Monitoring Endogenous Gpcrs Lessons For Drug Design

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Monitoring Endogenous Gpcrs Lessons For Drug Design

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Author : Dominique Massotte
language : en
Publisher: Frontiers Media SA
Release Date : 2015-10-07

Monitoring Endogenous Gpcrs Lessons For Drug Design written by Dominique Massotte and has been published by Frontiers Media SA this book supported file pdf, txt, epub, kindle and other format this book has been release on 2015-10-07 with Science (General) categories.

G protein-coupled receptors (GPCRs) are integral membrane proteins forming the fourth largest superfamily in the human genome. Many of these receptors play key physiological roles and several pathologies have been associated with receptor functional abnormalities. GPCRs therefore represent important goals for drug design in pharmaceutical companies since they constitute the target of about one third of the drugs currently on the market. However, endogenous GPCRs are most often difficult to study because of a lack of tools to target them specifically and single out their response to physiological or drug-elicited stimulations. Hence, studies mostly focused on recombinant receptors expressed in a variety of cellular models that do not always closely reflect the receptor natural environment and often deal with levels of expression exceeding by far physiological ranges. Recent technological developments combining for example genetically modified animals and advanced imaging approaches have improved our ability to visualize endogenous GPCRs. To date, trailing receptor activation, subsequent intracellular redistribution, changes in signaling cascade up to integrated response to a drug-elicited stimulation is at hand though the impact of a physiological challenge on receptor dynamics remains a major issue. Data however suggest that the receptor may embrace a different fate depending on the type of stimulation in particular if sustained or repeated. This suggests that current drugs may only partially mimic the genuine response of the receptor and may explain, at least in part, their secondary effects. Commonalities and specificities between physiological and drug-induced activation can thus represent valuable guidelines for the design of future drugs.

Monitoring Endogenous Gpcrs Lessons For Drug Design

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Author :
language : en
Publisher:
Release Date : 2015

Monitoring Endogenous Gpcrs Lessons For Drug Design written by and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 2015 with categories.

G protein-coupled receptors (GPCRs) are integral membrane proteins forming the fourth largest superfamily in the human genome. Many of these receptors play key physiological roles and several pathologies have been associated with receptor functional abnormalities. GPCRs therefore represent important goals for drug design in pharmaceutical companies since they constitute the target of about one third of the drugs currently on the market. However, endogenous GPCRs are most often difficult to study because of a lack of tools to target them specifically and single out their response to physiological or drug-elicited stimulations. Hence, studies mostly focused on recombinant receptors expressed in a variety of cellular models that do not always closely reflect the receptor natural environment and often deal with levels of expression exceeding by far physiological ranges. Recent technological developments combining for example genetically modified animals and advanced imaging approaches have improved our ability to visualize endogenous GPCRs. To date, trailing receptor activation, subsequent intracellular redistribution, changes in signaling cascade up to integrated response to a drug-elicited stimulation is at hand though the impact of a physiological challenge on receptor dynamics remains a major issue. Data however suggest that the receptor may embrace a different fate depending on the type of stimulation in particular if sustained or repeated. This suggests that current drugs may only partially mimic the genuine response of the receptor and may explain, at least in part, their secondary effects. Commonalities and specificities between physiological and drug-induced activation can thus represent valuable guidelines for the design of future drugs.

Label Free Technologies For Drug Discovery

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Author : Matthew Cooper
language : en
Publisher: John Wiley & Sons
Release Date : 2011-02-11

Label Free Technologies For Drug Discovery written by Matthew Cooper and has been published by John Wiley & Sons this book supported file pdf, txt, epub, kindle and other format this book has been release on 2011-02-11 with Medical categories.

Over the past two decades the benefits of label-free biosensor analysis have begun to make an impact in the market, and systems are beginning to be used as mainstream research tools in many drug discovery laboratories. Label-Free Technologies For Drug Discovery summarises the latest and emerging developments in label-free detection systems, their underlying technology principles and end-user case studies that reveal the power and limitations of label-free in all areas of drug discovery. Label-free technologies discussed include SPR, NMR, high-throughput mass spectrometry, resonant waveguide plate-based screening, transmitted-light imaging, isothermal titration calorimetry, optical and impedance cell-based assays and other biophysical methods. The technologies are discussed in relation to their use as screening technologies, high-content technologies, hit finding and hit validation strategies, mode of action and ADME/T, access to difficult target classes, cell-based receptor/ligand interactions particularly orphan receptors, and antibody and small molecule affinity and kinetic analysis. Label-Free Technologies For Drug Discovery is an essential guide to this emerging class of tools for researchers in drug discovery and development, particularly high-throughput screening and compound profiling teams, medicinal chemists, structural biologists, assay developers, ADME/T specialists, and others interested in biomolecular interaction analysis.

Biophysical Techniques In Drug Discovery

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Author : Angeles Canales
language : en
Publisher: Royal Society of Chemistry
Release Date : 2017-11-14

Biophysical Techniques In Drug Discovery written by Angeles Canales and has been published by Royal Society of Chemistry this book supported file pdf, txt, epub, kindle and other format this book has been release on 2017-11-14 with Science categories.

Biophysical techniques are used in many key stages of the drug discovery process including in screening for new receptor ligands, in characterising drug mechanisms, and in validating data from biochemical and cellular assays. This book provides an overview of the biophysical methods applied in drug discovery today, including traditional techniques and newer developments. Perspectives from academia and industry across a spectrum of techniques are brought together in a single volume. Small and biotherapeutic approaches are covered and strengths and limitations of each technique are presented. Case studies illustrate the application of each technique in real applied examples. Finally, the book covers recent developments in areas such as electron microscopy with discussions of their possible impact on future drug discovery. This is a go-to volume for biophysicists, analytical chemists and medicinal chemists providing a broad overview of techniques of contemporary interest in drug discovery.

Handbook Of Drug Screening

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Author : Ramakrishna Seethala
language : en
Publisher: CRC Press
Release Date : 2016-04-19

Handbook Of Drug Screening written by Ramakrishna Seethala and has been published by CRC Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2016-04-19 with Medical categories.

Building upon the foundation of basics discussed in the previous edition, the Second Edition provides a more in-depth look at the latest methods and technologies of advanced drug screening, an essential function of drug discovery. With extensively updated content and 21 new chapters, this text examines:quality and efficiency of drug target validati

Advances In Combinatorial Chemistry High Throughput Screening

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Author : Rathnam Chaguturu
language : en
Publisher: Bentham Science Publishers
Release Date : 2013-08-06

Advances In Combinatorial Chemistry High Throughput Screening written by Rathnam Chaguturu and has been published by Bentham Science Publishers this book supported file pdf, txt, epub, kindle and other format this book has been release on 2013-08-06 with Science categories.

Advances in Combinatorial Chemistry & High Throughput Screening, is an e-book series comprising updated research articles previously published in the impact factor journal, Combinatorial Chemistry & High Throughput Screening (CCHTS). A wide range of topics are covered by these articles including chemical biology, high throughput screening, combinatorial chemistry, chemoinformatics, laboratory automation and compound management. This series is, therefore, a testament to CCHTS contributions in advancing drug discovery on full throttle. This eBook series opens up a new avenue for rapid access for readers – including academic researchers and industry professionals - to a focused collection of highly regarded contributions in the field.

Exploiting Chemical Diversity For Drug Discovery

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Author : Paul A Bartlett
language : en
Publisher: Royal Society of Chemistry
Release Date : 2007-10-31

Exploiting Chemical Diversity For Drug Discovery written by Paul A Bartlett and has been published by Royal Society of Chemistry this book supported file pdf, txt, epub, kindle and other format this book has been release on 2007-10-31 with Science categories.

Conceptual and technological advances in chemistry and biology have transformed the drug discovery process. Evolutionary pressure among the diverse scientific and engineering disciplines that contribute to the identification of biologically active compounds has resulted in synergistic improvements at every step in the process. Exploiting Chemical Diversity for Drug Discovery encompasses the many components of this transformation and presents the current state-of-the-art of this critical endeavour. From the theoretical and operational considerations in generating a collection of compounds to screen, to the design and implementation of high-capacity and high-quality assays that provide the most useful biological information, this book provides a comprehensive overview of modern approaches to lead identification. Beginning with an introductory overview, subsequent chapters address topics that include the design of chemical libraries and methods for optimizing their diversity; automated and accelerated chemistry; high throughput assay design and detection techniques; and strategies for data analysis and property optimization. Written by experts in the field, both academic and industrial, and illustrated in full colour, this book provides an excellent overview for current practitioners and will also serve as a stimulating resource for future generations. Researchers in organic and medicinal chemistry, the biological and pharmacological sciences, as well as those interested in allied computational and engineering disciplines will value the comprehensive and up-to-date coverage.

Functional Protein Microarrays In Drug Discovery

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Author : Paul F. Predki
language : en
Publisher: CRC Press
Release Date : 2007-03-30

Functional Protein Microarrays In Drug Discovery written by Paul F. Predki and has been published by CRC Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2007-03-30 with Medical categories.

An ideal text for biotechnologists, protein chemists, and biochemists, Functional Protein Microarrays in Drug Discovery explores all aspects of functional protein microarrays, including basic principles, methods, and applications. The book discusses the generation of functional protein content and describes both standard and state-of-the-art fabrication methods. It reviews current and next generation approaches to assay detection and presents a wide range of applications, from biomolecular interaction discovery and characterization to immune response profiling. The book also addresses several fundamental computational issues, bioinformatics and data analysis.

G Protein Coupled Receptors

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Author :
language : en
Publisher: Academic Press
Release Date : 2016-02-26

G Protein Coupled Receptors written by and has been published by Academic Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2016-02-26 with Science categories.

G-Protein-Coupled Receptors: Signaling, Trafficking, and Regulation, a new volume in the Methods in Cell Biology series continues the legacy of this premier serial with quality chapters authored by leaders in the field. This volume covers research methods in G-Protein-Coupled Receptors, and includes sections on such topics signaling, trafficking and regulation. - Covers the increasingly appreciated cell biology field of G-protein-coupled receptors - Includes both established and new technologies - Contributed by experts in the field - Covers topics such as signaling, trafficking, and regulation

Label Free Biosensors

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Author : Matthew A. Cooper
language : en
Publisher: Cambridge University Press
Release Date : 2009-02-02

Label Free Biosensors written by Matthew A. Cooper and has been published by Cambridge University Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2009-02-02 with Science categories.

Label-free biosensors are devices that use biological or chemical receptors to detect analytes (molecules) in a sample. They give detailed information on the selectivity, affinity, and, in many cases, also the binding kinetics and thermodynamics of an interaction. Although they can be powerful tools in the hands of a skilled user, there is often a lack of knowledge of the best methods for using label-free assays to screen for biologically active molecules and accurately and precisely characterize molecular recognition events. This book reviews both established and newer label-free techniques giving both the expert user and the general reader interested in the technologies and applications behind label-free an insight into the field from expert opinion leaders and practitioners of the technologies. Most importantly, chapters contain worked examples from leaders in the field that take the reader through the basics of experimental design, setup, assay development, and data analysis.