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Titlebook: G Protein-Coupled Receptors in Drug Discovery; Wayne R. Leifert Book 2009 Humana Press 2009 Calcium.Cellular signalling.Chemokine.Drug dev

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书目名称G Protein-Coupled Receptors in Drug Discovery
编辑Wayne R. Leifert
视频video
概述Contains several comprehensive reviews of GPCR screening technologies by authoritative leaders.Provides an easily accessible reference volume for cell-based GPCR screening written by leading researche
丛书名称Methods in Molecular Biology
图书封面Titlebook: G Protein-Coupled Receptors in Drug Discovery;  Wayne R. Leifert Book 2009 Humana Press 2009 Calcium.Cellular signalling.Chemokine.Drug dev
描述The 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 bioactive and drug discovery programs. It is estimated that greater than 50% of all drugs, including those in development, currently target GPCRs. Many of the characterized GPCRs have known ligands; however, approximately 20% of GPCRs are described as orphan GPCRs, apparent GPCRs that share the generic high-level structure charact- istic of GPCRs but whose endogenous ligand is not known. Therefore, it is expected that the field of GPCR drug discovery and development will greatly expand in the coming years with emphasis on new generations of drugs against GPCRs with unique therapeuticuseswhichmayincludedrugssuchasallostericregulators,inverseagonists, and identification of orphan GPCR ligands. AswelearnmoreaboutthemolecularsignalingcascadesfollowingGPCRactivation, we acquire a better appreciation of the complexity of cell signaling and as a result, also acquire a vast array ofnew molecularmethods toinvestigate these andother processes. Thegeneralaimofthisb
出版日期Book 2009
关键词Calcium; Cellular signalling; Chemokine; Drug development; GPCRs; Ligands; physiology
版次1
doihttps://doi.org/10.1007/978-1-60327-317-6
isbn_softcover978-1-4939-5706-4
isbn_ebook978-1-60327-317-6Series ISSN 1064-3745 Series E-ISSN 1940-6029
issn_series 1064-3745
copyrightHumana Press 2009
The information of publication is updating

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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
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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
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,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
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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
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,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 (
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