Effect of p53 status on sensitivity to platinum complexes in a human ovarian cancer cell line.

abstract：:The nuclear receptor peroxisome proliferator-activated receptor (PPAR) is activated by a diverse group of acidic ligands, including many peroxisome proliferator chemicals present in the environment. Janus tyrosine kinase-signal transducer and activator of transcription (JAK-STAT) signaling is activated by multiple cyt...

journal_title：Molecular pharmacology

authors： Shipley JM,Waxman DJ

更新日期：2003-08-01 00:00:00

abstract：:The cannabinoid analog abnormal cannabidiol [abn-cbd; (-)-4-(3-3,4-trans-p-menthadien-[1,8]-yl)-olivetol] does not bind to CB(1) or CB(2) receptors, yet it acts as a full agonist in relaxing rat isolated mesenteric artery segments. Vasorelaxation by abn-cbd is endothelium-dependent, pertussis toxin-sensitive, and is i...

journal_title：Molecular pharmacology

authors： Offertáler L,Mo FM,Bátkai S,Liu J,Begg M,Razdan RK,Martin BR,Bukoski RD,Kunos G

更新日期：2003-03-01 00:00:00

abstract：:The cytolytic ionotropic ATP receptor P2X7 has several important roles in immune cell regulation, such as cytokine release, apoptosis, and microbial killing. Although P2X7 receptors are frequently coexpressed with another subtype of P2X receptor, P2X4, they are believed not to form heteromeric assemblies but to functi...

journal_title：Molecular pharmacology

authors： Guo C,Masin M,Qureshi OS,Murrell-Lagnado RD

更新日期：2007-12-01 00:00:00

abstract：:The human mu-opioid receptor (HmuOR) is a G-protein coupled receptor that mediates analgesia, euphoria and other important central and peripheral neurological functions. In this study, we found in a yeast two-hybrid screen that a protein kinase C-interacting protein (PKCI) specifically interacts with the C terminus of...

journal_title：Molecular pharmacology

authors： Guang W,Wang H,Su T,Weinstein IB,Wang JB

更新日期：2004-11-01 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：:High-affinity glycine transport in neurons and glial cells is a primary means of inactivating synaptic glycine. We have synthesized a potent selective inhibitor of glycine transporter 1 (GlyT1), and characterized its activity using a quail fibroblast cell line (QT6). The glycine transporters GlyT1A, GlyT1B, GlyT1C, an...

journal_title：Molecular pharmacology

authors： Atkinson BN,Bell SC,De Vivo M,Kowalski LR,Lechner SM,Ognyanov VI,Tham CS,Tsai C,Jia J,Ashton D,Klitenick MA

更新日期：2001-12-01 00:00:00

abstract：:Poly(A)+ RNA from mammalian retina expresses bicuculline/baclofen-insensitive gamma-aminobutyric acid (GABA) receptors in Xenopus oocytes with properties similar to those of homooligomeric GABA rho 1 receptors. The pharmacological profile of these rho-like receptors was extended by measuring sensitivities to various G...

journal_title：Molecular pharmacology

authors： Woodward RM,Polenzani L,Miledi R

更新日期：1993-04-01 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：:Receptors have well-conserved regions that are recognized and activated by hormones and neurotransmitters. Most drugs bind to these sites and mimic or block the action of the native ligands. Using a high-throughput functional screen, we identified a potent and selective M(1) muscarinic receptor agonist from a novel st...

journal_title：Molecular pharmacology

authors： Spalding TA,Trotter C,Skjaerbaek N,Messier TL,Currier EA,Burstein ES,Li D,Hacksell U,Brann MR

更新日期：2002-06-01 00:00:00

abstract：:The ligand-binding sites of many G protein-coupled receptors (GPCRs) are situated around and deeply embedded within the central pocket formed by their seven transmembrane-spanning α-helical domains. Generally, these binding sites are assumed accessible to endogenous ligands from the aqueous phase. Recent advances in t...

journal_title：Molecular pharmacology

authors： Szlenk CT,Gc JB,Natesan S

更新日期：2019-11-01 00:00:00

abstract：:It has been demonstrated previously that cannabinol (CBN) differentially modulates interleukin-2 (IL-2) protein secretion by T cells with a corresponding change in extracellular signal-regulated kinase activity. The objective of the present studies was to further investigate the molecular mechanism by which CBN enhanc...

journal_title：Molecular pharmacology

authors： Jan TR,Rao GK,Kaminski NE

更新日期：2002-02-01 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：:Many progestins have been developed for use in contraception, menopausal hormone therapy, and treatment of gynecological diseases. They are derived from either progesterone or testosterone, and they act by binding to the progesterone receptor (PR), a hormone-inducible transcription factor belonging to the nuclear rece...

journal_title：Molecular pharmacology

authors： Petit-Topin I,Turque N,Fagart J,Fay M,Ulmann A,Gainer E,Rafestin-Oblin ME

更新日期：2009-06-01 00:00:00

abstract：:The gene encoding a human 5-hydroxytryptamine (5-HT)1 receptor subtype was isolated from a human placental genomic library by using oligonucleotide probes derived from transmembrane regions of the cloned human 5-HT1D beta receptor. The deduced amino acid sequence of the genomic clone hp75d is identical to that of the ...

journal_title：Molecular pharmacology

authors： Zgombick JM,Schechter LE,Macchi M,Hartig PR,Branchek TA,Weinshank RL

更新日期：1992-08-01 00:00:00

abstract：:The successful synthesis of dolastatin 11, a depsipeptide originally isolated from the mollusk Dolabella auricularia, permitted us to study its effects on cells. The compound arrested cells at cytokinesis by causing a rapid and massive rearrangement of the cellular actin filament network. In a dose-and time-dependent ...

journal_title：Molecular pharmacology

authors： Bai R,Verdier-Pinard P,Gangwar S,Stessman CC,McClure KJ,Sausville EA,Pettit GR,Bates RB,Hamel E

更新日期：2001-03-01 00:00:00

abstract：:The exofacial part of transmembrane domain 5 (TMD 5) of the cationic amine-binding subclass of 7-transmembrane receptors is thought to be important in binding the side chain of the agonist. Residues Ile-188 through Ala-196 in TMD 5 of the M(1) muscarinic acetylcholine receptor (mAChR) have been studied by Cys- and Ala...

journal_title：Molecular pharmacology

authors： Allman K,Page KM,Curtis CA,Hulme EC

更新日期：2000-07-01 00:00:00

abstract：:In cells expressing both the insulin receptor isoform A (IRA) and the insulin-like growth factor-1 receptor (IGF1R), the presence of hybrid receptors, made up of an alphabeta-IRA chain associated with an alphabeta-IGF1R chain, has been demonstrated. These heterodimers are found in normal cells, and they also seem to p...

journal_title：Molecular pharmacology

authors： Blanquart C,Gonzalez-Yanes C,Issad T

更新日期：2006-11-01 00:00:00

abstract：:The nonselective cation channel TRPA1 (ANKTM1, p120) is a potential mediator of pain, and selective pharmacological modulation of this channel may be analgesic. Although several TRPA1 activators exist, these tend to be either reactive or of low potency and/or selectivity. The aim of the present study, therefore, was t...

journal_title：Molecular pharmacology

authors： Maher M,Ao H,Banke T,Nasser N,Wu NT,Breitenbucher JG,Chaplan SR,Wickenden AD

更新日期：2008-04-01 00:00:00

abstract：:Benzamide riboside (BR) and tiazofurin (TR) are converted to analogs of NAD that inhibit IMP dehydrogenase (IMPDH), resulting in cellular depletion of GTP and dGTP and inhibition of proliferation. The current work was undertaken to identify the human nucleoside transporters involved in cellular uptake of BR and TR and...

journal_title：Molecular pharmacology

authors： Damaraju VL,Visser F,Zhang J,Mowles D,Ng AM,Young JD,Jayaram HN,Cass CE

更新日期：2005-01-01 00:00:00

abstract：:A UDP-glucuronosyltransferase (UDPGT) isoenzyme capable of morphine glucuronidation has been purified to apparent homogeneity and partially characterized from hepatic microsomes of female Wistar rats which have low 3 alpha-hydroxysteroid UDPGT. A rapid and sensitive assay was developed to quantify morphine glucuronide...

journal_title：Molecular pharmacology

authors： Puig JF,Tephly TR

更新日期：1986-12-01 00:00:00

abstract：:Smad4, a key transcription factor in the transforming growth factor-β signaling pathway, is involved in a variety of cell physiologic and pathologic processes. Here, we characterized megakaryocyte/platelet-specific Smad4 deficiency in mice to elucidate its effect on platelet function. We found that megakaryocyte/plate...

journal_title：Molecular pharmacology

authors： Wang Y,Jiang L,Mo X,Lan Y,Yang X,Liu X,Zhang J,Zhu L,Liu J,Wu X

更新日期：2017-09-01 00:00:00

abstract：:Nod2 is an intracellular pattern recognition receptor that detects a conserved moiety of bacterial peptidoglycan and subsequently activates proinflammatory signaling pathways. Mutations in Nod2 have been implicated to be linked to inflammatory granulomatous disorders, such as Crohn's disease and Blau syndrome. Many ph...

journal_title：Molecular pharmacology

authors： Huang S,Zhao L,Kim K,Lee DS,Hwang DH

更新日期：2008-07-01 00:00:00

abstract：:Previous studies have shown that at least two subtypes of somatostatin (SRIF) receptors (SRIF1 and SRIF2) are expressed in mammalian cells. SRIF1 receptors have high affinity for MK 678, whereas SRIF2 receptors have no affinity for MK 678 but selectively bind peptides with structures similar to that of CGP 23996. Rece...

journal_title：Molecular pharmacology

authors： Rens-Domiano S,Law SF,Yamada Y,Seino S,Bell GI,Reisine T

更新日期：1992-07-01 00:00:00

abstract：:The alpha2-adrenergic receptors (alpha2-ARs) mediate signals to intracellular second messengers via guanine nucleotide binding proteins. Three human genes encoding alpha2-AR subtypes (alpha2A, alpha2B, alpha2C) have been cloned. Several chemical compounds display subtype differences in their binding and/or functional ...

journal_title：Molecular pharmacology

authors： Marjamaki A,Pihlavisto M,Cockcroft V,Heinonen P,Savola JM,Scheinin M

更新日期：1998-03-01 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：:The heart is richly endowed with K(ATP) channels, which function as biological sensors, regulating membrane potentials and electrical excitability in response to metabolic alterations. We recently reported that the cytochrome P450 metabolites of arachidonic acid, epoxyeicosatrienoic acids (EETs), potently activate car...

journal_title：Molecular pharmacology

authors： Lu T,VanRollins M,Lee HC

更新日期：2002-11-01 00:00:00

abstract：:Kinetics of the interactions between the neuromuscular blocker alcuronium, the specific muscarinic antagonist N-[methyl-3H] methyl scopolamine ([3H]NMS), and muscarinic receptors were investigated in homogenates of rat heart atria. Two effects of alcuronium on the binding of [3H]NMS could be distinguished. (a) Alcuron...

journal_title：Molecular pharmacology

authors： Proska J,Tucek S

更新日期：1994-04-01 00:00:00

abstract：:Reversal of the multidrug-resistant (MDR) phenotype is very important for chemotherapy success. In fact, the expression of the MDR1 gene-encoded P-glycoprotein (P-gp) actively expels antitumor agents such as daunomycin (DNM) out of the cells, resulting in drug resistance. We show that upon conjugation to triplex-formi...

journal_title：Molecular pharmacology

authors： Stierlé V,Duca M,Halby L,Senamaud-Beaufort C,Capobianco ML,Laigle A,Jollès B,Arimondo PB

更新日期：2008-05-01 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：: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