当前位置： SCI文献检索 > MOLECULAR PHARMACOLOGY期刊下所有文献 > Subsecond modulation of formyl peptide-linked guanine nucleotide-binding proteins by guanosine 5'-O-(3-thio)triphosphate in permeabilized neutrophils.

Subsecond modulation of formyl peptide-linked guanine nucleotide-binding proteins by guanosine 5'-O-(3-thio)triphosphate in permeabilized neutrophils.

Abstract：

:Rapid activation of guanine nucleotide-binding protein (G protein)-mediated signal transduction mechanisms occurs in many tissues. The human neutrophil provides a useful model for studying the mechanisms of these fast processes. Fluorescent chemotactic tetrapeptide and pentapeptide exhibit 30-50% quenching of fluorescence upon binding to the neutrophil formyl peptide receptor, and their binding affinity is strongly regulated by the G protein Gi. We used rapid kinetic spectrofluorometric methods to study the assembly and disassembly of the ternary complex of ligand, receptor, and G protein in digitonin-permeabilized human neutrophils. Binding was studied up to 20 nM ligand, where the half-time for association was 1.2 sec. The rate constant of association was near that for diffusion-limited reactions of ligands and proteins, 2 x 10(7) M-1 sec-1. The rate of uncoupling of formyl peptide receptor from G protein in the presence of high concentrations of guanine nucleotide was > or = 5 sec-1 (i.e., t1/2 of 0.14 sec). Thus, disassembly of the formyl peptide receptor-G protein complex occurs in the millisecond time domain and may be faster than the next step in the signal transduction process.

journal_name

Mol Pharmacol

journal_title

Molecular pharmacology

authors

Neubig RR,Sklar LA

subject

Has Abstract

pub_date

1993-05-01 00:00:00

pages

734-40

issue

5

eissn

0026-895X

issn

1521-0111

journal_volume

43

pub_type

杂志文章

相关文献

MOLECULAR PHARMACOLOGY文献大全
  • [3H]ethylketocyclazocine binding to NCB-20 hybrid neurotumor cells.

    abstract：:Ethylketocyclazocine (EKC) binds to two sites on NCB-20 neuroblastoma X Chinese hamster brain hybrid cells (KDH = 2 nM, Bmax = 21,000 sites/cell; KDL = 27 nM, Bmax = 140,000 sites/cell. The high-affinity site has been characterized as a delta opiate receptor. The low-affinity site is relatively benzomorphan-specific; ...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：

    authors： West RE Jr,McLawhon RW,Dawson G,Miller RJ

    更新日期：1983-03-01 00:00:00

  • Cannabinol enhancement of interleukin-2 (IL-2) expression by T cells is associated with an increase in IL-2 distal nuclear factor of activated T cell activity.

    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

    pub_type： 杂志文章

    doi：10.1124/mol.61.2.446

    authors： Jan TR,Rao GK,Kaminski NE

    更新日期：2002-02-01 00:00:00

  • Alteration in accumulated aldosterone synthesis as a result of N-terminal cleavage of aldosterone synthase.

    abstract：:Aldosterone synthase (AS) regulates blood volume by synthesizing the mineralocorticoid aldosterone. Overproduction of aldosterone in the adrenal gland can lead to hypertension, a major cause of heart disease and stroke. Aldosterone production depends upon stimulation of AS expression by the renin-angiotensin system, w...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.111.076471

    authors： Adams BP,Bose HS

    更新日期：2012-03-01 00:00:00

  • Monod-Wyman-Changeux Allosteric Shift Analysis in Mutant α1β3γ2L GABAA Receptors Indicates Selectivity and Crosstalk among Intersubunit Transmembrane Anesthetic Sites.

    abstract：:Propofol, etomidate, and barbiturate anesthetics are allosteric coagonists at pentameric α1β3γ2 GABAA receptors, modulating channel activation via four biochemically established intersubunit transmembrane pockets. Etomidate selectively occupies the two β+/α- pockets, the barbiturate photolabel R-5-allyl-1-methyl-5-(m-...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.118.115048

    authors： Szabo A,Nourmahnad A,Halpin E,Forman SA

    更新日期：2019-04-01 00:00:00

  • Metabolism and mode of inhibition of varicella-zoster virus by L-beta-5-bromovinyl-(2-hydroxymethyl)-(1,3-dioxolanyl)uracil is dependent on viral thymidine kinase.

    abstract：:A nonnaturally occurring L-configuration nucleoside analog, L-beta-5-bromovinyl-(2-hydroxymethyl)-1,3-(dioxolanyl)uracil (L-BVOddU) selectively inhibited varicella-zoster virus growth in human embryonic lung (HEL) 299 cell culture with an EC(50) of 0.055 microM, whereas no inhibition of CEM and HEL 299 cell growth or ...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.58.5.1109

    authors： Li L,Dutschman GE,Gullen EA,Tsujii E,Grill SP,Choi Y,Chu CK,Cheng YC

    更新日期：2000-11-01 00:00:00

  • S-nitrosylating agents: a novel class of compounds that increase cystic fibrosis transmembrane conductance regulator expression and maturation in epithelial cells.

    abstract：:The endogenous bronchodilator, S-nitrosoglutathione (GSNO), increases expression, maturation, and function of both the wild-type and the DeltaF508 mutant of the cystic fibrosis transmembrane conductance regulatory protein (CFTR). Though transcriptional mechanisms of action have been identified, GSNO seems also to have...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.106.023242

    authors： Zaman K,Carraro S,Doherty J,Henderson EM,Lendermon E,Liu L,Verghese G,Zigler M,Ross M,Park E,Palmer LA,Doctor A,Stamler JS,Gaston B

    更新日期：2006-10-01 00:00:00

  • Expression of multiple forms of cytochrome P450 mRNAs in primary cultures of rat hepatocytes maintained on matrigel.

    abstract：:Freshly isolated rat hepatocytes rapidly lose their cytochrome P450 (P450) proteins and mRNAs, with no evidence of subsequent restoration, after placement into traditional systems of primary culture on type I collagen. We examined the patterns of expression of 10 constitutively expressed P450 mRNAs in rat hepatocytes ...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：

    authors： Kocarek TA,Schuetz EG,Guzelian PS

    更新日期：1993-03-01 00:00:00

  • Protection against toxic redox cycles between benzo(a)pyrene-3,6-quinone and its quinol by 3-methylcholanthrene-inducible formation of the quinol mono- and diglucuronide.

    abstract：:Cytotoxic effects of quinones are thought to be mediated by redox cycles between quinones and quinols whereby reactive oxygen species are generated. The role of glucuronidation in preventing these toxic redox cycles was investigated by using benzo(a)pyrene-3,6-quinone and isolated rat hepatocytes or Reuber hepatoma ce...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：

    authors： Lilienblum W,Bock-Hennig BS,Bock KW

    更新日期：1985-04-01 00:00:00

  • Modeling the effects of β1-adrenergic receptor blockers and polymorphisms on cardiac myocyte Ca2+ handling.

    abstract：:β-Adrenergic receptor blockers (β-blockers) are commonly used to treat heart failure, but the biologic mechanisms governing their efficacy are still poorly understood. The complexity of β-adrenergic signaling coupled with the influence of receptor polymorphisms makes it difficult to intuit the effect of β-blockers on ...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.113.090951

    authors： Amanfu RK,Saucerman JJ

    更新日期：2014-08-01 00:00:00

  • 14, 15-cis-episulfide-eicosatrienoic acid, an 'epoxygenase' eicosanoid analog, inhibits ionophore- but not thrombin-induced platelet aggregation.

    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

    pub_type： 杂志文章

    doi：

    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

  • Down-regulation and altered localization of gamma-catenin in cisplatin-resistant adenocarcinoma cells.

    abstract：:Resistance to cisplatin, one of the most widely used anticancer chemotherapeutic agents, is a major clinical problem. There is no effective way to predict development of cisplatin resistance in cancers. As determined by reverse transcription-polymerase chain reaction and Western blotting, the expression of gamma-caten...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.65.5.1217

    authors： Liang XJ,Shen DW,Gottesman MM

    更新日期：2004-05-01 00:00:00

  • Novel adamantane derivatives act as blockers of open ligand-gated channels and as anticonvulsants.

    abstract：:We examined the influence of the molecular structure of four novel adamantane derivatives on their ability to block the channels of nicotinic acetylcholine (ACh) and N-methyl-D-aspartate (NMDA) receptors. The structure of the drugs is Ad-CH2-N+H2-(CH2)5-R, where Ad is adamantane and R was varied from ammonium (IEM-175...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：

    authors： Antonov SM,Johnson JW,Lukomskaya NY,Potapyeva NN,Gmiro VE,Magazanik LG

    更新日期：1995-03-01 00:00:00

  • A novel metabotropic glutamate receptor 5 positive allosteric modulator acts at a unique site and confers stimulus bias to mGlu5 signaling.

    abstract：:Metabotropic glutamate receptor 5 (mGlu5) is a target for the treatment of central nervous system (CNS) disorders, such as schizophrenia and Alzheimer's disease. Furthermore, mGlu5 has been shown to play an important role in hippocampal synaptic plasticity, specifically in long-term depression (LTD) and long-term pote...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.112.082891

    authors： Noetzel MJ,Gregory KJ,Vinson PN,Manka JT,Stauffer SR,Lindsley CW,Niswender CM,Xiang Z,Conn PJ

    更新日期：2013-04-01 00:00:00

  • Positive cooperativity in the binding of alcuronium and N-methylscopolamine to muscarinic acetylcholine receptors.

    abstract：:The effect of the neuromuscular blocker alcuronium on the binding of N-[3H]-methylscopolamine [( 3H]NMS) and l-[3H]quinuclidinylbenzilate ([3H]QNB) to muscarinic binding sites in rat heart atria, longitudinal smooth muscle of the ileum, cerebral cortex, cerebellum, and submaxillary glands was measured using filtration...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：

    authors： Tucek S,Musílková J,Nedoma J,Proska J,Shelkovnikov S,Vorlícek J

    更新日期：1990-11-01 00:00:00

  • Evidence for a PCN-P450 enzyme in chickens and comparison of its development with that of other phenobarbital-inducible forms.

    abstract：:Of four monoclonal antibodies to purified rat liver cytochrome P450s, including those from 3-methylcholanthrene-, phenobarbital-, ethanol-, and pregnenolone-16-alpha-carbonitrile-treated rats, only the monoclonal antibody against pregnenolone-16-alpha-carbonitrile-inducible P450 immunodetected proteins in chicken live...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：

    authors： Lorr NA,Bloom SE,Park SS,Gelboin HV,Miller H,Friedman FK

    更新日期：1989-05-01 00:00:00

  • Structural domains of chimeric dopamine-noradrenaline human transporters involved in the Na(+)- and Cl(-)-dependence of dopamine transport.

    abstract：:Catecholamine transporters constitute the biological targets for several important drugs, including antidepressants, cocaine, and related compounds. Some information exists about discrete domains of these transporters that are involved in substrate translocation and uptake blockade, but delineation of domains mediatin...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.58.6.1404

    authors： Syringas M,Janin F,Mezghanni S,Giros B,Costentin J,Bonnet JJ

    更新日期：2000-12-01 00:00:00

  • Identification of transmembrane regions critical for ligand binding to the human D3 dopamine receptor using various D3/D1 transmembrane chimeras.

    abstract：:To investigate the roles of individual transmembrane segments (TM) of the human D3 dopamine receptor in its ligand-receptor interactions, we generated chimeric receptors in which its TMs were replaced, one at a time, partially or entirely, by the corresponding TM of the homologous human D1 receptor. Ligand binding pro...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.54.2.379

    authors： Alberts GL,Pregenzer JF,Im WB

    更新日期：1998-08-01 00:00:00

  • Role of human nucleoside transporters in the cellular uptake of two inhibitors of IMP dehydrogenase, tiazofurin and benzamide riboside.

    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

    pub_type： 杂志文章

    doi：10.1124/mol.104.004408

    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

  • Are alpha9alpha10 nicotinic acetylcholine receptors a pain target for alpha-conotoxins?

    abstract：:The synthetic alpha-conotoxin Vc1.1 is a small disulfide bonded peptide currently in development as a treatment for neuropathic pain. Unlike Vc1.1, the native post-translationally modified peptide vc1a does not act as an analgesic in vivo in rat models of neuropathic pain. It has recently been proposed that the primar...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.107.040568

    authors： Nevin ST,Clark RJ,Klimis H,Christie MJ,Craik DJ,Adams DJ

    更新日期：2007-12-01 00:00:00

  • Anti-HIV activity and resistance profile of the CXC chemokine receptor 4 antagonist POL3026.

    abstract：:We have studied the mechanism of action of Arg(*)-Arg-Nal(2)-Cys(1x)-Tyr-Gln-Lys-(d-Pro)-Pro-Tyr-Arg-Cit-Cys(1x)-Arg-Gly-(d-Pro)(*) (POL3026), a novel specific beta-hairpin mimetic CXC chemokine receptor (CXCR)4 antagonist. POL3026 specifically blocked the binding of anti-CXCR4 monoclonal antibody 12G5 and the intrace...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.107.042911

    authors： Moncunill G,Armand-Ugón M,Clotet-Codina I,Pauls E,Ballana E,Llano A,Romagnoli B,Vrijbloed JW,Gombert FO,Clotet B,De Marco S,Esté JA

    更新日期：2008-04-01 00:00:00

  • Ca2+ channels as integrators of G protein-mediated signaling in neurons.

    abstract：:The observations from Dunlap and Fischbach that transmitter-mediated shortening of the duration of action potentials could be caused by a decrease in calcium conductance led to numerous studies of the mechanisms of modulation of voltage-dependent calcium channels. Calcium channels are well known targets for inhibition...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章,评审

    doi：10.1124/mol.104.002261

    authors： Strock J,Diversé-Pierluissi MA

    更新日期：2004-11-01 00:00:00

  • Sazetidine-A is a potent and selective agonist at native and recombinant alpha 4 beta 2 nicotinic acetylcholine receptors.

    abstract：:Sazetidine-A has been recently proposed to be a "silent desensitizer" of alpha4beta2 nicotinic acetylcholine receptors (nAChRs), implying that it desensitizes alpha4beta2 nAChRs without first activating them. This unusual pharmacological property of sazetidine-A makes it, potentially, an excellent research tool to dis...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.108.045104

    authors： Zwart R,Carbone AL,Moroni M,Bermudez I,Mogg AJ,Folly EA,Broad LM,Williams AC,Zhang D,Ding C,Heinz BA,Sher E

    更新日期：2008-06-01 00:00:00

  • Modulators of CXCR4 and CXCR7/ACKR3 Function.

    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

    pub_type： 杂志文章,评审

    doi：10.1124/mol.119.117663

    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

  • Molecular basis of pimarane compounds as novel activators of large-conductance Ca(2+)-activated K(+) channel alpha-subunit.

    abstract：:Effects of pimaric acid (PiMA) and eight closely related compounds on large-conductance K(+) (BK) channels were examined using human embryonic kidney (HEK) 293 cells, in which either the alpha subunit of BK channel (HEKBKalpha) or both alpha and beta1 (HEKBKalphabeta1) subunits were heterologously expressed. Effects o...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.62.4.836

    authors： Imaizumi Y,Sakamoto K,Yamada A,Hotta A,Ohya S,Muraki K,Uchiyama M,Ohwada T

    更新日期：2002-10-01 00:00:00

  • Activation of trimeric P2X2 receptors by fewer than three ATP molecules.

    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

    pub_type： 杂志文章

    doi：10.1124/mol.112.080903

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

    更新日期：2012-10-01 00:00:00

  • Initiation of in vitro lipid peroxidation by N-hydroxynorcocaine and norcocaine nitroxide.

    abstract：:Norcocaine nitroxide and N-hydroxynorcocaine were found to stimulate hepatic microsomal lipid peroxidation in vitro, as measured by spin-trapping techniques using the spin trap alpha-[4-pyridyl-1-oxide]-N-tert-butylnitrone. It was determined that either norcocaine nitroxide or N-hydroxynorcocaine markedly enhanced the...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：

    authors： Rosen GM,Kloss MW,Rauckman EJ

    更新日期：1982-11-01 00:00:00

  • The human heart beta-adrenergic receptors. I. Heterogeneity of the binding sites: presence of 50% beta 1- and 50% beta 2-adrenergic receptors.

    abstract：:Beta-adrenergic receptors were characterized in a particulate fraction of human auricles obtained from patients operated upon for coronary insufficiency or valvular disease. [125I] Hydroxybenzylpindolol binding was evaluated in terms of kinetics; KD and Bmax values; and inhibition of binding in the presence of 10 micr...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：

    authors： Robberecht P,Delhaye M,Taton G,De Neef P,Waelbroeck M,De Smet JM,Leclerc JL,Chatelain P,Christophe J

    更新日期：1983-09-01 00:00:00

  • The Pharmacology and Function of Receptors for Short-Chain Fatty Acids.

    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

    pub_type： 杂志文章,评审

    doi：10.1124/mol.115.102301

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

    更新日期：2016-03-01 00:00:00

  • Sirtuin 1 Mediates the Actions of Peroxisome Proliferator-Activated Receptor δ on the Oxidized Low-Density Lipoprotein-Triggered Migration and Proliferation of Vascular Smooth Muscle Cells.

    abstract：:Peroxisome proliferator-activated receptor δ (PPARδ) has been implicated in vascular pathophysiology. However, its functions in atherogenic changes of the vascular wall have not been fully elucidated. PPARδ activated by GW501516 (2-[2-methyl-4-[[4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl]methylsulfanyl]ph...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.116.104679

    authors： Hwang JS,Ham SA,Yoo T,Lee WJ,Paek KS,Lee CH,Seo HG

    更新日期：2016-11-01 00:00:00

  • Molecular interactions underlying the unusually high adenosine affinity of a novel Trypanosoma brucei nucleoside transporter.

    abstract：:Trypanosoma brucei encodes a relatively high number of genes of the equilibrative nucleoside transporter (ENT) family. We report here the cloning and in-depth characterization of one T. brucei brucei ENT member, TbNT9/AT-D. This transporter was expressed in Saccharomyces cerevisiae and displayed a uniquely high affini...

    journal_title：Molecular pharmacology

    pub_type： 杂志文章

    doi：10.1124/mol.106.031559

    authors： Al-Salabi MI,Wallace LJ,Lüscher A,Mäser P,Candlish D,Rodenko B,Gould MK,Jabeen I,Ajith SN,de Koning HP

    更新日期：2007-03-01 00:00:00