Phosphatidylinositol-4,5-bisphosphate: actin dynamics and the regulation of ATP-dependent and -independent secretion.

abstract：:Pregnanolone [5 beta-pregnan-3 alpha-ol-20-one (5 beta 3 alpha)] and allopregnanolone [5 alpha-pregnan-3 alpha-ol-20-one (5 alpha 3 alpha)] are neuroactive steroids that are reduced metabolites of progesterone. Both 5 beta 3 alpha and 5 alpha 3 alpha are potent positive modulators of the gamma-aminobutyric acid respon...

journal_title：Molecular pharmacology

authors： Friedman L,Gibbs TT,Farb DH

更新日期：1993-07-01 00:00:00

abstract：:DNA topoisomerases are the molecular targets of a range of anticancer and antimicrobial therapeutics. Many of these drugs act by converting their target enzyme to a DNA-damaging agent through the trapping of the covalent enzyme/DNA intermediate. This drug-mediated trapping of the intermediate is reversible, and the le...

journal_title：Molecular pharmacology

authors： Nitiss JL,Wang JC

更新日期：1996-11-01 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：:Current evidence suggests that DNA fragmentation plays an integral role in mediating cytotoxicity that results from thymidine nucleotide depletion ("thymineless death"). Recently, Ayusawa et al. [Mutat. Res. 200:221-230 (1988)] reported that dTMP starvation induces cellular processes that result in the release of 50-2...

journal_title：Molecular pharmacology

authors： Dusenbury CE,Davis MA,Lawrence TS,Maybaum J

更新日期：1991-03-01 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：: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 present study was conducted to establish a pharmacological method of controlling growth of vascular smooth muscle cells (VSMC) by blocking calcium entry. In cultured rat VSMC, 1 nM platelet-derived growth factor (PDGF) induced a biphasic elevation of cytoplasmic free calcium concentration, ([Ca2+]c). The second su...

journal_title：Molecular pharmacology

authors： Nie L,Mogami H,Kanzaki M,Shibata H,Kojima I

更新日期：1996-10-01 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：:Isoproterenol increases and decreases contractile force at low and high concentrations, respectively, through beta(2)-adrenoceptors overexpressed in transgenic mouse heart (TG4), consistent with activation of both G(s) and G(i) proteins. Using TG4 hearts, we demonstrated that epinephrine behaves like isoproterenol, bu...

journal_title：Molecular pharmacology

authors： Heubach JF,Ravens U,Kaumann AJ

更新日期：2004-05-01 00:00:00

abstract：:The effects of saturating concentrations of DDT [1,1,1-trichloro-2,2-bis(p-chlorophenyl)ethane] and the pyrethroid insecticides cismethrin and deltamethrin on alkaloid-dependent activation of the voltage-sensitive sodium channel were studied using measurements of 22Na+ uptake into mouse brain synaptosomes. In survey e...

journal_title：Molecular pharmacology

authors： Bloomquist JR,Soderlund DM

更新日期：1988-05-01 00:00:00

abstract：:TWIK-related K(+) 1 (TREK1) potassium channels are members of the two-pore domain potassium channel family and contribute to background potassium conductances in many cell types, where their activity can be regulated by a variety of physiologic and pharmacologic mediators. Fenamates such as FFA (flufenamic acid; 2-{[3...

journal_title：Molecular pharmacology

authors： Veale EL,Al-Moubarak E,Bajaria N,Omoto K,Cao L,Tucker SJ,Stevens EB,Mathie A

更新日期：2014-05-01 00:00:00

abstract：:A collection of analogues of atrial natriuretic peptide (ANP) were screened for their ability to inhibit ANP-induced cGMP stimulation. The antagonists revealed through this screen are structurally related; almost all are substituted at either aspartate-13 or phenylalanine-26. This tendency is consistent throughout sev...

journal_title：Molecular pharmacology

authors： von Geldern TW,Budzik GP,Dillon TP,Holleman WH,Holst MA,Kiso Y,Novosad EI,Opgenorth TJ,Rockway TW,Thomas AM

更新日期：1990-12-01 00:00:00

abstract：:The ATP signaling mechanism in neuroblastoma x glioma hybrid NG108-15 cells differentiated by exposure to dibutyryl-cAMP was characterized. In cells loaded with fura-2, ATP rapidly raised the cytosolic Ca2+ concentration ([Ca2+]i); the magnitude of the rise was inversely proportional to the extracellular Na+ concentra...

journal_title：Molecular pharmacology

authors： Chueh SH,Hsu LS,Song SL

更新日期：1994-03-01 00:00:00

abstract：:Capsaicin (vanilloid) sensitivity has long served as the functional signature of a subset of nociceptive sensory neurons. Mutagenesis studies have revealed seemingly distinct regions involved in mediating ligand binding and channel activation at the capsaicin binding site. Residue 547 (transmembrane region 4) mediates...

journal_title：Molecular pharmacology

authors： Johnson DM,Garrett EM,Rutter R,Bonnert TP,Gao YD,Middleton RE,Sutton KG

更新日期：2006-09-01 00:00:00

abstract：:At central excitatory synapses, the transient elevation of intracellular calcium reduces N-methyl-D-aspartate (NMDA) receptor activity. Such 'calcium-dependent inactivation' is mediated by interactions of calcium/calmodulin and alpha-actinin with the C terminus of NMDA receptor 1 (NR1) subunit. However, inactivation i...

journal_title：Molecular pharmacology

authors： Vissel B,Krupp JJ,Heinemann SF,Westbrook GL

更新日期：2002-03-01 00:00:00

abstract：:The effects of 5-hydroxytryptamine (5-HT)2A receptor activation on cAMP formation were studied in a cell line derived from embryonic rat cortex (A1A1). 5-HT (EC50 = 0.87 microM) amplified the amount of cAMP formed in response to 5'-N-ethylcarboxamidoadenosine (an adenosine A2 receptor agonist), cholera toxin, and fors...

journal_title：Molecular pharmacology

authors： Berg KA,Clarke WP,Chen Y,Ebersole BJ,McKay RD,Maayani S

更新日期：1994-05-01 00:00:00

abstract：:P2X receptors are trimeric membrane proteins. When they bind extracellular ATP, a conformational change occurs that opens a transmembrane ion channel. The ATP-binding pocket is formed in a cleft between two subunits, and a critical amino acid residue for ATP contact is Lys⁶⁹ (P2X2 numbering). In the present work, we s...

journal_title：Molecular pharmacology

authors： Stelmashenko O,Lalo U,Yang Y,Bragg L,North RA,Compan V

更新日期：2012-10-01 00:00:00

abstract：:Proliferation of activated T cells and CD56 bright natural killer (Cytokine Growth Factor Rev 13:169-183, 1995) cells caused by interleukin-2 (IL-2) has been exploited in IL-2-based therapies for the treatment of metastatic renal cell carcinoma and melanoma (J Clin Oncol 13:688-696, 1995; J Clin Oncol 17: 2105-2116, 1...

journal_title：Molecular pharmacology

authors： Rao BM,Driver I,Lauffenburger DA,Wittrup KD

更新日期：2004-10-01 00:00:00

abstract：:The role of mitogen-activated protein kinase signaling and the transcription factor c-Jun in epidermal growth factor (EGF)-induced expression of 12-lipoxygenase in human epidermoid carcinoma A431 cells was studied. EGF increased the activation of extracellular signal-regulated kinase (ERK) and c-Jun amino terminal kin...

journal_title：Molecular pharmacology

authors： Chen BK,Kung HC,Tsai TY,Chang WC

更新日期：2000-01-01 00:00:00

abstract：:Immune-mediated drug hypersensitivity reactions (IDHRs) represent a significant problem due to their unpredictable and severe nature, as well as the lack of understanding of the pathogenesis. Sulfamethoxazole (SMX), a widely used antibiotic, has been used as a model compound to investigate the underlying mechanism of ...

journal_title：Molecular pharmacology

authors： Cheng L,Stewart BJ,You Q,Petersen DR,Ware JA,Piccotti JR,Kawabata TT,Ju C

更新日期：2008-06-01 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：:The two G protein-coupled receptors (GPCRs) C-X-C chemokine receptor type 4 (CXCR4) and atypical chemokine receptor 3 (ACKR3) are part of the class A chemokine GPCR family and represent important drug targets for human immunodeficiency virus (HIV) infection, cancer, and inflammation diseases. CXCR4 is one of only thre...

journal_title：Molecular pharmacology

authors： Adlere I,Caspar B,Arimont M,Dekkers S,Visser K,Stuijt J,de Graaf C,Stocks M,Kellam B,Briddon S,Wijtmans M,de Esch I,Hill S,Leurs R

更新日期：2019-12-01 00:00:00

abstract：:n-Dodecylguanidine (C12-G) is an amphipathic compound with a guanidine moiety, which is positively charged at physiological pH, and a hydrophobic side chain. Its effects on an A-type K+ channel clone (rKv1.4) expressed in Xenopus oocytes were examined. C12-G caused a concentration-dependent (1-20 microM) positive shif...

journal_title：Molecular pharmacology

authors： Yao JA,Saxena NC,Ziai MR,Ling S,Tseng GN

更新日期：1995-07-01 00:00:00

abstract：:Two human ovarian cancer cell lines were established from a patient before (PEO1) and after (PEO4) the onset of resistance to 5-fluorouracil (5-FU)/cisplatin-based chemotherapy. Using growth inhibition assays, we determined that the PEO4 line was almost 5-fold more resistant to 5-FU than the PEO1 line. The addition of...

journal_title：Molecular pharmacology

authors： Chu E,Lai GM,Zinn S,Allegra CJ

更新日期：1990-09-01 00:00:00

abstract：:The rat mu-opioid receptor clone in which novel exon 5 was found in the place of exon 4 (MOR-1B) was one of the first MOR-1 variants described. We now have identified the mouse homolog of the rat MOR-1B as well as four additional variants derived from splicing from exon 3 into different sites within exon 5. The sequen...

journal_title：Molecular pharmacology

authors： Pan YX,Xu J,Bolan E,Moskowitz HS,Xu M,Pasternak GW

更新日期：2005-09-01 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：:Combinations of coimmunoprecipitation, single-cell fluorescence resonance energy transfer, and cell-surface time-resolved fluorescence resonance energy transfer demonstrated protein-protein interactions and quaternary structure for the alpha(1b)-adrenoceptor. Self-association of transmembrane domain 1 and its interact...

journal_title：Molecular pharmacology

authors： Carrillo JJ,López-Giménez JF,Milligan G

更新日期：2004-11-01 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：:Our previous studies suggested that the dNTP/dNDP transporter systems that exist in mitochondria for transporting dNTP/dNDP from the cytoplasm to the mitochondria for mitochondrial DNA (mtDNA) synthesis play a critical role in delayed cytotoxicity of anti-human immunodeficiency virus (HIV) dideoxynucleoside analogs in...

journal_title：Molecular pharmacology

authors： Lam W,Chen C,Ruan S,Leung CH,Cheng YC

更新日期：2005-02-01 00:00:00

abstract：:We examined the effects on allosteric modulation and ligand binding of the mutation of amino acid residues of the human A(3) adenosine receptor (A(3)AR) that are hypothesized to be near one of three loci: the putative sodium binding site, the putative ligand binding site, and the DRY motif in transmembrane helical dom...

journal_title：Molecular pharmacology

authors： Gao ZG,Kim SK,Gross AS,Chen A,Blaustein JB,Jacobson KA

更新日期：2003-05-01 00:00:00