Download or read book A Functional Selectivity Mechanism at the Serotonin 2A GPCR Involves Ligand dependent Conformations of Intracellular Loop 2 written by and published by . This book was released on 2014 with total page 11 pages. Available in PDF, EPUB and Kindle. Book excerpt: With recent progress in determination of G protein-coupled receptor (GPCR) structure with crystallography, a variety of other experimental approaches (e.g., NMR spectroscopy, fluorescent-based assays, mass spectrometry techniques) are also being used to characterize state-specific and ligand-specific conformational states. MD simulations offer a powerful complementary approach to elucidate the dynamic features associated with ligand-specific GPCR conformations. To shed light on the conformational elements and dynamics of the important aspect of GPCR functional selectivity, we carried out unbiased microsecond-length MD simulations of the human serotonin 2A receptor (5-HT2AR) in the absence of ligand and bound to four distinct serotonergic agonists. The 5-HT2AR is a suitable system to study the structural features involved in the ligand-dependent conformational heterogeneity of GPCRs because it is well-characterized experimentally and exhibits a strong agonist-specific phenotype in that some 5-HT2AR agonists induce LSD-like hallucinations, while others lack this psychoactive property entirely. Here we report evidence for structural and dynamic differences in 5-HT2AR interacting with such pharmacologically distinct ligands, hallucinogens, and nonhallucinogens obtained from all-atom MD simulations. Differential ligand binding contacts were identified for structurally similar hallucinogens and nonhallucinogens and found to correspond to different conformations in the intracellular loop 2 (ICL2). From the different ICL2 conformations, functional selective phenotypes are suggested through effects on dimerization and/or distinct direct interaction with effector proteins. Lastly, the findings are presented in the context of currently proposed hallucinogenesis mechanisms, and ICL2 is proposed as a fine-tuning selective switch that can differentiates modes of 5-HT2AR activation.
Download or read book G Protein Coupled Receptors Part A written by and published by Academic Press. This book was released on 2017-10-02 with total page 262 pages. Available in PDF, EPUB and Kindle. Book excerpt: G Protein Coupled Receptors, Second Edition, Volume 143, 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. It contains a wide array of topics about the G protein coupled receptors, as well as updates of chapters from the first edition. - Contains contributions from experts in the field from across the world - Covers a wide array of topics on G protein coupled receptors - Includes analysis based topics
Download or read book G Protein Coupled Receptors written by and published by Academic Press. This book was released on 2019-01-05 with total page 332 pages. Available in PDF, EPUB and Kindle. Book excerpt: G-Protein-Coupled Receptors, Part B, 2nd Edition, Volume 149, the latest release 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 Optical Approaches for Visualization of Arrestin Binding to Muscarinic Receptors, Luciferase Reporter Assay for Unlocking Ligand-mediated Signaling of GPCRs, Assays to Measure GPCR Dependent Cellular Migration, Characterization of the Frizzled GPCRs, Binding Assays for Bradykinin and Angiotensin Receptors, Detection of Misfolded Rhodopsin Aggregates in Cells, Measuring GPCR Ubiquitination and Trafficking, Culture of Primary Neurons and its Use in Studying GPCR Trafficking, and much more. Covers the increasingly appreciated cell biology field of G-protein-coupled receptors Includes both established and new technologies Contributed by experts in the field
Download or read book Biomolecular Simulations in Structure Based Drug Discovery written by Francesco L. Gervasio and published by John Wiley & Sons. This book was released on 2019-04-29 with total page 368 pages. Available in PDF, EPUB and Kindle. Book excerpt: A guide to applying the power of modern simulation tools to better drug design Biomolecular Simulations in Structure-based Drug Discovery offers an up-to-date and comprehensive review of modern simulation tools and their applications in real-life drug discovery, for better and quicker results in structure-based drug design. The authors describe common tools used in the biomolecular simulation of drugs and their targets and offer an analysis of the accuracy of the predictions. They also show how to integrate modeling with other experimental data. Filled with numerous case studies from different therapeutic fields, the book helps professionals to quickly adopt these new methods for their current projects. Experts from the pharmaceutical industry and academic institutions present real-life examples for important target classes such as GPCRs, ion channels and amyloids as well as for common challenges in structure-based drug discovery. Biomolecular Simulations in Structure-based Drug Discovery is an important resource that: -Contains a review of the current generation of biomolecular simulation tools that have the robustness and speed that allows them to be used as routine tools by non-specialists -Includes information on the novel methods and strategies for the modeling of drug-target interactions within the framework of real-life drug discovery and development -Offers numerous illustrative case studies from a wide-range of therapeutic fields -Presents an application-oriented reference that is ideal for those working in the various fields Written for medicinal chemists, professionals in the pharmaceutical industry, and pharmaceutical chemists, Biomolecular Simulations in Structure-based Drug Discovery is a comprehensive resource to modern simulation tools that complement and have the potential to complement or replace laboratory assays for better results in drug design.
Download or read book Serotonin Receptors in Neurobiology written by Amitabha Chattopadhyay and published by CRC Press. This book was released on 2007-05-17 with total page 230 pages. Available in PDF, EPUB and Kindle. Book excerpt: A number of developments spanning a multitude of techniques makes this an exciting time for research in serotonin receptors. A comprehensive review of the subject from a multidisciplinary perspective, Serotonin Receptors in Neurobiology is among the first books to include information on serotonin receptor knockout studies. With contributions from l
Download or read book New Psychoactive Substances written by Hans H. Maurer and published by Springer. This book was released on 2019-02-20 with total page 566 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume is designed to feature the pharmacology of new psychoactive substances, legislative aspects, information exchange including epidemiology, and clinical, forensic, and analytical toxicology in order to facilitate the understanding of this complex and rapidly developing phenomenon.
Download or read book The Advances and Applications of Optogenetics written by Elena G. Govorunova and published by MDPI. This book was released on 2020-12-28 with total page 164 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book provides an update for the rapidly developing technology known as “optogenetics”, which is the use of genetically encoded light-sensitive molecular elements (usually derived from lower organisms) to control or report various physiological and biochemical processes within the cell. Two ongoing clinical trials use optogenetic tools for vision restoration, and optogenetic strategies have been suggested as novel therapies for several neurological, psychiatric and cardiac disorders. This Special Issue comprises two reviews and seven experimental papers on different types of light-sensitive modules widely used in optogenetic studies. These papers demonstrate the efficiency and versatility of optogenetics and are expected to be equally relevant for advanced users and beginners considering using optogenetic tools in their research.
Download or read book The Challenge to AI written by Stephen Robbins and published by Walter de Gruyter GmbH & Co KG. This book was released on 2023-12-22 with total page 329 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book invites readers to explore the intricate world where AI, consciousness, and human cognition intersect. This groundbreaking book considers the profound differences between man and machine, challenging existing notions in AI and cognitive science. It argues that the key to understanding intelligence lies not in software, but in the hardware of our brain - a complex biochemical system far removed from current AI architectures. Through a deep examination of time, perception, language, and the nature of thought, the book presents a compelling case for the indispensability of biology and consciousness in cognition. To achieve this, to engineer this, will indeed be a challenge for AI. FEATURES Presents an alternative to the conventional computer metaphor, offering a new framework for understanding the mind Introduces a fresh perspective on the role of time in AI and philosophy, highlighting its critical importance Explores the biochemical basis of cognition, challenging the traditional focus on symbol manipulation and neural networks
Download or read book Psychedelic Neuroscience written by Tanya Calvey and published by Academic Press. This book was released on 2018-11-21 with total page 272 pages. Available in PDF, EPUB and Kindle. Book excerpt: We are in the midst of what is being called the 'psychedelic renaissance' with growing interest into how psychedelics alter consciousness, brain function and brain connectivity. The acute, often profound, effects of the psychedelic experience can induce lasting improvements in mental health demonstrating that chemistry forms the basis of mystical experience, consciousness and mental wellbeing. - This volume is a collection of chapters by world leaders in fields of neurobiology, neuropsychiatry, psychology, ethnography and pharmacology, addressing the neurobiological mechanisms of action of various classic and atypical psychedelics, their therapeutic potential as well as the possible risks associated with their use
Download or read book Cannabidiol treatment in neurotherapeutic interventions volume II written by Gustavo Gonzalez-Cuevas and published by Frontiers Media SA. This book was released on 2023-04-06 with total page 112 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Principles of Endocrinology and Hormone Action written by Antonino Belfiore and published by Springer. This book was released on 2018-02-08 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume provides comprehensive coverage of the current knowledge of the physiology of the endocrine system and hormone synthesis and release, transport, and action at the molecular and cellular levels. It presents essential as well as in-depth information of value to both medical students and specialists in Endocrinology, Gynecology, Pediatrics, and Internal Medicine. Although it is well established that the endocrine system regulates essential functions involved in growth, reproduction, and homeostasis, it is increasingly being recognized that this complex regulatory system comprises not only hormones secreted by the classic endocrine glands but also hormones and regulatory factors produced by many organs, and involves extensive crosstalk with the neural and immune system. At the same time, our knowledge of the molecular basis of hormone action has greatly improved. Understanding this complexity of endocrine physiology is crucial to prevent endocrine disorders, to improve the sensitivity of our diagnostic tools, and to provide the rationale for pharmacological, immunological, or genetic interventions. It is such understanding that this book is designed to foster.
Download or read book Receptor Receptor Interactions written by Kjell Fuxe and published by Springer Science & Business Media. This book was released on 2013-03-13 with total page 577 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Drug Acceptor Interactions written by Niels Bindslev and published by CRC Press. This book was released on 2017-02-10 with total page 847 pages. Available in PDF, EPUB and Kindle. Book excerpt: Drug-Acceptor Interactions: Modeling theoretical tools to test and evaluate experimental equilibrium effects suggests novel theoretical tools to test and evaluate drug interactions seen with combinatorial drug therapy. The book provides an in-depth, yet controversial, exploration of existing tools for analysis of dose-response studies at equilibrium or steady state. The book is recommended reading for post-graduate students and researchers engaged in the study of systems biology, networks, and the pharmacodynamics of natural or industrial drugs, as well as for medical clinicians interested in drug application and combinatorial drug therapy. Even people without mathematical skills will be able to follow the pros and cons of reaction schemes and their related distribution equations. Chapter 9 is a hands-on guide for software to plot, fit and analyze one’s own data.
Download or read book G Protein Coupled Receptor Signaling written by Mario Tiberi and published by Humana Press. This book was released on 2019-03-01 with total page 406 pages. Available in PDF, EPUB and Kindle. Book excerpt: This detailed volume assembles comprehensive protocols to assist with the study of structural, molecular, cell biological, and in vivo facets of GPCRs, and to enable the development of experimental tools for screening novel GPCR drugs. Sections explore the tweaking of ligands, bioluminescence and FRET approaches, specific GPCR signaling properties, as well as visualization of subcellular compartmentalization. Written for the highly successful Methods in Molecular Biology series, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls. Authoritative and practical, G Protein-Coupled Receptor Signaling: Methods and Protocols serves as an ideal reference for life scientists working in a variety of research fields including molecular pharmacology, cell and developmental biology, brain behavior and physiology, drug development and screening. Chapter 4 is available open access under a CC BY 4.0 license via link.springer.com.
Download or read book G Protein Signaling written by Alan V. Smrcka and published by Springer Science & Business Media. This book was released on 2008-02-02 with total page 246 pages. Available in PDF, EPUB and Kindle. Book excerpt: Alan V. Smrcka presents a collection of cutting-edge methods for investigating G protein signaling from a variety of perspectives ranging from in vitro biochemistry to whole animal studies. Among the readily reproducible techniques presented are those for the purification of G proteins and effectors enzymes, assays of these purified G proteins and effector enzymes, and for the study of G proteins interactions with effectors in intact cells. Additional methods are provided for assaying G protein coupled receptor structure, function, and localization, and for studying the physiological roles for endogenous G proteins.
Download or read book Innovations and Implementations of Computer Aided Drug Discovery Strategies in Rational Drug Design written by Sanjeev Kumar Singh and published by Springer Nature. This book was released on 2021-02-02 with total page 334 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book presents various computer-aided drug discovery methods for the design and development of ligand and structure-based drug molecules. A wide variety of computational approaches are now being used in various stages of drug discovery and development, as well as in clinical studies. Yet, despite the rapid advances in computer software and hardware, combined with the exponential growth in the available biological information, there are many challenges that still need to be addressed, as this book shows. In turn, it shares valuable insights into receptor-ligand interactions in connection with various biological functions and human diseases. The book discusses a wide range of phylogenetic methods and highlights the applications of Molecular Dynamics Simulation in the drug discovery process. It also explores the application of quantum mechanics in order to provide better accuracy when calculating protein-ligand binding interactions and predicting binding affinities. In closing, the book provides illustrative descriptions of major challenges associated with computer-aided drug discovery for the development of therapeutic drugs. Given its scope, it offers a valuable asset for life sciences researchers, medicinal chemists and bioinformaticians looking for the latest information on computer-aided methodologies for drug development, together with their applications in drug discovery.
Download or read book Encyclopedia of Molecular Pharmacology written by Stefan Offermanns and published by Springer Science & Business Media. This book was released on 2008-08-14 with total page 1515 pages. Available in PDF, EPUB and Kindle. Book excerpt: An essential text, this is a fully updated second edition of a classic, now in two volumes. It provides rapid access to information on molecular pharmacology for research scientists, clinicians and advanced students. With the A-Z format of over 2,000 entries, around 350 authors provide a complete reference to the area of molecular pharmacology. The book combines the knowledge of classic pharmacology with the more recent approach of the precise analysis of the molecular mechanisms by which drugs exert their effects. Short keyword entries define common acronyms, terms and phrases. In addition, detailed essays provide in-depth information on drugs, cellular processes, molecular targets, techniques, molecular mechanisms, and general principles.
