Receptors & channels最新文献_第6页

Cellular signaling mechanisms for muscarinic acetylcholine receptors. 毒蕈碱乙酰胆碱受体的细胞信号传导机制。

Receptors & channels Pub Date : 2003-01-01 DOI: 10.3109/10606820308263

A. Lanzafame, A. Christopoulos, F. Mitchelson

{"title":"Cellular signaling mechanisms for muscarinic acetylcholine receptors.","authors":"A. Lanzafame, A. Christopoulos, F. Mitchelson","doi":"10.3109/10606820308263","DOIUrl":"https://doi.org/10.3109/10606820308263","url":null,"abstract":"Signaling pathways for muscarinic acetylcholine receptors (mAChRs) include several enzymes and ion channels. Recent studies have revealed the importance of various isoforms of both alpha and betagamma subunits of G proteins in initiation of signaling as well as the role of the small monomeric G protein, Rho, in the activation of phospholipase D. Modulation of adenylyl cyclase activity by mAChRs appears more diverse as the interaction of various receptor subtypes with the many isoforms of the enzyme are studied. Both alpha and beta subunits of G(i/o) may be involved. Some mAChR responses arise through release of nitric oxide from nitrergic nerves, including salivary gland secretion and hippocampal slow wave activity. mAChRs utilize a variety of intracellular pathways to activate various mitogen-activated protein kinases. The kinases are involved in cholinergic regulation of kidney epithelial function, catabolism of amyloid precursor protein, hippocampal long-term potentiation, activation of phospholipase A(2), and gene induction. mAChR activation can also stimulate or inhibit cellular growth and apoptosis, dependent on prior levels of cellular activity. Modulation of ion channels by mAChR agonists appears increasingly complex, based on recent studies. K(+) channels may be activated by M(2) and M(4) mAChR stimulation, although in the rat superior cervical ganglion topographical constraints appear to limit the effect to the M(2) mAChR. Another ganglionic K(+) current, the M current, is inhibited by M(1) mAChR activation, but in murine hippocampus inhibition involves another receptor subtype. R-type Ca(2+) channels are both facilitated and inhibited by M(1) and M(2) mAChRs; facilitation being more pronounced with activation of M(1) mAChRs and inhibition with M(2) mAChRs.","PeriodicalId":20928,"journal":{"name":"Receptors & channels","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2003-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87172823","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 69

Upscaling and Automation of Electrophysiology: Toward High Throughput Screening in Ion Channel Drug Discovery 电生理学的升级和自动化:迈向离子通道药物发现的高通量筛选

Receptors & channels Pub Date : 2003-01-01 DOI: 10.1080/10606820308258

M. Asmild, Nicholas Oswald, K. Krzywkowski, S. Friis, R. B. Jacobsen, Dirk Reuter, R. Taboryski, Jonathan Kutchinsky, R. Vestergaard, R. L. Schrøder, C. Sørensen, M. Bech, Mads P. G. Korsgaard, N. Willumsen

引用次数: 46

Cellular Signaling Mechanisms for Muscarinic Acetylcholine Receptors 毒蕈碱乙酰胆碱受体的细胞信号传导机制

Receptors & channels Pub Date : 2003-01-01 DOI: 10.1080/10606820308263

A. Lanzafame, A. Christopoulos, F. Mitchelson

{"title":"Cellular Signaling Mechanisms for Muscarinic Acetylcholine Receptors","authors":"A. Lanzafame, A. Christopoulos, F. Mitchelson","doi":"10.1080/10606820308263","DOIUrl":"https://doi.org/10.1080/10606820308263","url":null,"abstract":"Signaling pathways for muscarinic acetylcholine receptors (mAChRs) include several enzymes and ion channels. Recent studies have revealed the importance of various isoforms of both α and βγ subunits of G proteins in initiation of signaling as well as the role of the small monomeric G protein, Rho, in the activation of phospholipase D. Modulation of adenylyl cyclase activity by mAChRs appears more diverse as the interaction of various receptor subtypes with the many isoforms of the enzyme are studied. Both α and β subunits of Gi/o may be involved. Some mAChR responses arise through release of nitric oxide from nitrergic nerves, including salivary gland secretion and hippocampal slow wave activity. mAChRs utilize a variety of intracellular pathways to activate various mitogen-activated protein kinases. The kinases are involved in cholinergic regulation of kidney epithelial function, catabolism of amyloid precursor protein, hippocampal long-term potentiation, activation of phospholipase A2, and gene induction. mAChR activation can also stimulate or inhibit cellular growth and apoptosis, dependent on prior levels of cellular activity. Modulation of ion channels by mAChR agonists appears increasingly complex, based on recent studies. K + channels may be activated by M2 and M4 mAChR stimulation, although in the rat superior cervical ganglion topographical constraints appear to limit the effect to the M2 mAChR. Another ganglionic K + current, the M current, is inhibited by M1 mAChR activation, but in murine hippocampus inhibition involves another receptor subtype. R-type Ca 2+ channels are both facilitated and inhibited by M1 and M2 mAChRs; facilitation being more pronounced with activation of M1 mAChRs and inhibition with M2 mAChRs.","PeriodicalId":20928,"journal":{"name":"Receptors & channels","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2003-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78666165","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 88

Protein complexes involved in heptahelical receptor-mediated signal transduction. 参与七螺旋受体介导的信号转导的蛋白质复合物。

Receptors & channels Pub Date : 2003-01-01 DOI: 10.3109/10606820308243

R. V. Rebois, T. Hébert

引用次数: 92

Immunocytochemical study of alpha 1 and beta 2/3 subunits of GABAA receptors in freehand isolated vestibular Deiters' neurons. 手离体前庭Deiters神经元GABAA受体α 1和β 2/3亚基的免疫细胞化学研究

Receptors & channels Pub Date : 2003-01-01

Maria V Rapallino, Aroldo Cupello, Camilla Luccardini, Erica Nieddu, Andrea Seitun, Mauro Robello

{"title":"Immunocytochemical study of alpha 1 and beta 2/3 subunits of GABAA receptors in freehand isolated vestibular Deiters' neurons.","authors":"Maria V Rapallino, Aroldo Cupello, Camilla Luccardini, Erica Nieddu, Andrea Seitun, Mauro Robello","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Vestibular Deiters' neurons have been isolated from bovine brain by the Hydén's freehand dissection technique and challenged with monoclonal antibodies directed toward the alpha 1 and beta 2/3 subunits of the GABAA receptors. Subsequent challenge with fluorescent secondary antibodies and confocal microscopy allowed the study of the cellular distribution of such subunits. In Deiters' neurons the beta 2/3 subunit displayed a clear presence all along the cell body profile and the initial parts of the dendrites. The alpha 1 subunit was found highly present all over the cell interior except the nuclear profiles. The strong presence inside the cells possibly masked its presence on the plasma membrane. However, in part of the cells studied a distinct presence on the plasma membrane was evident. This subunit was visualized also all along the long dendrites of these neurons. The approach we describe here, involving freehand isolated mature neurons from adult animals, may allow a better characterization of the tridimensional distribution of different types of neuronal GABAA receptors in the respect of the approach with brain slices.</p>","PeriodicalId":20928,"journal":{"name":"Receptors & channels","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2003-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"22529264","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Disulfide bond structure and accessibility of cysteines in the ectodomain of the cholecystokinin receptor: specific mono-reactive receptor constructs examine charge-sensitivity of loop regions. 胆囊收缩素受体外域半胱氨酸的二硫键结构和可及性:特定的单反应性受体结构检查环路区域的电荷敏感性。

Receptors & channels Pub Date : 2003-01-01

Xi-Qin Ding, Vesile Dolu, Elizabeth M Hadac, Michael Schuetz, Laurence J Miller

引用次数: 0

Activity, regulation, and intracellular localization of RGS proteins. RGS蛋白的活性、调控和细胞内定位。

Receptors & channels Pub Date : 2003-01-01

Peter Chidiac, Anju A Roy

引用次数: 0

Pharmacological analysis of the contractile role of M2 and M3 muscarinic receptors in smooth muscle. 平滑肌中M2和M3毒蕈碱受体收缩作用的药理学分析。

Receptors & channels Pub Date : 2003-01-01 DOI: 10.3109/10606820308265

F. Ehlert

{"title":"Pharmacological analysis of the contractile role of M2 and M3 muscarinic receptors in smooth muscle.","authors":"F. Ehlert","doi":"10.3109/10606820308265","DOIUrl":"https://doi.org/10.3109/10606820308265","url":null,"abstract":"Muscarinic receptors expressed on smooth muscle cells are primarily of the M(2) and M(3) subtypes. The M(3) subtype triggers contraction through an interaction with G(q) proteins to stimulate phosphoinositide hydrolysis and mobilize Ca(2+). In contrast, activation of M(2) receptors modulates contraction by preventing relaxation or by potentiating M(3) receptor-mediated contractions, which enhances heterologous desensitization. These effects can be explained by the coupling of M(2) receptors to G(i) proteins that mediate an inhibition of adenylyl cyclase and calcium-activated potassium channels. The pharmacological antagonism of a response mediated through an interaction between M(2) and M(3) receptors has been shown to resemble the profile of the directly acting receptor (M(3)), primarily, and not that of the conditional receptor (M(2)). Evidence for a contractile role of the M(2) receptor has been obtained by inactivating its signaling pathway with pertussis toxin or by measuring contractile effects of muscarinic agonists after M(3) receptors have been covalently inactivated. Under these conditions, M(2) receptors have been shown to mediate an inhibition of the relaxant effects of agents, like isoproterenol, on the contractile effects of nonmuscarinic spasmogens. Muscarinic M(2) and M(3) receptor knockout mice are useful tools for exploring interactions between these receptors in smooth muscle.","PeriodicalId":20928,"journal":{"name":"Receptors & channels","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2003-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90622459","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 35

Disulfide bond structure and accessibility of cysteines in the ectodomain of the cholecystokinin receptor: specific mono-reactive receptor constructs examine charge-sensitivity of loop regions. 胆囊收缩素受体外域半胱氨酸的二硫键结构和可及性:特定的单反应性受体结构检查环路区域的电荷敏感性。

Receptors & channels Pub Date : 2003-01-01 DOI: 10.1080/10606820308249

Xi-Qin Ding, Vesile Dolu, E. Hadac, M. Schuetz, L. Miller

引用次数: 11

Development of a high-throughput viral-free assay for the measurement of CCR5-mediated HIV/cell fusion. 高通量无病毒检测ccr5介导的HIV/细胞融合的发展。

Receptors & channels Pub Date : 2003-01-01 DOI: 10.3109/10606820308248

S. Jenkinson, David C. McCoy, S. Kerner, R. Ferris, Wendell Lawrence, T. Fox, Chari D Smith

{"title":"Development of a high-throughput viral-free assay for the measurement of CCR5-mediated HIV/cell fusion.","authors":"S. Jenkinson, David C. McCoy, S. Kerner, R. Ferris, Wendell Lawrence, T. Fox, Chari D Smith","doi":"10.3109/10606820308248","DOIUrl":"https://doi.org/10.3109/10606820308248","url":null,"abstract":"M-tropic HIV strains gain access to their host cell via interaction of the viral envelope protein gp120 with the CCR5 coreceptor and CD4 located on the host cell. Inhibition of this event has been shown to reduce viral fusion and entry into cells in vitro. In the present study we describe the development of a novel cell/cell fusion assay that both mimics the viral/cell fusion process and allows quantification of this event. The assay has been characterized both biochemically, using selective antibodies, and pharmacologically, using selective CCR5 antagonists, and has been shown to be selective for examining the interaction of viral gp120 with hCCR5/hCD4. In addition, compound pIC50 data obtained from this cell/cell fusion assay correlates well (r2 = 0.7274) with data obtained from an HIV-1 replication assay. Furthermore, this assay has the added ability to simultaneously determine compound toxicity, thus allowing rapid determination of active, non-toxic compounds. In conclusion, the cell/cell fusion assay developed has been demonstrated to be a suitable surrogate assay that can be used to assess the effects of compounds on gp120/CCR5/CD4 mediated viral fusion into host cells.","PeriodicalId":20928,"journal":{"name":"Receptors & channels","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2003-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73840651","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 9