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.

TRP Channels as Therapeutic Targets, Second Edition is a comprehensive reference on the roles of TRP Channels in health and disease states. The Editor lined up a team of worldwide experts in academia and corporate R&D to provide diverse views into these promising drug development targets. Following the research development happened in the past ten years, since the first edition published, the revision includes seven new chapters. All remaining chapters are completely updated. New topics included in the book are TRP channels biology, the crystalline structure of TRP channels, targeting TRP channels for pain relief, the relationship with migraine, emerging pain targets, a comprehensive view of the role of TRP channels in respiratory diseases and COVID complications, anxiety relief, renal disease, arthritis, and therapeutic opportunities for thermal regulation. TRP Channels as Therapeutic Targets, Second Edition is a reference for broad segments of the scientific and medical community. Researchers working on TRP channel drug discovery will benefit from the overview of applications to conditions in specific organ systems. Clinicians interested in new drugs in the pipeline, will find in this book their biologic principles of action. - Presents the perspectives of several life science research specialties on the topic - Provides a comprehensive picture of the TRP field, from TRP channel dysfunction through TRP drug discovery and development to clinical trials and everyday medical practice - Represents an updated and complete reference

Comprehensive Medicinal Chemistry III, Eight Volume Set provides a contemporary and forward-looking critical analysis and summary of recent developments, emerging trends, and recently identified new areas where medicinal chemistry is having an impact. The discipline of medicinal chemistry continues to evolve as it adapts to new opportunities and strives to solve new challenges. These include drug targeting, biomolecular therapeutics, development of chemical biology tools, data collection and analysis, in silico models as predictors for biological properties, identification and validation of new targets, approaches to quantify target engagement, new methods for synthesis of drug candidates such as green chemistry, development of novel scaffolds for drug discovery, and the role of regulatory agencies in drug discovery. Reviews the strategies, technologies, principles, and applications of modern medicinal chemistry Provides a global and current perspective of today's drug discovery process and discusses the major therapeutic classes and targets Includes a unique collection of case studies and personal assays reviewing the discovery and development of key drugs

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.

Edited by the most prominent person in the field and top researchers at US pharmaceutical companies, this is a unique resource for drug developers and physiologists seeking a molecular-level understanding of ion channel pharmacology. After an introduction to the topic, the authors evaluate the structure and function of ion channels, as well as related drug interaction. A section on assay technologies is followed by a section each on calcium, sodium and potassium channels. Further chapters cover genetic and acquired channelopathies, before the book closes with a look at safety issues in ion channel drug development. For medicinal and pharmaceutical chemists, biochemists, molecular biologists and those working in the pharmaceutical industry.

Backed by leading authorities, this is a professional guide to successful compound screening in pharmaceutical research and chemical biology, including the chemoinformatic tools needed for correct data evaluation. Chapter authors from leading pharmaceutical companies as well as from Harvard University discuss such factors as chemical genetics, binding, cell-based and biochemical assays, the efficient use of compound libraries and data mining using cell-based assay results. For both academics and professionals in the pharma and biotech industries working on small molecule screening.

This new handbook covers the world of biophotonics not only geographically -- with the editors coming from different continents -- but also in terms of content, since the authors come from the whole spectrum of biophotonic basic and applied research. Designed to set the standard for the scientific community, these three volumes break new ground by providing readers with the physics basics as well as the biological and medical background, together with detailed reports on recent technical advances. The Handbook also adopts an application-related approach, starting with the application and then citing the various tools to solve the scientific task, making it of particular value to medical doctors. Divided into several sections, the first part offers introductory chapters on the different fields of research, with subsequent parts focusing on the applications and techniques in various fields of industry and research. The result is a handy source for scientists seeking the basics in a condensed form, and equally a reference for quickly gathering the knowledge from neighboring disciplines. Absolutely invaluable for biophotonic scientists in their daily work.

A presentation of screening techniques, modern technologies, and high-capacity instrumentation for increased productivity in the development and discovery of new drugs, chemical compounds, and targeted delivery of pharmaceuticals. It contains practical applications and examples of strategies in cell-based and cell-free screens as well as homogeneous, fluorescence, chemiluminescence, and radioactive-based technologies.

The New Benchmark for Understanding the Latest Developments of Ion ChannelsIon channels control the electrical properties of neurons and cardiac cells, mediate the detection and response to sensory stimuli, and regulate the response to physical stimuli. They can often interact with the cellular environment due to their location at the surface of ce

Ion channels are proteins that make pores in the membranes of excitable cells present both in the brain and the body. These cells are not only responsible for converting chemical and mechanical stimuli into the electrical signals but are also liable for monitoring vital functions. All our activities, from the blinking of our eyes to the beating of our heart and all our senses from smell to sight, touch, taste and hearing are regulated by the ion channels. This book will take us on an expedition describing the role of ion channels in congenital and acquired diseases and the challenges and limitations scientist are facing in the development of drugs targeting these membrane proteins.