Download or read book GPCRs From Deorphanization to Lead Structure Identification written by H. Bourne and published by Springer Science & Business Media. This book was released on 2007-07-03 with total page 275 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book offers an insight into the approaches taken by industry and academia to address GPCRs and depict how mature this target class-oriented research has become in the last decade. Coverage also reflects the actual trends in the fast-emerging field of GPCR research in academia and industry. It is based on the international workshop GPCRs: From Deorphanisation to Lead Structure Identification, held in Berlin in May 2006.
Download or read book The G Protein Coupled Receptors Handbook written by Lakshmi A. Devi and published by Springer Science & Business Media. This book was released on 2008-03-01 with total page 414 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Download or read book GPCRs written by Beata Jastrzebska and published by Academic Press. This book was released on 2019-09-12 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Download or read book GPCR Molecular Pharmacology and Drug Targeting written by Annette Gilchrist and published by Wiley. This book was released on 2010-08-09 with total page 536 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
Download or read book Computational Methods for GPCR Drug Discovery written by Alexander Heifetz and published by Humana Press. This book was released on 2017-11-30 with total page 436 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume looks at modern computational strategies and techniques used in GPCR drug discovery including structure and ligand-based approaches and cheminformatics. The chapters in this book describe how these approaches can be applied to address key drug discovery issues, such as receptor structure modelling, function and dynamics, prediction of protein-water-ligand interactions and binding kinetics, free energy of binding, interconversion between agonists and antagonists, deorphanization of GPCRs, and the discovery of biased and allosteric modulators. Written in the highly successful Methods in Molecular Biology series format, chapters include introductions to their respective topics, lists of the necessary software and tools, step-by-step, readily reproducible modelling protocols, and tips on troubleshooting and avoiding known pitfalls. Cutting-edge and unique,Computational Methods for GPCR Drug Discovery is a valuable resource for structural and molecular biologists, computational and medicinal chemists, pharmacologists, and drug designers.
Download or read book Receptor Based Drug Design written by Paul Leff and published by CRC Press. This book was released on 1998-04-10 with total page 816 pages. Available in PDF, EPUB and Kindle. Book excerpt: Employing a wide range of examples from G-protein-coupled receptors and ligand-gated ion channels, this detailed, single-source reference illustrates the principles of pharmacological analysis and receptor classification that are the basis of rational drug design. Explains the experimental and theoretical methods used to characterize interactions between ligands and receptors-providing the pharmacological information needed to solve treatment problems and facilitate the drug design process! Demonstrating the achievements of the receptor-based approach in therapeutics and indicating future directions, Receptor-Based Drug Design introduces novel computer-assisted strategies for the design of new agonists, antagonists, and inverse agonists for G-protein-coupled receptors shows how to assess agonist concentration-effect curve data discusses radioligand binding assays presents new in vitro multiarray assays for G-protein-coupled receptors explains the use of individual second messenger signaling responses in analyzing drug-receptor interactions examines the role of electrophysiology in finding new drugs and drug targets describes selectively acting b-adrenoceptor agonists and glucocorticoid steroids for asthma treatment outlines the rationale for using angiotensin receptor antagonists and more! Written by over 25 international authorities and containing nearly 1200 bibliographic citations, Receptor-Based Drug Design is a practical resource for pharmacologists, pharmacists, and pharmaceutical scientists; organic and medicinal chemists and biochemists; molecular biologists; biomedical researchers; and upper-level undergraduate and graduate students in these disciplines.
Download or read book Computational Molecular Modelling in Structural Biology written by and published by Academic Press. This book was released on 2018-08-24 with total page 152 pages. Available in PDF, EPUB and Kindle. Book excerpt: Computational Molecular modelling in Structural Biology, Volume 113, the latest release in the Advances in Protein Chemistry and Structural Biology, highlights new advances in the field, with this new volume presenting interesting chapters on charting the Bromodomain BRD4: Towards the Identification of Novel Inhibitors with Molecular Similarity and Receptor Mapping, and Computational Methods to Discover Compounds for the Treatment of Chagas Disease. Provides the authority and expertise of leading contributors from an international board of authors Presents the latest release in the Advances in Protein Chemistry and Structural Biology series Updated, with the latest information on Computational Molecular Modelling in Structural Biology
Download or read book Fundamental Concepts written by Fidele Ntie-Kang and published by Walter de Gruyter GmbH & Co KG. This book was released on 2020-02-24 with total page 478 pages. Available in PDF, EPUB and Kindle. Book excerpt: Vol. 1 of Chemoinformatics of Natural Products presents an overview of natural products chemistry, discussing the chemical space of naturally occurring compounds, followed by an overview of computational methods.
Download or read book QSPR QSAR Analysis Using SMILES and Quasi SMILES written by Alla P. Toropova and published by Springer Nature. This book was released on 2023-06-10 with total page 470 pages. Available in PDF, EPUB and Kindle. Book excerpt: This contributed volume overviews recently presented approaches for carrying out QSPR/QSAR analysis by using a simplifying molecular input-line entry system (SMILES) to represent the molecular structure. In contrast to traditional SMILES, quasi-SMILES is a sequence of special symbols-codes that reflect molecular features and codes of experimental conditions. SMILES and quasi-SMILES serve as a basis to develop QSPR/QSAR as well Nano-QSPR/QSAR via the Monte Carlo calculation that provides the so-called optimal descriptors for QSPR/QSAR models. The book presents a reliable technology for developing Nano-QSPR/QSAR while it also includes the description of the algorithms of the Monte Carlo optimization. It discusses the theory and practice of the technique of variational authodecoders (VAEs) based on SMILES and analyses in detail the index of ideality of correlation (IIC) and the correlation intensity index (CII) which are new criteria for the predictive potential of the model. The mathematical apparatus used is simple so that students of relevant specializations can easily follow. This volume is a valuable contribution to the field and will be of great interest to developers of models of physicochemical properties and biological activity, chemical technologists, and toxicologists involved in the area of drug design.
Download or read book Immunotherapy in 2020 written by Andreas Radbruch and published by Springer Science & Business Media. This book was released on 2007-06-22 with total page 116 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume features contributions from participants of the ESRF symposium on Immunotherapy in 2020—Visions and Trends for Targeting Inflammatory Diseases held in Potsdam near Berlin, Germany, in October 2006. The symposium presentations covered the main mechanisms of immunoregulation.
Download or read book Progestins and the Mammary Gland written by Orla M. Conneely and published by Springer Science & Business Media. This book was released on 2008-03-27 with total page 211 pages. Available in PDF, EPUB and Kindle. Book excerpt: Progestins play a key role in reproductive endocrinology and as pharmaceutical drugs for contraception and in combined hormone therapy. To further our understanding of progestin action in the mammary gland, an international symposium, attended by leading researchers from academia and industry, was held in Berlin, 21–23 March 2007. Genetic mouse models helped to elucidate the role of progestins, both in normal breast development and in disease. Mechanistic molecular studies inspired the design of new progestins with improved tissue selectivity. In addition, the clinical impact of progesterone receptor agonists and antagonists for the prevention and treatment of breast cancer was discussed.
Download or read book Organocatalysis written by Manfred Reetz and published by Springer Science & Business Media. This book was released on 2008-05-27 with total page 348 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book provides an excellent overview on state-of-the-art of modern organocatalysis. It presents the contributions from leading experts, with backgrounds in academia and industry, to an Ernst Schering Research Foundation Symposium held in April 2007. It will be of interest to those who want a general overview of the topic, but also to those who want to learn more about the state-of-the-art, current trends and perspectives in this highly dynamic field of research.
Download or read book Oncogenes Meet Metabolism written by Guido Kroemer and published by Springer Science & Business Media. This book was released on 2008-07-25 with total page 275 pages. Available in PDF, EPUB and Kindle. Book excerpt: In 1920s, Otto Warburg described the phenomenon of ‘aerobic glycolysis’, the ability of tumour cells to convert glucose to lactate in the presence of normal oxygen conditions. Warburg’s hypothesis of an altered metabolism in cancer cells found no immediate acceptance, though it was latter confirmed for most human tumours. With the advent of molecular biology the focus in tumour research has shifted towards the search for oncogenes. However, the interest in cancer molecular profiling eventually led to a renaissance of the Warburg effect trying to combine genetic alterations with effects on metabolism with the help of modern analytic technologies to rapidly analyze broad varieties of metabolites in various tissues and bodyfluids (metabonomics).
Download or read book New Avenues to Efficient Chemical Synthesis written by P.H. Seeberger and published by Springer Science & Business Media. This book was released on 2007-06-02 with total page 247 pages. Available in PDF, EPUB and Kindle. Book excerpt: In modern drug discovery and development, chemical synthesis is one of the key technologies. For the rapid preparation of new test compounds and drug development candidates, several innovative technologies with great potential have emerged. This book offers a compact overview of the current status of these technologies and includes many real-life examples from industry and academic institutions.
Download or read book Protein Homeostasis Diseases written by Angel L. Pey and published by Academic Press. This book was released on 2020-02-13 with total page 450 pages. Available in PDF, EPUB and Kindle. Book excerpt: Protein Homeostasis Diseases: Mechanisms and Novel Therapies offers an interdisciplinary examination of the fundamental aspects, biochemistry and molecular biology of protein homeostasis disease, including the use of natural and pharmacological small molecules to treat common and rare protein homeostasis disorders. Contributions from international experts discuss the biochemical and genetic components of protein homeostasis disorders, the mechanisms by which genetic variants may cause loss-of-function and gain-of-toxic-function, and how natural ligands can restore protein function and homeostasis in genetic diseases. Applied chapters provide guidance on employing high throughput sequencing and screening methodologies to develop pharmacological chaperones and repurpose approved drugs to treat protein homeostasis disorders. Provides an interdisciplinary examination of protein homeostasis disorders, with an emphasis on treatment strategies employing small natural and pharmacological ligands Offers applied approaches in employing high throughput sequencing and screening to develop pharmacological chaperones to treat protein homeostasis disease Gathers expertise from a range of international chapter authors who work across various biological methods and disease specific disciplines of relevance
Download or read book Crystallization of Membrane Proteins written by Hartmut Michel and published by CRC Press. This book was released on 2018-01-18 with total page 343 pages. Available in PDF, EPUB and Kindle. Book excerpt: The precise knowledge of the structure of biological macromolecules forms the basis of understanding their function and their mechanism of action. It also lays the foundation for rational protein and drug design. The only method to obtain this knowledge is still crystallography. At present, the structures of about 400 proteins are known at or nearly at atomic proteins. However, only two of them are membrane proteins or complexes of the membrane proteins. The reasons for the difference is not the crystals of membrane proteins resists forming special problems when being analysed. The reason is that the membrane proteins resist into forming into well-ordered crystals. The intention of this book is to help to produce well-ordered crystals proteins and to provide guidelines, it is aimed at both biochemists and protein crystallographer‘s.
Download or read book Encyclopedia of Signaling Molecules written by Sangdun Choi and published by Springer. This book was released on 2017-12-15 with total page 6330 pages. Available in PDF, EPUB and Kindle. Book excerpt: The second edition of this encyclopedia presents over 400 biologically important signaling molecules and the content is built on the core concepts of their functions along with early findings written by some of the world’s foremost experts. The molecules are described by recognized leaders in each molecule. The interactions of these single molecules in signal transduction networks will also be explored. This encyclopedia marks a new era in overview of current cellular signaling molecules for the specialist and the interested non-specialist alike. Currently, there are more than 30,000 genes in human genome. However, not all the proteins encoded by these genes work equally in order to maintain homeostasis. Understanding the important signaling molecules as completely as possible will significantly improve our research-based teaching and scientific capabilities.
