title：Molecular pharmacology

authors： Brimijoin S,Mintz KP,Prendergast FG

更新日期：1985-12-01 00:00:00

abstract：:Most anticancer drugs have their origin in traditional medicinal plants. We describe here a flavone, 5,3'-dihydroxy-3,6,7,8,4'-pentamethoxyflavone (PMF), from the leaves of the Thai plant Gardenia obtusifolia, that has anti-inflammatory and anticancer potential. Because the nuclear factor-κB (NF-κB) pathway is linked ...

journal_title：Molecular pharmacology

authors： Phromnoi K,Reuter S,Sung B,Prasad S,Kannappan R,Yadav VR,Chanmahasathien W,Limtrakul P,Aggarwal BB

更新日期：2011-02-01 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