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G Protein-Coupled Receptors as Drug Targets: Analysis of Activation and Constitutive Activity
eBook Publisher: John Wiley & Sons
Imprint: Wiley-VCH
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With its particular emphasis on the constitutive activity of G-protein-coupled receptors (GPCRs)s, this book comprehensively discusses an important biological process that has not yet been covered in such depth in any other existing books on GPCRs. The international team of highly distinguished authors addresses in detail current models and concepts, to introduce medicinal chemists, physiologists, pharmacologists, and medical researchers into the advances in the understanding of GPCR activation and constitutive activity. In addition, the book provides an overview on methods of investigating constitutive GPCR activity. The text is well illustrated by selected experimental data and schemes._The chaptes are all cross-referenced with each other and cover general mechnisms, methodological approaches and cover selected important GPCR sysstems, the consequences for drug action, including, side effects, and rational drug design for GPCR targets. A highly recommended reference for researchers in academia and industry.
authors addresses in detail current models and concepts, so as to introduce pharmaceutical chemists, physiologists and medical researchers to the advances in the understanding of GPCR activation and constitutive activity, and provides an overview of the methods of investigating GPCR activity. The text is backed by abundant case studies and methodological advice for analyzing GPCRs, covering selected pharmacologically relevant GPCR systems, the consequences for drug action, including unwanted side effects, and rational drug design for GPCR targets.
A highly practical reference for researchers in academia and industry.
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| Title of eBook: G Protein-Coupled Receptors as Drug Targets: Analysis of Activation and Constitutive Activity | |
| Release Date: 06-27-2006 | |
| Publisher: Wiley-VCH |
This eBook download is available in the following formats:
| Parent title | G Protein-Coupled Receptors as Drug... |
|---|---|
| Encrypted (DRM) | Yes |
| SKU | 9783527606955 |
| File size | 2679 |
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| Note | Excellent navigation features are available via Adobe such as bookmarks and a quick access table of contents. Text search is easily accessible. An Adobe DRM-protected file is different than a pdf file in that it uses Adobe DRM (Digital Rights Management) technology, which authors and publishers use to protect their content from illegal online distribution and to set certain privileges such as restrictions on copying and printing. |
G Protein-Coupled Receptors as Drug Targets: Analysis of Activation and Constitutive Activity
Chapter One
Historical Background and IntroductionRichard A. Bond and Robert J. Lefkowitz
Paul Ehrlich (1854-1915) and John Newport Langley (1854-1936) are generally credited with the introduction of the concept of receptors or receptive substances to describe the interaction of drugs with cells. A few years later, Alfred J. Clarke (1885-1941) began the process of applying mathematical modeling to the ligand/receptor interaction, and could thus be said to be the father of modern receptor theory. Receptor theory was then modified and expanded by others: Ariens' concept of partial agonists, Stephenson's seminal paper on efficacy, and Furchgott's modification of Stephenson's theory to produce the system-independent concept of intrinsic efficacy. (For a detailed account of the evolution of receptor theory and references see Kenakin, 2004.) These developments, along with other contributions such as the Schild regression analysis, had receptor theory firmly established by the 1960s.
However, the theory was still very much based on the 'black box' concept; many scientists were still highly dubious that receptors existed as distinct proteins or entities. By the 1980s, new discoveries had begun to change the 'black box' concept. One was the cloning of receptors and another was the clear separation of ion channel receptors from receptors coupled to the newly discovered G proteins (initially also referred to as N-proteins, as an acronym for nucleotide-binding proteins). The discovery of G proteins also produced a modification of receptor theory to include pre-coupled receptors in what is now termed the ternary complex model. Thanks to technolo
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