Activation of the c-jun protooncogene in human myeloid leukemia cells treated with etoposide.

abstract：:We present a mechanism for agonist-promoted alpha(2A)-adrenergic receptor (alpha(2A)-AR) activation based on structural, pharmacological, and theoretical evidence of the interactions between phenethylamine ligands and alpha(2A)-AR. In this study, we have: 1) isolated enantiomerically pure phenethylamines that differ b...

journal_title：Molecular pharmacology

authors： Nyrönen T,Pihlavisto M,Peltonen JM,Hoffrén AM,Varis M,Salminen T,Wurster S,Marjamäki A,Kanerva L,Katainen E,Laaksonen L,Savola JM,Scheinin M,Johnson MS

更新日期：2001-05-01 00:00:00

abstract：:The toxicity of acetaminophen (4'-hydroxyacetanilide), 3,5-dimethylacetaminophen (3'-5'-dimethyl-4'-hydroxyacetanilide), and 2,6-dimethylacetaminophen (2',6'-dimethyl-4'-hydroxyacetanilide) was investigated in hepatocytes isolated from phenobarbital-pretreated rats. At a concentration of 5 mM, acetaminophen was found ...

journal_title：Molecular pharmacology

authors： Porubek DJ,Rundgren M,Harvison PJ,Nelson SD,Moldéus P

更新日期：1987-06-01 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：:TNP-ATP has become widely recognized as a potent and selective P2X receptor antagonist, and is currently being used to discriminate between subtypes of P2X receptors in a variety of tissues. We have investigated the ability of TNP-ATP to inhibit alpha,beta-methylene ATP (alpha,beta-meATP)-evoked responses in 1321N1 hu...

journal_title：Molecular pharmacology

authors： Burgard EC,Niforatos W,van Biesen T,Lynch KJ,Kage KL,Touma E,Kowaluk EA,Jarvis MF

更新日期：2000-12-01 00:00:00

abstract：:The anti-human immunodeficiency virus (-HIV) nucleoside analogs azidothymidine (AZT), dideoxycytidine (ddC), dideoxyinosine (ddl), dideoxydidehydrothymidine (D4T), and dideoxydidehydrocytidine (D4C) and the anticancer drug cytosine arabinoside (AraC) were compared for their effects on the mitochondrial DNA (mtDNA) con...

journal_title：Molecular pharmacology

authors： Chen CH,Vazquez-Padua M,Cheng YC

更新日期：1991-05-01 00:00:00

abstract：:Unlike the majority of G protein-coupled receptors, the prostaglandin E(2) (PGE(2)) E-prostanoid 3 (EP3) receptor binds agonist with high affinity that is insensitive to the presence of guanosine 5[prime]-O-(3-thio)triphosphate (GTPγS). We report the identification of mutations that confer GTPγS sensitivity to agonist...

journal_title：Molecular pharmacology

authors： Natarajan C,Hata AN,Hamm HE,Zent R,Breyer RM

更新日期：2013-01-01 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 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

abstract：:In light of the potential use of the thiazolidinedione family of peroxisome proliferator-activated receptor-gamma (PPARgamma) agonists in prostate cancer treatment, this study assessed the mechanism by which these agents suppress prostate-specific antigen (PSA) secretion in prostate cancer cells. Two lines of evidence...

journal_title：Molecular pharmacology

authors： Yang CC,Ku CY,Wei S,Shiau CW,Chen CS,Pinzone JJ,Ringel MD,Chen CS

更新日期：2006-05-01 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：: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：:Four piperazinoquinolone antibacterial drugs (norfloxacin, ciprofloxacin, enoxacin, and pipemidic acid), known to be gamma-aminobutyric acid (GABA) antagonists, fully reversed the inhibitory effect of GABA on [35S]t-butylbicyclophosphorothionate ([35S] TBPS) binding to rat brain membranes in vitro. Twelve indomethacin...

journal_title：Molecular pharmacology

authors： Squires RF,Saederup E

更新日期：1993-05-01 00:00:00

abstract：:Circular RNAs (circRNAs) are a distinct category of single-stranded, covalently closed RNAs formed by backsplicing. The functions of circRNAs are incompletely known and are under active investigation. Here, we report that in addition to traditional linear mRNAs (linRNA), mouse, rat, and human opioid receptor genes gen...

journal_title：Molecular pharmacology

authors： Irie T,Shum R,Deni I,Hunkele A,Le Rouzic V,Xu J,Wilson R,Fischer GW,Pasternak GW,Pan YX

更新日期：2019-08-01 00:00:00

abstract：:The instability of the solubilized/purified form, the lack of catalytic activity of the stabilized, macrolide-complexed form, and the compromised catalytic activity of the decomplexed form of steroid-inducible cytochrome P450IIIA1 motivated further investigations of the substrate specificity of this isozyme. A major c...

journal_title：Molecular pharmacology

authors： Namkung MJ,Yang HL,Hulla JE,Juchau MR

更新日期：1988-11-01 00:00:00

abstract：:Lysophosphatidic acid (LPA) and sphingosine-1-phosphate (S1P) are members of the phospholipid growth factor family. A major limitation in the field to date has been a lack of receptor subtype-specific agonists and antagonists. Here, we report that dioctylglycerol pyrophosphate and dioctylphosphatidic acid are selectiv...

journal_title：Molecular pharmacology

authors： Fischer DJ,Nusser N,Virag T,Yokoyama K,Wang Da,Baker DL,Bautista D,Parrill AL,Tigyi G

更新日期：2001-10-01 00:00:00

abstract：:Poly(ADP-ribose) polymerase-1 (PARP-1) is a NAD-consuming enzyme with an emerging key role in epigenetic regulation of gene transcription. Although PARP-1 expression is characteristically restricted to the nucleus, a few studies report the mitochondrial localization of the enzyme and its ability to regulate organelle ...

journal_title：Molecular pharmacology

authors： Lapucci A,Pittelli M,Rapizzi E,Felici R,Moroni F,Chiarugi A

更新日期：2011-06-01 00:00:00

abstract：:Metallothioneins (MTs) are cytoplasmic proteins that sequester certain divalent cations and are considered a primary cellular defense against the toxic transition metal cadmium (Cd(2+)). MT-I/II(-/-) knockout [MT(-/-)] cells are available and serve as an excellent tool to study non-MT-related mechanisms in metal toler...

journal_title：Molecular pharmacology

authors： Leslie EM,Liu J,Klaassen CD,Waalkes MP

更新日期：2006-02-01 00:00:00

abstract：:Extracellular protons inhibit N-methyl-D-aspartate (NMDA) receptors with an IC50 value in the physiological pH range. To identify the molecular determinants of proton sensitivity, we used scanning mutagenesis of the NR1 subunit to search for residues that control proton inhibition of NMDA receptors. Homology modeling ...

journal_title：Molecular pharmacology

authors： Low CM,Lyuboslavsky P,French A,Le P,Wyatte K,Thiel WH,Marchan EM,Igarashi K,Kashiwagi K,Gernert K,Williams K,Traynelis SF,Zheng F

更新日期：2003-06-01 00:00:00

abstract：:Voltage-gated potassium (Kv) channels regulate many physiological functions and represent important therapeutic targets in the treatment of several clinical disorders. Although some of these channels have been well-characterized, the study of others, such as Kv3 channels, has been hindered because of limited pharmacol...

journal_title：Molecular pharmacology

authors： Yan L,Herrington J,Goldberg E,Dulski PM,Bugianesi RM,Slaughter RS,Banerjee P,Brochu RM,Priest BT,Kaczorowski GJ,Rudy B,Garcia ML

更新日期：2005-05-01 00:00:00

abstract：:In PC12 cells stably expressing alpha(1A)-adrenergic receptors (ARs), norepinephrine (NE) activates several mitogen-activated protein kinase pathways and causes differentiation (). Using retroviral luciferase reporters, we found that NE also activated both signal transducers and activators of transcription (Stat) and ...

journal_title：Molecular pharmacology

authors： Zhong H,Murphy TJ,Minneman KP

更新日期：2000-05-01 00:00:00

abstract：:Cardiac function is regulated by many hormones and neurotransmitters that exert their physiological effects through the activation of G protein-coupled receptors (GPCRs). Identification of new GPCRs that might display a specific pattern of expression within the heart and differentially regulate specific cardiac functi...

journal_title：Molecular pharmacology

authors： Moore-Morris T,Varrault A,Mangoni ME,Le Digarcher A,Negre V,Dantec C,Journot L,Nargeot J,Couette B

更新日期：2009-05-01 00:00:00

abstract：:Adaptive changes in gene expression are thought to contribute to dependence, addiction and other behavioral responses to chronic ethanol abuse. DNA array studies provide a nonbiased detection of networks of gene expression changes, allowing insight into functional consequences and mechanisms of such molecular response...

journal_title：Molecular pharmacology

authors： Thibault C,Lai C,Wilke N,Duong B,Olive MF,Rahman S,Dong H,Hodge CW,Lockhart DJ,Miles MF

更新日期：2000-12-01 00:00:00

abstract：:Acetylsalicylic acid (aspirin) is a cyclooxygenase (COX) inhibitor, yet some of its therapeutic effects are thought to derive from mechanisms unrelated to prostaglandin synthesis inhibition. In human intestinal myofibroblasts, aspirin, at therapeutic doses, had the unexpected effect of inducing prolonged COX-2 express...

journal_title：Molecular pharmacology

authors： Mifflin RC,Saada JI,Di Mari JF,Valentich JD,Adegboyega PA,Powell DW

更新日期：2004-02-01 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：: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：:Reversible binding of warfarin to defatted serum albumin was studied by equilibrium dialysis at pH 7.4, in a 66 mM sodium phosphate buffer at 37 degrees. The binding isotherm could be described by two stoichiometric binding constants, K1 in the range 141,000 to 192,000 M-1 and K2 at 39,000 to 57,000 M-1. At least two ...

journal_title：Molecular pharmacology

authors： Larsen FG,Larsen CG,Jakobsen P,Brodersen R

更新日期：1985-02-01 00:00:00

abstract：:Studies in vertebrate neuromuscular synapses have revealed previously that ATP, via P2Y receptors, plays a critical role in regulating postsynaptic gene expressions. An equivalent regulatory role of ATP and its P2Y receptors would not necessarily be expected for the very different situation of the brain synapses, but ...

journal_title：Molecular pharmacology

authors： Siow NL,Choi RC,Xie HQ,Kong LW,Chu GK,Chan GK,Simon J,Barnard EA,Tsim KW

更新日期：2010-12-01 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：:In rat pancreatic zymogen granules (ZG), an ATP-sensitive K(+) conductance and a Cl(-) conductance have been characterized that are inversely regulated by an approximately 65-kDa multidrug resistance P-glycoprotein (mdr1) gene product. In search of a label for purification of this protein, we found that the dihydropyr...

journal_title：Molecular pharmacology

authors： Braun M,Thévenod F

更新日期：2000-02-01 00:00:00

abstract：:Voltage-gated sodium channels are inhibited by many local anesthetics, antiarrhythmics, and antiepileptic drugs. The local anesthetic lidocaine appears to be able to access its binding site in the sodium channel only from the membrane phase or from the internal face of the channel. In contrast, the antiepileptic drug ...

journal_title：Molecular pharmacology

authors： Jo S,Bean BP

更新日期：2014-02-01 00:00:00