Preferential coassembly of alpha4 and delta subunits of the gamma-aminobutyric acidA receptor in rat thalamus.

abstract：:The aim of this study was to create and characterize constitutively active mutant (CAM) histamine H(1) receptors (H(1)R) using random mutagenesis methods to further investigate the activation process of the rhodopsin-like family of G protein-coupled receptors (GPCRs). This approach identified position 6.40 in TM 6 as ...

journal_title：Molecular pharmacology

authors： Bakker RA,Jongejan A,Sansuk K,Hacksell U,Timmerman H,Brann MR,Weiner DM,Pardo L,Leurs R

更新日期：2008-01-01 00:00:00

abstract：:Metabotropic glutamate receptor 5 (mGlu5) is a target for the treatment of central nervous system (CNS) disorders, such as schizophrenia and Alzheimer's disease. Furthermore, mGlu5 has been shown to play an important role in hippocampal synaptic plasticity, specifically in long-term depression (LTD) and long-term pote...

journal_title：Molecular pharmacology

authors： Noetzel MJ,Gregory KJ,Vinson PN,Manka JT,Stauffer SR,Lindsley CW,Niswender CM,Xiang Z,Conn PJ

更新日期：2013-04-01 00:00:00

abstract：:Cytokines are thought to cause the depression of cytochrome P-450 (CYP)-associated drug metabolism in humans during inflammation and infection. We have examined the role of five cytokines, i.e., interleukin-1 beta, interleukin-4, interleukin-6, tumor necrosis factor-alpha, and interferon-gamma, on the expression of CY...

journal_title：Molecular pharmacology

authors： Abdel-Razzak Z,Loyer P,Fautrel A,Gautier JC,Corcos L,Turlin B,Beaune P,Guillouzo A

更新日期：1993-10-01 00:00:00

abstract：:Tumors provide an extremely abnormal microenvironment that stimulates neovascularization from surrounding vessels and causes altered gene expression within vascular cells. Up-regulation of vascular endothelial growth factor (VEGF) receptors has allowed selective destruction of tumor vessels by administration of a chim...

journal_title：Molecular pharmacology

authors： Akiyama H,Mohamedali KA,E Silva RL,Kachi S,Shen J,Hatara C,Umeda N,Hackett SF,Aslam S,Krause M,Lai H,Rosenblum MG,Campochiaro PA

更新日期：2005-12-01 00:00:00

abstract：:The compound 4-(5-(4-bromophenyl)-3-(6-methyl-2-oxo-4-phenyl-1,2-dihydroquinolin-3-yl)-4,5-dihydro-1H-pyrazol-1-yl)-4-oxobutanoic acid (DQP-1105) is a representative member of a new class of N-methyl-d-aspartate (NMDA) receptor antagonists. DQP-1105 inhibited GluN2C- and GluN2D-containing receptors with IC(50) values ...

journal_title：Molecular pharmacology

authors： Acker TM,Yuan H,Hansen KB,Vance KM,Ogden KK,Jensen HS,Burger PB,Mullasseril P,Snyder JP,Liotta DC,Traynelis SF

更新日期：2011-11-01 00:00:00

abstract：:Dysfunction of p53 and resistance to cancer drugs can arise through mutually exclusive overexpression of MDM2 or MDM4. Cisplatin-resistant cells, however, can demonstrate increased binding of both MDM2 and MDM4 to p53 but in absence of cellular overexpression. Whether MDM2 inhibitors alone can activate p53 in these re...

journal_title：Molecular pharmacology

authors： Xie X,He G,Siddik ZH

更新日期：2020-04-01 00:00:00

abstract：:Effects of ethanol on the function of Ca(2+)-activated Cl- channels activated by G protein-coupled serotonin (5-hydroxytryptamine, (5-HT)1c) and muscarinic M1 cholinergic receptors were studied in Xenopus oocytes expressing mouse whole-brain mRNA. Ethanol (25-200 mM) inhibited currents evoked by both 5-HT and acetylch...

journal_title：Molecular pharmacology

authors： Sanna E,Dildy-Mayfield JE,Harris RA

更新日期：1994-05-01 00:00:00

abstract：:Matrix metalloproteinases (MMPs) are synthesized in response to diverse stimuli, including cytokines, growth factors, hormones, and oxidative stress. Here we show that the nitric oxide (NO) donor 2-(N,N-diethylamino)-diazenolate-2-oxide (DEA-NO) and NO from murine macrophages transcriptionally regulate MMP-13 expressi...

journal_title：Molecular pharmacology

authors： Zaragoza C,Soria E,López E,Browning D,Balbín M,López-Otín C,Lamas S

更新日期：2002-10-01 00:00:00

abstract：:Arrestins mediate G protein-coupled receptor desensitization, internalization, and signaling. Dopamine D(2) and D(3) receptors have similar structures but distinct characteristics of interaction with arrestins. The goals of this study were to compare arrestin-binding determinants in D(2) and D(3) receptors other than ...

journal_title：Molecular pharmacology

authors： Lan H,Liu Y,Bell MI,Gurevich VV,Neve KA

更新日期：2009-01-01 00:00:00

abstract：:Neurotrophins are a family of secreted proteins that play an important role in the development, differentiation, and survival of neurons. Studies also suggest that aberrant neurotrophin signaling may play a role in processes underlying disease states such as schizophrenia, Alzheimer's disease, and depression. Whereas ...

journal_title：Molecular pharmacology

authors： Lewis MA,Hunihan L,Franco D,Robertson B,Palmer J,Laurent DR,Balasubramanian BN,Li Y,Westphal RS

更新日期：2006-04-01 00:00:00

abstract：:We investigated the interactions of the anticancer drug vinorelbine with drug efflux transporters and cytochrome P450 3A drug-metabolizing enzymes. Vinorelbine was transported by human multidrug-resistance associated protein (MRP) 2, and Mrp2 knockout mice displayed increased vinorelbine plasma exposure after oral adm...

journal_title：Molecular pharmacology

authors： Lagas JS,Damen CW,van Waterschoot RA,Iusuf D,Beijnen JH,Schinkel AH

更新日期：2012-10-01 00:00:00

abstract：:To learn more about the binding conformation of phencyclidine (PCP) and to arrive at analogues of higher affinity, which may serve as noncompetitive N-methyl-D-aspartate receptor antagonists, eight optically pure PCP analogues were designed with the aid of computer. These compounds represent conformationally constrain...

journal_title：Molecular pharmacology

authors： Kozikowski AP,Pang YP

更新日期：1990-03-01 00:00:00

abstract：:The chelator di-2-pyridylketone 4,4-dimethyl-3-thiosemicarbazone (Dp44mT) shows potent and selective anticancer and antimetastatic activity. However, the mechanism by which it is initially transported into cells to induce cytotoxicity is unknown. Hence, the current investigation examined the cellular uptake of ¹⁴C-Dp4...

journal_title：Molecular pharmacology

authors： Merlot AM,Pantarat N,Menezes SV,Sahni S,Richardson DR,Kalinowski DS

更新日期：2013-12-01 00:00:00

abstract：:Polyamides are a class of synthetic molecules that exhibit high-affinity, sequence-specific reversible binding in the DNA minor groove but are incapable of inducing DNA damage. In cell-free systems, polyamides have been shown to regulate gene expression by activation, repression, and antirepression. However, effective...

journal_title：Molecular pharmacology

authors： Philips BJ,Chang AY,Dervan PB,Beerman TA

更新日期：2005-03-01 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：:Sulfated polymannuroguluronate (SPMG) has entered the phase II clinical trial as the first anti-AIDS drug candidate in China. Herein, we report that SPMG was effective at protecting T lymphocytes against apoptosis. Further studies indicated that SPMG significantly elevated mitochondrial membrane potential (MMP) of T c...

journal_title：Molecular pharmacology

authors： Miao B,Li J,Fu X,Gan L,Xin X,Geng M

更新日期：2005-12-01 00:00:00

abstract：:Receptors for the serine protease thrombin and for lysophospholipids are coupled to G proteins and control a wide range of cellular functions, including mitogenesis. Activators of these receptors are present in blood, and can enter the brain during central nervous system (CNS) injury. Reactive astrogliosis, a prominen...

journal_title：Molecular pharmacology

authors： Sorensen SD,Nicole O,Peavy RD,Montoya LM,Lee CJ,Murphy TJ,Traynelis SF,Hepler JR

更新日期：2003-11-01 00:00:00

abstract：:Membrane trafficking of the δ-opioid receptor (DOR) from intracellular compartments to plasma membrane in central neurons, induced by various pathological conditions such as long-term opioid exposure, represents unique receptor plasticity involved in the mechanisms of long-term opioid effects in opioid addiction and o...

journal_title：Molecular pharmacology

authors： Zhang Z,Pan ZZ

更新日期：2012-03-01 00:00:00

abstract：:Although both second messenger response systems are fully functional in both cell lines, activation of muscarinic cholinergic receptors only results in inhibition of adenylate cyclase in NG108-15 neuroblastoma X glioma cells and stimulation of phosphoinositide hydrolysis in 1321N1 human astrocytoma cells. Muscarinic r...

journal_title：Molecular pharmacology

authors： Liang M,Martin MW,Harden TK

更新日期：1987-10-01 00:00:00

abstract：:The human histamine H(4)-receptor (hH(4)R) possesses high constitutive activity and, like the human H(1)-receptor (hH(1)R), is involved in the pathogenesis of type-I allergic reactions. The study aims were to explore the value of dual H(1)/H(4)R antagonists as antiallergy drugs and to address the question of whether H...

journal_title：Molecular pharmacology

authors： Deml KF,Beermann S,Neumann D,Strasser A,Seifert R

更新日期：2009-11-01 00:00:00

abstract：:A family of five cholinergic muscarinic receptor genes (m1, m2, m3, m4, and m5) has recently been identified and cloned. In order to investigate the pharmacological properties of the individual muscarinic receptors, we have transfected each of these genes into Chinese hamster ovary cells (CHO-K1) and have established ...

journal_title：Molecular pharmacology

authors： Buckley NJ,Bonner TI,Buckley CM,Brann MR

更新日期：1989-04-01 00:00:00

abstract：:Inhibition of cannabinoid receptor 1 (CB1) has shown efficacy in reducing body weight and improving metabolic parameters, with the effects correlating with target engagement in the brain. The peripheral effects of inhibiting the CB1 receptor has been appreciated through studies in diet-induced obese and liver-specific...

journal_title：Molecular pharmacology

authors： Zhao W,Fong O,Muise ES,Thompson JR,Weingarth D,Qian S,Fong TM

更新日期：2010-09-01 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：:The immunosuppressive agent cyclosporine A has been shown to reverse multidrug resistance (MDR) in malignant cells. In the present study, a 3H-cyclosporine diazirine analogue was used to photolabel viable MDR Chinese hamster ovary cells. The 170-kDa membrane P-glycoprotein, which functions as a drug efflux pump, was s...

journal_title：Molecular pharmacology

authors： Foxwell BM,Mackie A,Ling V,Ryffel B

更新日期：1989-10-01 00:00:00

abstract：:Adenosine uptake via nucleoside transporters is inhibited when S49 and NG108-15 cell lines cells are exposed to ethanol. This inhibition leads to an accumulation of extracellular adenosine that binds to adenosine A2 receptors and increases cAMP production. Subsequently, there is a heterologous desensitization of recep...

journal_title：Molecular pharmacology

authors： Krauss SW,Ghirnikar RB,Diamond I,Gordon AS

更新日期：1993-11-01 00:00:00

abstract：:The aryl hydrocarbon receptor (AHR) binds planar aromatic compounds and up-regulates the transcription of a battery of xenobiotic-metabolizing enzymes. To identify proteins involved in the biosynthesis of endogenous AHR ligands, we screened extracts of various mouse tissues for AHR signaling activity. We found heart e...

journal_title：Molecular pharmacology

authors： Bittinger MA,Nguyen LP,Bradfield CA

更新日期：2003-09-01 00:00:00

abstract：:We show here that arsenite (As(3+)) elicits multiple effects on gene control, such as the interruption of cell cycle control by initiating G(2)/M arrest as well as inhibiting the aryl hydrocarbon (Ah) receptor-mediated 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD)-inducible expression of CYP1A1. This raises the question ...

journal_title：Molecular pharmacology

authors： Bonzo JA,Chen S,Galijatovic A,Tukey RH

更新日期：2005-04-01 00:00:00

abstract：:Thiourea, phenylthiourea, and methimazole perfused into rat liver stimulated the biliary efflux of GSSG without affecting the excretion of GSH into either the bile or the caval perfusate. The thiocarbamide moiety appears essential, since perfusion with urea, phenylurea, or N-methylimidazole did not stimulate GSSG rele...

journal_title：Molecular pharmacology

authors： Krieter PA,Ziegler DM,Hill KE,Burk RF

更新日期：1984-07-01 00:00:00

abstract：:The bile salt export pump (BSEP/ABCB11) transports bile salts from hepatocytes into bile canaliculi. Its malfunction is associated with severe liver disease. One reason for functional impairment of BSEP is systemic administration of drugs, which as a side effect inhibit the transporter. Therefore, drug candidates are ...

journal_title：Molecular pharmacology

authors： Sohail MI,Schmid D,Wlcek K,Spork M,Szakács G,Trauner M,Stockner T,Chiba P

更新日期：2017-10-01 00:00:00

abstract：:We describe here the cloning and characterization of a rat homolog of the chemokine receptor CXCR3. The predicted amino acid sequence of rat CXCR3 contains 367 amino acid residues, sharing 96 and 87% amino acid sequence identity to the murine and human CXCR3, respectively. Among a large panel of chemokines tested, onl...

journal_title：Molecular pharmacology

authors： Wang X,Li X,Schmidt DB,Foley JJ,Barone FC,Ames RS,Sarau HM

更新日期：2000-06-01 00:00:00