GPCRs

GPCRs PDF Author: Beata Jastrzebska
Publisher: Academic Press
ISBN: 9780128162286
Category : Science
Languages : en
Pages : 0

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Book Description
GPCRS: Structure, Function, and Drug Discovery provides a comprehensive overview of recent discoveries and our current understanding of GPCR structure, signaling, physiology, pharmacology and methods of study. In addition to the fundamental aspects of GPCR function and dynamics, international experts discuss crystal structures, GPCR complexes with partner proteins, GPCR allosteric modulation, biased signaling through protein partners, deorphanization of GPCRs, and novel GPCR-targeting ligands that could lead to the development of new therapeutics against human diseases. GPCR association with, and possible therapeutic pathways for, retinal degenerative diseases, Alzheimer's disease, Parkinson's disease, cancer and diabetic nephropathy, among other illnesses, are examined in-depth.

GPCRs

GPCRs PDF Author: Beata Jastrzebska
Publisher: Academic Press
ISBN: 9780128162286
Category : Science
Languages : en
Pages : 0

Get Book Here

Book Description
GPCRS: Structure, Function, and Drug Discovery provides a comprehensive overview of recent discoveries and our current understanding of GPCR structure, signaling, physiology, pharmacology and methods of study. In addition to the fundamental aspects of GPCR function and dynamics, international experts discuss crystal structures, GPCR complexes with partner proteins, GPCR allosteric modulation, biased signaling through protein partners, deorphanization of GPCRs, and novel GPCR-targeting ligands that could lead to the development of new therapeutics against human diseases. GPCR association with, and possible therapeutic pathways for, retinal degenerative diseases, Alzheimer's disease, Parkinson's disease, cancer and diabetic nephropathy, among other illnesses, are examined in-depth.

GPCR Signalling Complexes – Synthesis, Assembly, Trafficking and Specificity

GPCR Signalling Complexes – Synthesis, Assembly, Trafficking and Specificity PDF Author: Denis J. Dupré
Publisher: Springer Science & Business Media
ISBN: 9400747659
Category : Medical
Languages : en
Pages : 298

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Book Description
Main Question: G protein coupled receptors are involved in highly efficient and specific activation of signalling pathways. How do GPCR signalling complexes get assembled to generate such specificity? In order to answer this question, we need to understand how receptors and their signalling partners are synthesized, folded and quality-controlled in order to generate functional proteins. Then, we need to understand how each partner of the signalling complex is selected to join a complex, and what makes this assembly possible. GPCRs are known to be able to function as oligomers, what drives the assembly into oligomers and what will be the effects of such organization on specificity and efficacy of signal transduction. Once the receptor complexes are assembled, they need to reach different locations in the cell; what drives and controls the trafficking of GPCR signalling complexes. Finally, defects in synthesis, maturation or trafficking can alter functionality of GPCRs signalling complexes; how can we manipulate the system to make it function normally again? Pharmacological chaperones may just be part of the answer to this question.

Research and Trends in Data Mining Technologies and Applications

Research and Trends in Data Mining Technologies and Applications PDF Author: Taniar, David
Publisher: IGI Global
ISBN: 1599042738
Category : Computers
Languages : en
Pages : 350

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Book Description
Activities in data warehousing and mining are constantly emerging. Data mining methods, algorithms, online analytical processes, data mart and practical issues consistently evolve, providing a challenge for professionals in the field. Research and Trends in Data Mining Technologies and Applications focuses on the integration between the fields of data warehousing and data mining, with emphasis on the applicability to real-world problems. This book provides an international perspective, highlighting solutions to some of researchers' toughest challenges. Developments in the knowledge discovery process, data models, structures, and design serve as answers and solutions to these emerging challenges.

G Protein-Coupled Receptors in Drug Discovery

G Protein-Coupled Receptors in Drug Discovery PDF Author: Wayne R. Leifert
Publisher: Humana Press
ISBN: 9781603273169
Category : Medical
Languages : en
Pages : 0

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Book Description
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. Thegeneralaimofthisbookistoprovideresearcherswitharangeofprotocolsthatmay be useful in their GPCR drug discovery programs. It is also the basis for the devel- ment of future assays in this field. Therefore, the range of topics covered and the appropriate methodological approaches in GPCR drug discovery are reflected in this book. Itisinterestingtonotethatfuturedirectionsindrugdiscoverywillrequireinput and collaboration from a plethora of fields of research. As such, this book will likely be of interest to scientists involved in such fields as molecular biology, pharmacology, biochemistry, cellular signaling, and bio-nanotechnology.

GPCR Molecular Pharmacology and Drug Targeting

GPCR Molecular Pharmacology and Drug Targeting PDF Author: Annette Gilchrist
Publisher: John Wiley & Sons
ISBN: 1118035178
Category : Medical
Languages : en
Pages : 675

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Book Description
G protein-coupled receptors (GPCRs) are a large protein family of transmembrane receptors vital in dictating cellular responses. GPCRs are involved in many diseases, but are also the target of around half of all modern medicinal drugs. Shifting Paradigms in G Protein Coupled Receptors takes a look at the way GPCRs are examined today, how they react, how their mutations lead to disease, and the many ways in which they can be screened for compounds that modulate them. Chemists, pharmacologists, and biologists will find essential information in this comprehensive reference.

Physics, Pharmacology and Physiology for Anaesthetists

Physics, Pharmacology and Physiology for Anaesthetists PDF Author: Matthew E. Cross
Publisher: Cambridge University Press
ISBN: 1107615887
Category : Medical
Languages : en
Pages : 439

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Book Description
A quick reference to basic science for anaesthetists, containing all the key information needed for FRCA exams.

Protein Allostery in Drug Discovery

Protein Allostery in Drug Discovery PDF Author: Jian Zhang
Publisher: Springer Nature
ISBN: 9811387192
Category : Medical
Languages : en
Pages : 386

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Book Description
The book focuses on protein allostery in drug discovery. Allosteric regulation, ʹthe second secret of lifeʹ, fine-tunes virtually most biological processes and controls physiological activities. Allostery can both cause human diseases and contribute to development of new therapeutics. Allosteric drugs exhibit unparalleled advantages compared to conventional orthosteric drugs, rendering the development of allosteric modulators as an appealing strategy to improve selectivity and pharmacodynamic properties in drug leads. The Series delineates the immense significance of protein allostery—as demonstrated by recent advances in the repertoires of the concept, its mechanistic mechanisms, and networks, characteristics of allosteric proteins, modulators, and sites, development of computational and experimental methods to predict allosteric sites, small-molecule allosteric modulators of protein kinases and G-protein coupled receptors, engineering allostery, and the underlying role of allostery in precise medicine. Comprehensive understanding of protein allostery is expected to guide the rational design of allosteric drugs for the treatment of human diseases. The book would be useful for scientists and students in the field of protein science and Pharmacology etc.

The G Protein-Coupled Receptors Handbook

The G Protein-Coupled Receptors Handbook PDF Author: Lakshmi A. Devi
Publisher: Springer Science & Business Media
ISBN: 1592599192
Category : Medical
Languages : en
Pages : 414

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Book Description
A comprehensive survey of the many recent advances in the field of G protein-coupled receptors (GPCR). The authors describe the current knowledge of GPCR receptor structure and function, the different mechanisms involved in the regulation of GPCR function, and the role of pharmacological chaperones in GPCR folding and maturation. They also present new findings about how GPCR dimerization/oligomerization modifies the properties of individual receptors and show how recent developments are leading to significant advances in drug discovery, such as the detection of ligands for orphan GPCRs. Also discussed are the most recent developments that could lead to new drug discoveries: the role of GPCRs in mediating pain, the development of receptor-type selective drugs based on the structural plasticity of receptor activation, and the identification of natural ligands of orphan GPCRs (deorphanization) as possible drug targets.

G Protein-Coupled Receptor Screening Assays

G Protein-Coupled Receptor Screening Assays PDF Author: Duarte Miguel F. Prazeres
Publisher: Humana
ISBN: 9781493955800
Category : Medical
Languages : en
Pages : 0

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Book Description
This volume explores the considerable efforts that have been directed towards the development of G Protein-Coupled Receptors (GPCR) screening assays in order to disclose GPCR acting compounds, elucidate signaling mechanisms or evaluate compound’s efficacy. New discoveries in the field, along with the widely recognized need for better and safer pharmaceutical drugs constitute the main motivation for this book. Readers, both beginners and experienced researchers, will receive an updated overview of not only the established, but also the innovative technologies that promise to advance GPCR drug research. This book is organized into two major parts: the introductory part discusses the necessary foundations for the understanding of GPCR action and the rationale behind the design of the available screening assays; and part two provides detailed protocols for different screening approaches. Written in the highly successful Methods in Molecular Biology series format, the chapters include the kind of detailed description and implementation advice that is crucial for getting optimal results in the laboratory. Practical and innovative, G Protein-Coupled Receptor Screening Assays: Methods and Protocols reaches out to everyone involved in the discovery of GPCR-active drugs, and provides a transversal overview of the different levels of GPCR signaling addressable in the different screening strategies and presents practical examples of how current assay technologies are contributing to new paradigms in GPCR drug research.

G Protein-Coupled Receptors in Immune Response and Regulation

G Protein-Coupled Receptors in Immune Response and Regulation PDF Author:
Publisher: Academic Press
ISBN: 0128124040
Category : Science
Languages : en
Pages : 400

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Book Description
G Protein-Coupled Receptors in Immune Response and Regulation, Volume 136 presents emerging concepts related to the role of GPCRs in immune response and regulation. Users will find updated chapters on a variety of topics, including Beta-adrenergic signaling in the onset and progression of asthma, the Emerging roles of Regulators of G protein signaling (RGS) proteins in the immune system, information on Kinin receptors in immune response and pathogenic infections, and sections on GPCR signaling in C. elegans and its implications in immune response, GPCR Kinases in Inflammatory response and signaling, and GRK2 in Inflammation: Regulation of T cell receptors and IgE signaling. Chapters in this book discuss not only the well-known aspects of GPCR signaling in immunology, but also presents many emerging paradigms that have not yet been reported in classical textbooks. Each chapter presents a forward-looking discussion, providing a glimpse of the tremendous potential associated with the specific receptor systems discussed. - Brings together contributions from leading experts in the area of GPCR biology - Discusses current paradigms and the future potential of understanding GPCR signaling in immune response and regulation - Presents the first of its kind book to focus on specific GPCR systems in various aspects of immunology, all brought together in one volume