Thiosemicarbazones Functioning as Zinc Metallochaperones to Reactivate Mutant p53.

abstract：:We have examined alpha1beta2gamma2L GABAA receptor modulation by the endogenous steroids allopregnanolone (3alpha5alphaP), pregnenolone sulfate, and beta-estradiol in the absence and presence of ethanol. Coapplication of 0.1 to 1% (17-170 mM) ethanol influenced receptor modulation by 3alpha5alphaP but not that by preg...

journal_title：Molecular pharmacology

authors： Akk G,Li P,Manion BD,Evers AS,Steinbach JH

更新日期：2007-02-01 00:00:00

abstract：:We have identified alpha 2-adrenergic receptors on human erythroleukemia (HEL) cells, a suspension-grown cell line related to human platelets. properties of receptors were assessed in intact cells by binding of the antagonist [3H]yohimbine and by inhibition of cAMP accumulation. [3H]Yohimbine labeled 5900 +/- 2100 rec...

journal_title：Molecular pharmacology

authors： McKernan RM,Howard MJ,Motulsky HJ,Insel PA

更新日期：1987-08-01 00:00:00

abstract：:Previously, we showed that the human kappa-opioid receptor (hkor) stably expressed in Chinese hamster ovary (CHO) cells underwent down-regulation after prolonged U50,488H treatment. In the present study, we determined the mechanisms underlying this process. U50, 488H caused a significant down-regulation of the hkor, a...

journal_title：Molecular pharmacology

authors： Li JG,Benovic JL,Liu-Chen LY

更新日期：2000-10-01 00:00:00

abstract：:The human dopamine and norepinephrine transporters (hDAT and hNET, respectively) control neurotransmitter levels within the synaptic cleft and are the site of action for amphetamine (AMPH) and cocaine. We investigated the role of a threonine residue within the highly conserved and putative phosphorylation sequence RET...

journal_title：Molecular pharmacology

authors： Guptaroy B,Fraser R,Desai A,Zhang M,Gnegy ME

更新日期：2011-03-01 00:00:00

abstract：:The regulation of cellular responsiveness to dopamine via the D2 dopamine receptor was investigated in mouse fibroblast Ltk-cells stably expressing the rat D2-short receptor [Nature (Lond.) 336:783-787 (1988)]. Dopamine inhibited forskolin-stimulated cAMP levels in these cells (half-maximal inhibition at 3.9 +/- 1.1 n...

journal_title：Molecular pharmacology

authors： Bates MD,Senogles SE,Bunzow JR,Liggett SB,Civelli O,Caron MG

更新日期：1991-01-01 00:00:00

abstract：:KARs, new semisynthetic antitumor bis-indole derivatives, were found to be inhibitors of tubulin polymerization with lower toxicity than vinblastine or vincristine, used in chemotherapy. Here, we compare the effect of KARs with those of vinblastine and vincristine on cell viability, cell proliferation, and cell cycle ...

journal_title：Molecular pharmacology

authors： Comín-Anduix B,Agell N,Bachs O,Ovádi J,Cascante M

更新日期：2001-12-01 00:00:00

abstract：:The mitogen-activated protein kinase (MAPK) pathway plays a pivotal role in intracellular signaling, and this cascade may impinge on cAMP response elements (CREs) of target genes. Both the MAPK pathway and chromogranin A expression may be activated by cytosolic calcium influx, and calcium-dependent signals map onto th...

journal_title：Molecular pharmacology

authors： Tang K,Wu H,Mahata SK,O'Connor DT

更新日期：1998-07-01 00:00:00

abstract：:Nicotine biotransformation affects the smoking habits of addicted individuals and therefore their health risk. Using an improved analytical method, we have discovered that the human UDP-glucuronosyltransferase (UGT) 2B10, a liver enzyme previously unknown to conjugate nicotine or exhibit considerable activity toward a...

journal_title：Molecular pharmacology

authors： Kaivosaari S,Toivonen P,Hesse LM,Koskinen M,Court MH,Finel M

更新日期：2007-09-01 00:00:00

abstract：:An 'epoxygenase' eicosanoid analog, 14, 15-cis-episulfide-eicosatrienoic acid, has several unique pharmacological effects on platelets. These include (i) inhibition of ionophore A23187- but not thrombin-induced activation, (ii) inhibition of thromboxane B2 biosynthesis derived from endogenous but not exogenous arachid...

journal_title：Molecular pharmacology

authors： Bernstrom K,Malcolm K,McGee J,Maclouf J,Levy-Toledano S,Falck JR,Fitzpatrick FA

更新日期：1991-02-01 00:00:00

abstract：:Prolonged ethanol exposure causes central nervous system hyperexcitability that involves a loss of GABAergic inhibition. We previously demonstrated that long-term ethanol exposure enhances the internalization of synaptic GABA(A) receptors composed of alpha1beta2/3gamma2 subunits. However, the mechanisms of ethanol-med...

journal_title：Molecular pharmacology

authors： Kumar S,Suryanarayanan A,Boyd KN,Comerford CE,Lai MA,Ren Q,Morrow AL

更新日期：2010-05-01 00:00:00

abstract：:The sympathetic nervous system modulates cardiac contractility and rate by activating beta-adrenergic receptors (beta AR) expressed on cardiac myocytes and specialized cells in the sinoatrial node and the conduction system. Recent clinical studies have suggested that beta-adrenergic receptors also play a role in cardi...

journal_title：Molecular pharmacology

authors： Devic E,Xiang Y,Gould D,Kobilka B

更新日期：2001-09-01 00:00:00

abstract：:A method was developed to measure the formation of glutathione adducts of 1-chloro-2,4-dinitrobenzene (CDNB) and 2,4-dichloro-1-nitrobenzene (DCNB) in periportal and pericentral regions of the liver lobule in the isolated perfused rat liver by surface reflectance spectrophotometry. Conjugates of DCNB and CDNB are rele...

journal_title：Molecular pharmacology

authors： Harris C,Thurman RG

更新日期：1986-01-01 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：:Glutathione-S-transferase-catalyzed conjugation of glutathione (GSH) to aflatoxin B1-8,9-epoxide plays an important role in preventing binding of this ultimate carcinogen to target macromolecules. Once formed, the aflatoxin B1-epoxide-GSH conjugates are actively extruded from the cell by an unidentified ATP-dependent ...

journal_title：Molecular pharmacology

authors： Loe DW,Stewart RK,Massey TE,Deeley RG,Cole SP

更新日期：1997-06-01 00:00:00

abstract：:PDE4A11 is a novel cAMP-specific phosphodiesterase that is conserved in humans, mouse, rat, pig, and bat. Exon-1(4A11) encodes its unique, 81 amino acid N-terminal region. Reverse-transcriptase polymerase chain reaction performed across the splice junction, plus identification of expressed sequence tags, identifies PD...

journal_title：Molecular pharmacology

authors： Wallace DA,Johnston LA,Huston E,MacMaster D,Houslay TM,Cheung YF,Campbell L,Millen JE,Smith RA,Gall I,Knowles RG,Sullivan M,Houslay MD

更新日期：2005-06-01 00:00:00

abstract：:The gamma-aminobutyric acid(A) (GABA(A)) receptor contains a binding site (or sites) for benzodiazepines and related ligands. Previous studies have shown that the residue occupying position 101 (rat numbering) of the alpha subunit is particularly important in determining how some of these compounds interact with the r...

journal_title：Molecular pharmacology

authors： Dunn SM,Davies M,Muntoni AL,Lambert JJ

更新日期：1999-10-01 00:00:00

abstract：:The 5'-flanking region of the mouse mu opioid receptor (MOR) gene has two promoters, referred to as distal and proximal. MOR mRNA is predominantly initiated by the proximal promoter. Previously, several important cis-elements and trans-factors have been shown to play a functional role in the proximal promoter of the M...

journal_title：Molecular pharmacology

authors： Choi HS,Hwang CK,Kim CS,Song KY,Law PY,Wei LN,Loh HH

更新日期：2005-05-01 00:00:00

abstract：:Avermectins are a family of potent broad-spectrum anthelmintic compounds, which bind with high affinity to membranes isolated from the free-living nematode Caenorhabditis elegans. Binding of avermectins is thought to modulate chloride channel activity, but the exact mechanism for anthelmintic activity remains to be de...

journal_title：Molecular pharmacology

authors： Arena JP,Liu KK,Paress PS,Cully DF

更新日期：1991-09-01 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 competitive antagonist alpha-conotoxin-MII (alpha-CTx-MII) is highly selective for the alpha3beta2 neuronal nicotinic receptor. Other receptor subunit combinations (alpha2beta2, alpha4beta2, alpha3beta4) are >200-fold less sensitive to blockade by this toxin. Using chimeric and mutant subunits, we identified amino...

journal_title：Molecular pharmacology

authors： Harvey SC,McIntosh JM,Cartier GE,Maddox FN,Luetje CW

更新日期：1997-02-01 00:00:00

abstract：:Binding by 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) to the Ah receptor leads to transcriptional activation of several genes and a toxicity syndrome that includes tumor promotion, wasting, hormonal and immune system dysfunction, and death. Recent findings indicate that TCDD may also affect cardiac function. Here, we ...

journal_title：Molecular pharmacology

authors： Canga L,Paroli L,Blanck TJ,Silver RB,Rifkind AB

更新日期：1993-12-01 00:00:00

abstract：:ATP-gated purinergic receptors (P2XRs) are a family of cation-permeable channels that conduct Ca(2+) and facilitate voltage-sensitive Ca(2+) entry in excitable cells. To study Ca(2+) signaling by P2XRs and its dependence on voltage-sensitive Ca(2+) influx, we expressed eight cloned P2XR subtypes individually in gonado...

journal_title：Molecular pharmacology

authors： Koshimizu TA,Van Goor F,Tomić M,Wong AO,Tanoue A,Tsujimoto G,Stojilkovic SS

更新日期：2000-11-01 00:00:00

abstract：:Voltage-gated sodium (Na(V)1) channels play a critical role in modulating the excitability of sensory neurons, and human genetic evidence points to Na(V)1.7 as an essential contributor to pain signaling. Human loss-of-function mutations in SCN9A, the gene encoding Na(V)1.7, cause channelopathy-associated indifference ...

journal_title：Molecular pharmacology

authors： Schmalhofer WA,Calhoun J,Burrows R,Bailey T,Kohler MG,Weinglass AB,Kaczorowski GJ,Garcia ML,Koltzenburg M,Priest BT

更新日期：2008-11-01 00:00:00

abstract：:Based on biochemical and ligand binding studies in various tissues and species, evidence for several alpha 2-adrenergic receptor subtypes has accumulated. The current alpha 2-adrenergic receptor classification (alpha 2A, alpha 2B, alpha 2C) is based exclusively on pharmacological criteria. The molecular cloning of thr...

journal_title：Molecular pharmacology

authors： Lorenz W,Lomasney JW,Collins S,Regan JW,Caron MG,Lefkowitz RJ

更新日期：1990-11-01 00:00:00

abstract：:NAD(P):quinone acceptor oxidoreductase (quinone reductase) (DT-diaphorase, EC 1.6.99.2) is involved in the process of reductive activation of cytotoxic antitumor quinones and nitrobenzenes. In this study, we initially examined the relative abilities of mouse, rat, and human quinone reductases to reduce two prodrugs, C...

journal_title：Molecular pharmacology

authors： Chen S,Knox R,Lewis AD,Friedlos F,Workman P,Deng PS,Fung M,Ebenstein D,Wu K,Tsai TM

更新日期：1995-05-01 00:00:00

abstract：:In previous studies, we have shown that mouse RAW 264.7 macrophages possess pyrimidinoceptors, coupled to a phosphoinositide-specific phospholipase C, with a higher specificity for UTP than for ATP. In the current study, we explored the mechanism involved in the UTP-induced intracellular acidification seen in this cel...

journal_title：Molecular pharmacology

authors： Lin WW,Chang SH,Wu ML

更新日期：1998-02-01 00:00:00

abstract：:The intracellular pathways taken by galactose-terminal glycoproteins were examined following endocytosis by the asialoglycoprotein receptor in monolayers of the human hepatoma cell line, Hep G2. In addition to a pathway leading to lysosomal degradation, single cohort kinetics revealed that up to 28% of surface-bound a...

journal_title：Molecular pharmacology

authors： Simmons CF Jr,Schwartz AL

更新日期：1984-11-01 00:00:00

abstract：:Despite some blockbuster G protein-coupled receptor (GPCR) drugs, only a small fraction (∼ 15%) of the more than 390 nonodorant GPCRs have been successfully targeted by the pharmaceutical industry. One way that this issue might be addressed is via translation of recent deorphanization programs that have opened the pro...

journal_title：Molecular pharmacology

authors： Bolognini D,Tobin AB,Milligan G,Moss CE

更新日期：2016-03-01 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：: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