Orientation of the heterodimeric aryl hydrocarbon (dioxin) receptor complex on its asymmetric DNA recognition sequence.

abstract：:Ca2-dependent protein phosphorylations activated by calmodulin or phospholipid were studied using selective inhibitors. Both protein phosphorylations were inhibited by N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide (W-7) and its derivatives. Kinetic analysis indicated that the primary effect of these agents was me...

journal_title：Molecular pharmacology

authors： Tanaka T,Ohmura T,Yamakado T,Hidaka H

更新日期：1982-09-01 00:00:00

abstract：:Previously, we reported the presence of dual promoters, referred to as distal (DP) and proximal, with a negative regulatory element between them in the mouse mu-opioid receptor (mor) gene. Here we have identified a positive regulatory element influencing mor DP transcription, which contains multiple consensus binding ...

journal_title：Molecular pharmacology

authors： Im HJ,Smirnov D,Yuhi T,Raghavan S,Olsson JE,Muscat GE,Koopman P,Loh HH

更新日期：2001-06-01 00:00:00

abstract：:A number of different agonists activate G protein-coupled receptors to stimulate adenylyl cyclase (AC), increase cAMP formation, and promote relaxation in vascular smooth muscle. To more fully understand this stimulation of AC, we assessed the expression, regulation, and compartmentation of AC isoforms in rat aortic s...

journal_title：Molecular pharmacology

authors： Ostrom RS,Liu X,Head BP,Gregorian C,Seasholtz TM,Insel PA

更新日期：2002-11-01 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：:Purified assembly-competent vimentin, an intermediate filament protein, was obtained from bovine lens in this study. The effects of withangulatin A on vimentin assembly with or without phosphorylation were examined by negative-stain electron microscopy. Soluble tetrameric vimentin was assembled into irregular fibrils ...

journal_title：Molecular pharmacology

authors： Perng MD,Cheng TJ,Chen CM,Lai YK

更新日期：1994-10-01 00:00:00

abstract：:Interleukin-2 (IL-2) is an immunoregulatory cytokine whose biological effects are mediated through interaction with specific receptors on the surface of target cells. Due to its presumed role in generating a normal immune response, IL-2 is being evaluated for the treatment of a variety of tumors, in addition to infect...

journal_title：Molecular pharmacology

authors： Chang DZ,Tasayco ML,Ciardelli TL

更新日期：1995-01-01 00:00:00

abstract：:Estrogenic and carcinogenic activity are shown to be separable properties. 2-Fluoroestradiol, a modified estrogen, did not induce renal clear-cell carcinoma in male Syrian hamsters despite its estrogenic potency, which is comparable to that of estradiol. 4-Fluoroestradiol, also a potent estrogen, did induce renal clea...

journal_title：Molecular pharmacology

authors： Liehr JG

更新日期：1983-03-01 00:00:00

abstract：:Cyclic nucleotide phosphodiesterases (PDEs) from canine trachealis were characterized with respect to their kinetic properties, sensitivity to selective inhibitors, and subcellular distribution. Extracts from whole tissue homogenates were applied to DEAE-Sepharose anion exchange columns and eluted with a linear sodium...

journal_title：Molecular pharmacology

authors： Torphy TJ,Cieslinski LB

更新日期：1990-02-01 00:00:00

abstract：:Both human ether-à-go-go-related gene (hERG1) and the closely related human ether-à-go-go (hEAG1) channel are aberrantly expressed in a large proportion of human cancers. In the present study, we demonstrate that transfection of hERG1 into mouse fibroblasts is sufficient to induce many features characteristic of malig...

journal_title：Molecular pharmacology

authors： Pier DM,Shehatou GS,Giblett S,Pullar CE,Trezise DJ,Pritchard CA,Challiss RA,Mitcheson JS

更新日期：2014-08-01 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：:Monoamine oxidases (MAOs) A and B, flavin-containing enzymes found in the outer mitochondrial membrane, oxidize many important biogenic and xenobiotic amines. The two enzymes are expressed in many tissues, with some tissues containing primarily one form and others containing both. Although MAO in placental mitochondri...

journal_title：Molecular pharmacology

authors： Riley LA,Waguespack MA,Denney RM

更新日期：1989-07-01 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：:Electrical recordings were made in Xenopus oocytes to study the modulatory effects of steroids on gamma-aminobutyric acid (GABA) receptors expressed by RNA from mammalian brain and retina. GABA responses expressed by rat cerebral cortex poly(A)+ RNA were bicuculline-sensitive Cl- currents mediated by GABAA receptors. ...

journal_title：Molecular pharmacology

authors： Woodward RM,Polenzani L,Miledi R

更新日期：1992-01-01 00:00:00

abstract：:Reconstitution experiments with purified components reproduce the basic characteristics of receptor/G protein coupling, i.e., GTP-sensitive high affinity agonist binding and receptor-promoted GTP binding. However, the interaction of agonists with the A1 adenosine receptor in rat and bovine but not human brain membrane...

journal_title：Molecular pharmacology

authors： Nanoff C,Mitterauer T,Roka F,Hohenegger M,Freissmuth M

更新日期：1995-11-01 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：: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：: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：:Serotonin [5-hydroxytryptamine (5-HT)] receptors are distinguished pharmacologically by their characteristic affinities for agonists and antagonists. Two serotonin receptors, the 5-HT2 and 5-HT1c, share a number of pharmacologic and structural properties while differing in their affinities for certain agonists and ant...

journal_title：Molecular pharmacology

authors： Choudhary MS,Craigo S,Roth BL

更新日期：1992-10-01 00:00:00

abstract：:ORKAMBI, a combination of the corrector, lumacaftor, and the potentiator, ivacaftor, partially rescues the defective processing and anion channel activity conferred by the major cystic fibrosis-causing mutation, F508del, in in vitro studies. Clinically, the improvement in lung function after ORKAMBI treatment is modes...

journal_title：Molecular pharmacology

authors： Wu YS,Jiang J,Ahmadi S,Lew A,Laselva O,Xia S,Bartlett C,Ip W,Wellhauser L,Ouyang H,Gonska T,Moraes TJ,Bear CE

更新日期：2019-10-01 00:00:00

abstract：:Bryostatin 1 and phorbol-12-myristate-13-acetate (PMA) are both potent activators of protein kinase C (PKC), although in primary mouse keratinocytes bryostatin 1 does not induce differentiation and blocks PMA-induced differentiation. We report here that in primary mouse keratinocytes PMA caused translocation of PKC-ep...

journal_title：Molecular pharmacology

authors： Szallasi Z,Denning MF,Smith CB,Dlugosz AA,Yuspa SH,Pettit GR,Blumberg PM

更新日期：1994-11-01 00:00:00

abstract：:Microinjection, but not extracellular application, of cytidine-5'-diphosphate-D-glucose (CDPG) has been shown to elicit Ca(2+)-dependent currents in Xenopus laevis oocytes. These responses were comparable to those of inositol-1,4,5-trisphosphate (InsP3) in being both rapid and dose dependent. For example, maximal ampl...

journal_title：Molecular pharmacology

authors： Kim HY,Thomas D,Hanley MR

更新日期：1996-02-01 00:00:00

abstract：:2,3,7,8-Tetrachlorodibenzo-p-dioxin (TCDD), beta-naphthoflavone (beta NF), and phenobarbital (PB) cause marked induction of cytochrome P-450 (P-450)-mediated arachidonic acid metabolism in chick embryo liver. We show here that the P-450 arachidonic acid epoxygenases induced by TCDD and beta NF are immunochemically ind...

journal_title：Molecular pharmacology

authors： Kanetoshi A,Ward AM,May BK,Rifkind AB

更新日期：1992-12-01 00:00:00

abstract：:Rat liver and brain membrane alpha 1-adrenergic receptors were purified greater than 500-fold by successive chromatographic steps using heparin-agarose, an affinity matrix constructed by coupling a novel derivative of the alpha 1-selective antagonist prazosin to Affigel-102 and wheat germ agglutinin-agarose. Several l...

journal_title：Molecular pharmacology

authors： Terman BI,Riek RP,Grodski A,Hess HJ,Graham RM

更新日期：1990-04-01 00:00:00

abstract：:Prior studies indicate that adenosine and the adenosine A2A receptor play a role in hepatic fibrosis by a mechanism that has been proposed to involve direct stimulation of hepatic stellate cells (HSCs). The objective of this study was to determine whether primary hepatic stellate cells produce collagen in response to ...

journal_title：Molecular pharmacology

authors： Che J,Chan ES,Cronstein BN

更新日期：2007-12-01 00:00:00

abstract：:Undesired block of human ERG1 potassium channels is the basis for cardiac side effects of many different types of drugs. Therefore, it is important to know exactly why some drugs particularly bind to these channels with high affinity. Upon expression in mammalian cells and Xenopus laevis oocytes, we investigated the i...

journal_title：Molecular pharmacology

authors： Gessner G,Zacharias M,Bechstedt S,Schönherr R,Heinemann SH

更新日期：2004-05-01 00:00:00

abstract：:Benzbromarone (BBR), a potent uricosuric agent for the management of gout, is known to cause fatal fulminant hepatitis. While the mechanism of BBR-induced idiosyncratic hepatotoxicity remains unelucidated, cytochrome P450 enzyme (CYP450)-mediated bioactivation of BBR to electrophilic reactive metabolites is commonly r...

journal_title：Molecular pharmacology

authors： Tang LWT,Verma RK,Fan H,Chan ECY

更新日期：2021-01-12 00:00:00

abstract：:Activators of G protein signaling (AGS), initially discovered in the search for receptor-independent activators of G protein signaling, define a broad panel of biologic regulators that influence signal transfer from receptor to G-protein, guanine nucleotide binding and hydrolysis, G protein subunit interactions, and/o...

journal_title：Molecular pharmacology

authors： Blumer JB,Lanier SM

更新日期：2014-03-01 00:00:00

abstract：:The presence of DNA damage initiates signaling through the ataxia-telangiectasia mutated kinase (ATM) and the ATM- and the Rad3-related kinase (ATR), which phosphorylate, thus activating, the checkpoint kinases (Chk) 1 and 2, which leads to cell cycle arrest. The bifunctional DNA alkylator 1,3-bis(2-chloroethyl)-1-nit...

journal_title：Molecular pharmacology

authors： Cui B,Johnson SP,Bullock N,Ali-Osman F,Bigner DD,Friedman HS

更新日期：2009-06-01 00:00:00

abstract：:Tetrodotoxin-sensitive Na(+) currents have been extensively studied because they play a major role in neuronal firing and bursting. In this study, we showed that voltage-dependent Na(+) currents are regulated in a slow manner by oxotremorine (oxo-M) and angiotensin II in rat sympathetic neurons. We found that these cu...

journal_title：Molecular pharmacology

authors： Puente EI,De la Cruz L,Arenas I,Elias-Viñas D,Garcia DE

更新日期：2016-04-01 00:00:00

abstract：:Iron is a biologically essential metal, but excess iron can cause damage to the cardiovascular and nervous systems. We examined the effects of extracellular Fe²⁺ on permeation and gating of Ca(V)3.1 channels stably transfected in HEK293 cells, by using whole-cell recording. Precautions were taken to maintain iron in t...

journal_title：Molecular pharmacology

authors： Lopin KV,Gray IP,Obejero-Paz CA,Thévenod F,Jones SW

更新日期：2012-12-01 00:00:00