標(biāo)題: Titlebook: G Protein-Coupled Receptors in Drug Discovery; Wayne R. Leifert Book 2009 Humana Press 2009 Calcium.Cellular signalling.Chemokine.Drug dev [打印本頁(yè)] 作者: Inoculare 時(shí)間: 2025-3-21 19:15
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書(shū)目名稱G Protein-Coupled Receptors in Drug Discovery讀者反饋學(xué)科排名
作者: Dictation 時(shí)間: 2025-3-21 23:38 作者: Tortuous 時(shí)間: 2025-3-22 01:12 作者: 襲擊 時(shí)間: 2025-3-22 05:12 作者: 評(píng)論性 時(shí)間: 2025-3-22 11:35
Margret Liehn,Hannelore Schlautmanncular targets was elucidated. Over the years, this family of proteins has become more important in the understanding and treatment of different human pathologies, representing today close to 30% of the molecular targets of all marketed drugs. The sequencing of the human genome unveiled the existence作者: GRAIN 時(shí)間: 2025-3-22 16:18
Margret Liehn,Hannelore Schlautmannon (FDA)-approved drugs. Consequently, there are a wide variety of . plate-based screening technologies that enable the measurement of compound affinity, potency, and efficacy for almost every type of GPCR. However, to maximize success it is prudent to ensure that (i) the most suitable assay formats作者: GRAIN 時(shí)間: 2025-3-22 18:45
,Versuche über Lochleibungsdruck,ial role in drug discovery today. Classically, a number of drugs based on GPCRs have been developed for such different indications as cardiovascular, metabolic, neurodegenerative, psychiatric, and oncologic diseases. Owing to the restricted structural information on GPCRs, only limited exploration o作者: obstinate 時(shí)間: 2025-3-22 22:17
Conference proceedings 1986Latest edition discovery. Yet, little is known about the specific interactions between GPCRs and G proteins. For a better perspective on the ternary complex dynamics, we adapted a β.-adrenergic receptor(β.AR)–tetGs. reconstitution system and found evidence that for efficient coupling of the β.AR to Gs does not re作者: FLAGR 時(shí)間: 2025-3-23 03:00
,Jernej Lorenci: “People Are the Key”,ew results and decisions based on them. The simple data summaries are the basis for all composite assay and screening data quality measures, for example, the signal-to-noise ratio, signal-to-background ratio, assay and screening window coefficients . and ., or strictly standardized mean difference (作者: 草率女 時(shí)間: 2025-3-23 09:17 作者: Intuitive 時(shí)間: 2025-3-23 11:14
Wandel in Patientengut und Therapiekonzeptenpression system produces high yields of functional receptor, is able to perform post-translational modifications, and is readily adaptable to large-scale culture. Here, we describe the generic methods for expressing a GPCR using baculovirus-infected insect cells, including the maintenance of insect 作者: Cholagogue 時(shí)間: 2025-3-23 16:37
https://doi.org/10.1007/978-3-322-83139-2-coupled receptors in vascular smooth muscle. AngII receptors are therefore an important target in patients with high blood pressure. Strategies to lower high blood pressure (hypertension) include the use of drugs that compete for AngII at the angiotensin II Type 1 receptors (ATR) using ATR antagoni作者: Delectable 時(shí)間: 2025-3-23 18:23 作者: 釘牢 時(shí)間: 2025-3-24 00:22
https://doi.org/10.1007/978-981-13-8106-5ir receptors have been implicated in several disease processes, particularly inflammatory and autoimmune disorders and cancer, and are therefore attractive targets for drug development. Chemokine receptors are members of the seven-transmembrane, G protein-coupled receptor (GPCR) family. As such they作者: 種屬關(guān)系 時(shí)間: 2025-3-24 04:20 作者: 純樸 時(shí)間: 2025-3-24 08:45
Matthias C. Angermeyer,Holger Steinbergdrugs targeted at GPCRs are marketed in virtually every therapeutic area. GPCRs can be classified by virtue of their coupling to second messenger signaling systems. In the last decade functional evaluation of Gαq-coupled GPCRs has been enabled by advances in fluorescence dye-based methodologies and 作者: Boycott 時(shí)間: 2025-3-24 11:34
Thomas Wiedenhorn,Ursula Pfeiffer-Blattnerlls. They are easily, inexpensively, and rapidly generated and provide a versatile solution for G protein-coupled receptor (GPCR) cell-based assay development. Using BacMam technology, target gene expression levels are easily controlled and simultaneous delivery of multiple genes is possible, for ex作者: 雄辯 時(shí)間: 2025-3-24 15:32
,Sensationen durch ?Medien-Mathematik?,ed as an experimental system for ligand identification and for characterizing receptor pharmacology and signal transduction mechanisms. A number of groups have developed yeast strains using various modifications to this signaling pathway, especially manipulation of the G protein alpha subunit Gpa1p,作者: 雕鏤 時(shí)間: 2025-3-24 22:59
,Die Ann?herung an potenzielle Kunden,through multiple assay steps, and amenability to a microplate format for screening are core requirements for the practical large-scale implementation of microarray technology. G protein-coupled receptor (GPCR) microarrays require the co-immobilization of the receptors and their associated lipid memb作者: Ascendancy 時(shí)間: 2025-3-25 00:26
200 Tipps für Verk?ufer im Au?endienstto a point-of-contact readout and as a consequence are mostly pathway biased. Recently, we have developed label-free optical biosensor cellular assays that are capable of examining systems cell biology of endogenous receptors and systems cell pharmacology of GPCR ligands in both physiologically and 作者: 過(guò)濾 時(shí)間: 2025-3-25 05:42 作者: 不容置疑 時(shí)間: 2025-3-25 09:47 作者: convert 時(shí)間: 2025-3-25 15:27
1064-3745 e for cell-based GPCR screening written by leading researcheThe G protein-coupled receptors (GPCRs) and associated peripheral G proteins underpin a multitude of physiological processes. The GPCRs represent one of the largest superfamilies in the human genome and are a significant target for bioactiv作者: 主動(dòng)脈 時(shí)間: 2025-3-25 19:11 作者: alliance 時(shí)間: 2025-3-25 20:32
20. H?mophilie-Symposion Hamburg 1989enous assay systems can be used to monitor the signaling cascades of GPCRs. This chapter details the authors’ collective experience of using the DiscoverX Hit Hunter cAMPII kit from GE Healthcare/DiscoverX Corporation for the direct quantification of cAMP levels in Gs and Gi GPCRs.作者: fetter 時(shí)間: 2025-3-26 01:40
,Psychopharmaka — ja oder nein?,ique targeted therapeutic uses, including “designer” drugs such as allosteric regulators, inverse agonists, and drugs targeting hetero-oligomeric complexes. This has been facilitated by the development of new screening technologies to identify novel drugs against both known and orphan GPCRs.作者: 嘮叨 時(shí)間: 2025-3-26 06:39
,Versuche über Lochleibungsdruck,f structure-based drug design has been possible. Much effort has been dedicated to structural biology on GPCRs and very recently an X-ray structure of the β2-adrenergic receptor was obtained. This breakthrough will certainly increase the efforts in structural biology on GPCRs and furthermore speed up and facilitate the drug discovery process.作者: 朋黨派系 時(shí)間: 2025-3-26 08:40 作者: optional 時(shí)間: 2025-3-26 15:35 作者: Hormones 時(shí)間: 2025-3-26 19:42
Thomas Wiedenhorn,Ursula Pfeiffer-Blattnerample, coexpression of a receptor and a G protein or a reporter gene. BacMam viruses are compatible with the GPCR cell-based assay formats typically used in high-throughput screening and provide an unparalleled level of experimental flexibility that is simply not possible when using stable recombinant cell lines.作者: 格言 時(shí)間: 2025-3-26 23:20 作者: 舉止粗野的人 時(shí)間: 2025-3-27 02:56 作者: 創(chuàng)作 時(shí)間: 2025-3-27 08:27
New Insights into GPCR Function: Implications for HTS,ique targeted therapeutic uses, including “designer” drugs such as allosteric regulators, inverse agonists, and drugs targeting hetero-oligomeric complexes. This has been facilitated by the development of new screening technologies to identify novel drugs against both known and orphan GPCRs.作者: 滔滔不絕地說(shuō) 時(shí)間: 2025-3-27 09:26
An Overview on GPCRs and Drug Discovery: Structure-Based Drug Design and Structural Biology on GPCRf structure-based drug design has been possible. Much effort has been dedicated to structural biology on GPCRs and very recently an X-ray structure of the β2-adrenergic receptor was obtained. This breakthrough will certainly increase the efforts in structural biology on GPCRs and furthermore speed up and facilitate the drug discovery process.作者: Prognosis 時(shí)間: 2025-3-27 16:02 作者: cipher 時(shí)間: 2025-3-27 20:33 作者: 航海太平洋 時(shí)間: 2025-3-27 23:53
BacMam: Versatile Gene Delivery Technology for GPCR Assays,ample, coexpression of a receptor and a G protein or a reporter gene. BacMam viruses are compatible with the GPCR cell-based assay formats typically used in high-throughput screening and provide an unparalleled level of experimental flexibility that is simply not possible when using stable recombinant cell lines.作者: 新陳代謝 時(shí)間: 2025-3-28 03:58 作者: 籠子 時(shí)間: 2025-3-28 08:17
Resonant Waveguide Grating Biosensor for Whole-Cell GPCR Assays,disease relevant environments. We have shown that these biosensor assays enable high-throughput screening of pathway-biased ligands acting on endogenous β.-adrenergic receptor in cells. These biosensor cellular assays hold the potential to reduce attrition rates in drug discovery and development process.作者: 泰然自若 時(shí)間: 2025-3-28 11:17 作者: 無(wú)情 時(shí)間: 2025-3-28 17:02
,Understanding the Ligand–Receptor–G Protein Ternary Complex for GPCR Drug Discovery, protein activation by using β.AR receptor–tetGs. system . at the close proximity of the receptor may constitute a simple screening system that avoids false positives and potentially adapted to screen drugs for other GPCRs.作者: 微生物 時(shí)間: 2025-3-28 20:12 作者: 確定無(wú)疑 時(shí)間: 2025-3-29 00:27
Margret Liehn,Hannelore Schlautmanneffects. To achieve this, an understanding of the pathways and mechanisms of receptor activation relevant to the disease mechanism, as well as the benefits and/or limitations of the specific techniques, is key.作者: 未開(kāi)化 時(shí)間: 2025-3-29 03:47
Wandel in Patientengut und Therapiekonzeptenults demonstrate that expressed receptor could be detected and quantified using radiolabeled ligand binding, that expression was maximal at approximately 72?h post-infection, and that expression levels could be altered by addition of various ligands to cultures of infected insect cells.作者: Instinctive 時(shí)間: 2025-3-29 10:04
200 Years of Ricardian Trade Theorytly less making them obtainable even for academic groups. Here, we present a protocol for measuring changes in intracellular calcium levels in living mammalian cells based on the fluorescent calcium binding dye, fluo-4.作者: Mumble 時(shí)間: 2025-3-29 14:16
GPCR Signaling: Understanding the Pathway to Successful Drug Discovery,effects. To achieve this, an understanding of the pathways and mechanisms of receptor activation relevant to the disease mechanism, as well as the benefits and/or limitations of the specific techniques, is key.作者: Inculcate 時(shí)間: 2025-3-29 16:30
GPCR Expression Using Baculovirus-Infected ,9 Cells,ults demonstrate that expressed receptor could be detected and quantified using radiolabeled ligand binding, that expression was maximal at approximately 72?h post-infection, and that expression levels could be altered by addition of various ligands to cultures of infected insect cells.作者: Precursor 時(shí)間: 2025-3-29 21:26 作者: Anterior 時(shí)間: 2025-3-30 02:05 作者: Congestion 時(shí)間: 2025-3-30 06:05
Use of the DiscoveRx Hithunter cAMPII Assay for Direct Measurement of cAMP in Gs and Gi GPCRs,enous assay systems can be used to monitor the signaling cascades of GPCRs. This chapter details the authors’ collective experience of using the DiscoverX Hit Hunter cAMPII kit from GE Healthcare/DiscoverX Corporation for the direct quantification of cAMP levels in Gs and Gi GPCRs.作者: Notify 時(shí)間: 2025-3-30 09:13 作者: Nebulizer 時(shí)間: 2025-3-30 14:15 作者: 厚顏 時(shí)間: 2025-3-30 18:42 作者: ALIEN 時(shí)間: 2025-3-30 21:51 作者: guardianship 時(shí)間: 2025-3-31 01:03 作者: 灰心喪氣 時(shí)間: 2025-3-31 08:13 作者: 疏遠(yuǎn)天際 時(shí)間: 2025-3-31 10:05
Homology Modeling of GPCRs,this number may grow with the refinement of a number of different genomes. However, despite recent efforts in the crystallization of these proteins, homology modeling approaches are becoming widely used as a method for obtaining quantitative and qualitative information for structure-based drug desig作者: Firefly 時(shí)間: 2025-3-31 17:09
GPCR Expression Using Baculovirus-Infected ,9 Cells,pression system produces high yields of functional receptor, is able to perform post-translational modifications, and is readily adaptable to large-scale culture. Here, we describe the generic methods for expressing a GPCR using baculovirus-infected insect cells, including the maintenance of insect 作者: 延期 時(shí)間: 2025-3-31 19:12 作者: 行為 時(shí)間: 2025-3-31 23:21 作者: 讓空氣進(jìn)入 時(shí)間: 2025-4-1 02:49
A Time-Resolved Fluorescent Lanthanide (Eu)-GTP Binding Assay for Chemokine Receptors as Targets inir receptors have been implicated in several disease processes, particularly inflammatory and autoimmune disorders and cancer, and are therefore attractive targets for drug development. Chemokine receptors are members of the seven-transmembrane, G protein-coupled receptor (GPCR) family. As such they作者: thalamus 時(shí)間: 2025-4-1 07:10
Use of the DiscoveRx Hithunter cAMPII Assay for Direct Measurement of cAMP in Gs and Gi GPCRs,n be employed to detect agonists (inverse, partial, and full) in addition to allosteric and classical orthosteric antagonists. Several different homogenous assay systems can be used to monitor the signaling cascades of GPCRs. This chapter details the authors’ collective experience of using the Disco作者: 祖?zhèn)髫?cái)產(chǎn) 時(shí)間: 2025-4-1 13:47
