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Targeting Ion Channels for Drug Discovery: Emerging Challenges for High Throughput Screening Technologies

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Release : 2024-06-07
Genre : Science
Kind : eBook
Book Rating : 169/5 ( reviews)

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Book Synopsis Targeting Ion Channels for Drug Discovery: Emerging Challenges for High Throughput Screening Technologies by : Ciria Hernandez

Download or read book Targeting Ion Channels for Drug Discovery: Emerging Challenges for High Throughput Screening Technologies written by Ciria Hernandez. This book was released on 2024-06-07. Available in PDF, EPUB and Kindle. Book excerpt: Ligand and voltage-gated ion channels are highly regulated protein molecules that cross the cell membrane allowing ion flow from one side of the membrane to the other. They are ubiquitously expressed in human tissues and consist of one of the largest and best understood functional groups of proteins, with more than 400 members spanning nearly 1% of the human genome. They are involved in a variety of fundamental physiological processes, and their malfunction causes numerous diseases. In terms of the challenges faced in the effort to discover specific drugs in ancient and emerging diseases, ion channels are the third-largest class of target proteins after G-protein-coupled receptors (GPCRs) and kinases. 15% of small molecule drug targets have been reported to be voltage- or ligand-gated ion channels, resulting in approximately 150 new drug candidates in preclinical and clinical studies. Of the ion channel targeting drugs found on the market, these were identified more than a decade ago, and many of the current studies are at various stages of scientific approval. Overcoming these challenges has led the field of ion channel drug discovery to transform over the past 15 years through major advancements in genetic target detection, validation, structure-based drug design, and drug modeling of cell-based diseases.

Ion channel screening: advances in technologies and analysis

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Kind : eBook
Book Rating : 358/5 ( reviews)

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Book Synopsis Ion channel screening: advances in technologies and analysis by : Ralf F. Kettenhofen

Download or read book Ion channel screening: advances in technologies and analysis written by Ralf F. Kettenhofen. This book was released on . Available in PDF, EPUB and Kindle. Book excerpt: Ion channel research has increased tremendously in the past 35 years since the first publication of the patch clamp technique by Neher and Sakmann in 1976. This is documented by the rising number of publications listed in Pubmed (http://www.ncbi.nlm.nih.gov/pubmed) including the keyword ‘ion channel’ from just 186 hits in 1976 to almost 180,000 hits today. Ion channels attract this great interest due to their pivotal role in the control of fundamental physiological processes in a plethora of different tissues. Moreover, their importance in a wide range of inherited and drug-induced pathologies spanning all major therapeutic areas makes them attractive targets for pharmacological drug screening and potential risk factors when assessing drug safety (Ashcroft, 2006; Clare, 2010; Dunlop 2008; Milligan 2009). Several methods and technologies have been developed to meet the analytical needs for studying ion channels. These approaches have addressed ion channel function directly as well as in the context of the cell and tissue. Scaling of these technologies has allowed ion channel analysis to be carried out on high throughput and high content assay systems. In this Research Topic we want to provide an up-to-date collection of the latest developments and improvements in ion channel screening; defining the cutting edge and indicating further developments required in the future.

Ion Channel Drug Discovery

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Release : 2014-09-03
Genre : Science
Kind : eBook
Book Rating : 085/5 ( reviews)

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Book Synopsis Ion Channel Drug Discovery by : Brian Cox

Download or read book Ion Channel Drug Discovery written by Brian Cox. This book was released on 2014-09-03. Available in PDF, EPUB and Kindle. Book excerpt: Ion channel drug discovery is a rapidly evolving field fuelled by recent, but significant, advances in our understanding of ion channel function combined with enabling technologies such as automated electrophysiology. The resurgent interest in this target class by both pharmaceutical and academic scientists was clearly highlighted by the over-subscribed RSC/BPS 'Ion Channels as Therapeutic Targets' symposium in February 2009. This book builds on the platform created by that meeting, covering themes including advances in screening technology, ion channel structure and modelling and up-to-date case histories of the discovery of modulators of a range of channels, both voltage-gated and non-voltage-gated channels. The editors have built an extensive network of contacts in the field through their first-hand scientific experience, collaborations and conference participation and the organisation of the meeting at Novartis, Horsham, increased the network enabling the editors to draw on the experience of eminent researchers in the field. Interest and investment in ion channel modulation in both industrial and academic settings continues to grow as new therapeutic opportunities are identified and realised for ion channel modulation. This book provides a reference text by covering a combination of recent advances in the field, from technological and medicinal chemistry perspectives, as well as providing an introduction to the new 'ion channel drug discoverer'. The book has contributions from highly respected academic researchers, industrial researchers at the cutting edge of drug discovery and experts in enabling technology. This combination provides a complete picture of the field of interest to a wide range of readers.

Advances in Ion Channel Drug Discovery

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Release : 2012
Genre :
Kind : eBook
Book Rating : /5 ( reviews)

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Book Synopsis Advances in Ion Channel Drug Discovery by : Wilma Keighley

Download or read book Advances in Ion Channel Drug Discovery written by Wilma Keighley. This book was released on 2012. Available in PDF, EPUB and Kindle. Book excerpt: Advances in target validation, screening technologies, and discovery of new ion channel families combine to enable the investigation and commercialization of this largely unexploited target family with potential in a range of major therapeutic areas.

Label-Free Technologies For Drug Discovery

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Release : 2011-02-11
Genre : Medical
Kind : eBook
Book Rating : 270/5 ( reviews)

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Book Synopsis Label-Free Technologies For Drug Discovery by : Matthew Cooper

Download or read book Label-Free Technologies For Drug Discovery written by Matthew Cooper. This book was released on 2011-02-11. Available in PDF, EPUB and Kindle. Book excerpt: 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.

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