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Tracking The Protac Degradation Pathway In Living Cells Highlights The Importance Of Ternary Complex Measurement For Protac Optimization
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Book Synopsis Modern Methods of Drug Design and Development by :
Download or read book Modern Methods of Drug Design and Development written by and published by Elsevier. This book was released on 2023-10-18 with total page 600 pages. Available in PDF, EPUB and Kindle. Book excerpt: Modern Methods of Drug Design and Development, a volume in the Methods in Enzymology series highlights new advances in the field with this new volume presenting interesting chapters on a variety of topics, including Recombinant protein purification for structural and kinetic studies, Steady-state kinetic analysis of reversible enzyme inhibitors, Steady-State Enzyme Kinetics, Analysis of enzyme kinetic data using ICEKAT, NMR techniques in drug discovery, Dynamic simulations and pre-steady state kinetics to guide drug discovery, Design and assay of substrate-product analogues for racemases and epimerases, Sensitive high throughput methods to screen for P450 inhibition: A- MI complex forming drugs, and more. Other chapters cover Sensitive high throughput methods to screen for P450 inhibition: B-Heme loss causing drugs, Discovery and development of inhibitors of acetyltransferase Eis to combat Mycobacterium tuberculosis, Crystallographic fragment screening in academic cancer drug discovery, Fast fragment- and compound-screening pipeline at the Swiss Light Source, Chemical biology, enzymology and drug discovery, PROTACs, Proximity-Induced Pharmacology (PROTACs), and much more. Provides the authority and expertise of leading contributors from an international board of authors Presents the latest release in the Methods in Enzymology series Updated release includes the latest information on Modern Methods of Drug Design and Development
Book Synopsis Targeted Protein Degradation by : Angela M. Cacace
Download or read book Targeted Protein Degradation written by Angela M. Cacace and published by Humana. This book was released on 2021-08-26 with total page 351 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume contains a collection of innovative techniques for studying targeted protein degradation. Chapters guide readers through heterobifunctional proteolysis-targeting chimeras (PROTACs) approaches, E3 ligase, E3 ligase-induced ubiquitylation, proteomic approaches, novel degrader molecules, molecular glue, and stabilize binding interaction between a target and E3 ubiquitin ligase. Written in the format of the highly successful Methods in Molecular Biology series, each chapter includes an introduction to the topic, lists necessary materials and reagents, includes tips on troubleshooting and known pitfalls, and step-by-step, readily reproducible protocols. Authoritative and cutting-edge, Targeted Protein Degradation: Methods and Protocols aims to ensure successful results in this emerging field of drug discovery.
Book Synopsis PI3K signalling by : Klaus Okkenhaug
Download or read book PI3K signalling written by Klaus Okkenhaug and published by Frontiers Media SA. This book was released on 2015-03-05 with total page 140 pages. Available in PDF, EPUB and Kindle. Book excerpt: The PI3Ks control many key functions in immune cells. PI3Ks phosphorylate PtdIns(4,5)P2 to yield PtdIns(3,4,5)P3. Initially, PI3K inhibitors such as Wortmannin, LY294002 and Rapamycin were used to establish a central role for Pi3K pathway in immune cells. Considerable progress in understanding the role of this pathway in cells of the immune system has been made in recent years, starting with analysis of various PI3K and Pten knockout mice and subsequently mTOR and Foxo knockout mice. Together, these experiments have revealed how PI3Ks control B cell and T cell development, T helper cell differentiation, regulatory T cell development and function, B cell and T cell trafficking, immunoglobulin class switching and much, much more. The PI3Kd inhibitor idelalisib has recently been approved for the treatment of B cell lymphoma. Clinical trials of other PI3K inhibitors in autoimmune and inflammatory diseases are also in progress. This is an opportune time to consider a Research Topic considering when what we have learned about the PI3K signalling module in lymphocyte biology and how this is making an impact on clinical immunology and haematology.
Book Synopsis Activity-Based Protein Profiling by : Benjamin F. Cravatt
Download or read book Activity-Based Protein Profiling written by Benjamin F. Cravatt and published by Springer. This book was released on 2019-01-25 with total page 420 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume provides a collection of contemporary perspectives on using activity-based protein profiling (ABPP) for biological discoveries in protein science, microbiology, and immunology. A common theme throughout is the special utility of ABPP to interrogate protein function and small-molecule interactions on a global scale in native biological systems. Each chapter showcases distinct advantages of ABPP applied to diverse protein classes and biological systems. As such, the book offers readers valuable insights into the basic principles of ABPP technology and how to apply this approach to biological questions ranging from the study of post-translational modifications to targeting bacterial effectors in host-pathogen interactions.
Book Synopsis Platform Technologies in Drug Discovery and Validation by :
Download or read book Platform Technologies in Drug Discovery and Validation written by and published by Academic Press. This book was released on 2017-11-21 with total page 692 pages. Available in PDF, EPUB and Kindle. Book excerpt: Platform Technologies in Drug Discovery and Validation, Volume 50, the latest release in the Annual Reports in Medicinal Chemistry series, provides timely and critical reviews of important topics in medicinal chemistry, with an emphasis on emerging topics in the biological sciences. Topics covered in this new volume include DELT, Oligos: ASO, siRNA, CRISPR, Micro-fluidic chemistry, High throughput screening, Kinase-centric computational drug development, Virtual Screening, Phenotypic screening, PROTACS, Chemical Biology, Fragment-based lead generation, Antibody-Drug Conjugates, Antibody-recruiting small molecules, Deuteration, and Peptides. - Unique for its treatment of platform technologies for medicinal chemistry and target validation - Provides a single, rich volume that summaries a broad spectrum of expertise relevant to the field - Presents state-of-the-art summaries of platform technologies
Book Synopsis Fragment-Based Drug Discovery by : Steven Howard
Download or read book Fragment-Based Drug Discovery written by Steven Howard and published by Royal Society of Chemistry. This book was released on 2015-06-17 with total page 314 pages. Available in PDF, EPUB and Kindle. Book excerpt: Fragment-based drug discovery is a rapidly evolving area of research, which has recently seen new applications in areas such as epigenetics, GPCRs and the identification of novel allosteric binding pockets. The first fragment-derived drug was recently approved for the treatment of melanoma. It is hoped that this approval is just the beginning of the many drugs yet to be discovered using this fascinating technique. This book is written from a Chemist's perspective and comprehensively assesses the impact of fragment-based drug discovery on a wide variety of areas of medicinal chemistry. It will prove to be an invaluable resource for medicinal chemists working in academia and industry, as well as anyone interested in novel drug discovery techniques.
Book Synopsis Thorium—Energy for the Future by : A.K. Nayak
Download or read book Thorium—Energy for the Future written by A.K. Nayak and published by Springer. This book was released on 2019-01-30 with total page 533 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book comprises selected proceedings of the ThEC15 conference. The book presents research findings on various facets of thorium energy, including exploration and mining, thermo-physical and chemical properties of fuels, reactor physics, challenges in fuel fabrication, thorium fuel cycles, thermal hydraulics and safety, material challenges, irradiation experiences, and issues and challenges for the design of advanced thorium fueled reactors. Thorium is more abundant than uranium and has the potential to provide energy to the world for centuries if used in a closed fuel cycle. As such, technologies for using thorium for power generation in nuclear reactors are being developed worldwide. Since there is a strong global thrust towards designing nuclear reactors with thorium-based fuel, this book will be of particular interest to nuclear scientists, reactor designers, regulators, academics and policymakers.
Download or read book Dark Remedy written by Trent Stephens and published by Basic Books. This book was released on 2009-04-27 with total page 244 pages. Available in PDF, EPUB and Kindle. Book excerpt: In this riveting medical detective story, Trent Stephens and Rock Brynner recount the history of thalidomide, from the epidemic of birth defects in the 1960's to the present day, as scientists work to create and test an alternative drug that captures thalidomide's curative properties without its cruel side effects. A parable about compassion-and the absence of it-Dark Remedy is a gripping account of thalidomide's extraordinary impact on the lives of individuals and nations over half a century.
Book Synopsis Advances in Medicinal Chemistry by : B.E. Maryanoff
Download or read book Advances in Medicinal Chemistry written by B.E. Maryanoff and published by Elsevier. This book was released on 1999-04-01 with total page 338 pages. Available in PDF, EPUB and Kindle. Book excerpt: Volume 4 of Advances in Medicinal Chemistry is comprised of six chapters on a wide range of topics in medicinal chemistry, including molecular modeling, structure-based drug design, organic synthesis, peptide conformational analysis, biological assessment, structure-activity correlation, and lead optimization. Chapter 1 presents an account about amino acid-based peptide mimetics corresponding to b-turn, loop, helical motifs in proteins as a probe of ligand-receptor and ligand-enzyme molecular interactions. Chapter 2 addresses new facets of the medicinal chemistry of the important anticancer drug Taxol® (paclitaxel). Chapter 3 relates an account of the search for new drugs for the treatment of malaria based on the natural product artemisinin. Chapter 4 applies computational chemistry to the evaluation of compound libraries for biological testing. Chapter 5 describes the construction of a 3-dimensional molecular model of the human thrombin receptor, the first protease-activated G-protein coupled receptor (PAR-1), as a means to explore the intermolecular contacts involved in agonist peptide recognition. Finally, Chapter 6 describes the research conducted at Merck on inhibitors of farnesyl transferase as a potential treatment for human cancers.
Book Synopsis Forestborn by : Elayne Audrey Becker
Download or read book Forestborn written by Elayne Audrey Becker and published by Tor Teen. This book was released on 2021-08-31 with total page 323 pages. Available in PDF, EPUB and Kindle. Book excerpt: A young, orphaned shapeshifter in a world that fears magic must risk everything if she hopes to save her only friend in Elayne Audrey Becker's Forestborn, first in a new fantasy series with a timeless feel. TO BE BORN OF THE FOREST IS A GIFT AND A CURSE. Rora is a shifter, as magical as all those born in the wilderness—and as feared. She uses her abilities to spy for the king, traveling under different guises and listening for signs of trouble. When a magical illness surfaces across the kingdom, Rora uncovers a devastating truth: Finley, the young prince and her best friend, has caught it, too. His only hope is stardust, the rarest of magical elements, found deep in the wilderness where Rora grew up—and to which she swore never to return. But for her only friend, Rora will face her past and brave the dark, magical wood, journeying with her brother and the obstinate, older prince who insists on coming. Together, they must survive sentient forests and creatures unknown, battling an ever-changing landscape while escaping human pursuers who want them dead. With illness gripping the kingdom and war on the horizon, Finley’s is not the only life that hangs in the balance. At the Publisher's request, this title is being sold without Digital Rights Management Software (DRM) applied.
Book Synopsis Structural DNA Nanotechnology by : Nadrian C. Seeman
Download or read book Structural DNA Nanotechnology written by Nadrian C. Seeman and published by Cambridge University Press. This book was released on 2015 with total page 269 pages. Available in PDF, EPUB and Kindle. Book excerpt: Written by the founder of the field, this is a comprehensive and accessible introduction to structural DNA nanotechnology.
Book Synopsis Inhibitors of Protein–Protein Interactions by : Ali Tavassoli
Download or read book Inhibitors of Protein–Protein Interactions written by Ali Tavassoli and published by Royal Society of Chemistry. This book was released on 2020-12-07 with total page 357 pages. Available in PDF, EPUB and Kindle. Book excerpt: Protein-protein interactions (PPI) are at the heart of the majority of cellular processes, and are frequently dysregulated or usurped in disease. Given this central role, the inhibition of PPIs has been of significant interest as a means of treating a wide variety of diseases. However, there are inherent challenges in developing molecules capable of disrupting the relatively featureless and large interfacial areas involved. Despite this, there have been a number of successes in this field in recent years using both traditional drug discovery approaches and innovative, interdisciplinary strategies using novel chemical scaffolds. This book comprehensively covers the various aspects of PPI inhibition, encompassing small molecules, peptidomimetics, cyclic peptides, stapled peptides and macrocycles. Illustrated throughout with successful case studies, this book provides a holistic, cutting-edge view of the subject area and is ideal for chemical biologists and medicinal chemists interested in developing PPI inhibitors.
Book Synopsis The Proteomics Protocols Handbook by : John M. Walker
Download or read book The Proteomics Protocols Handbook written by John M. Walker and published by Springer Science & Business Media. This book was released on 2007-10-09 with total page 969 pages. Available in PDF, EPUB and Kindle. Book excerpt: Hands-on researchers describe in step-by-step detail 73 proven laboratory methods and bioinformatics tools essential for analysis of the proteome. These cutting-edge techniques address such important tasks as sample preparation, 2D-PAGE, gel staining, mass spectrometry, and post-translational modification. There are also readily reproducible methods for protein expression profiling, identifying protein-protein interactions, and protein chip technology, as well as a range of newly developed methodologies for determining the structure and function of a protein. The bioinformatics tools include those for analyzing 2D-GEL patterns, protein modeling, and protein identification. All laboratory-based protocols follow the successful Methods in Molecular BiologyTM series format, each offering step-by-step laboratory instructions, an introduction outlining the principle behind the technique, lists of the necessary equipment and reagents, and tips on troubleshooting and avoiding known pitfalls.
Book Synopsis Nanopore-Based Technology by : Maria E. Gracheva
Download or read book Nanopore-Based Technology written by Maria E. Gracheva and published by Humana Press. This book was released on 2012-04-18 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: Nanopores are vital biological features, described as tiny holes in cellular membranes used for recognition and transport of ions and molecules between compartments within the cell, as well as between the extracellular environment and the cell itself. Their study, ever growing in esteem, leads toward the promise of ultra-fast sequencing of DNA molecules with the ultimate goal of building a nanoscale device that will make rapid and cheap DNA sequencing a reality. In Nanopore-Based Technology, expert researchers in the forefront of the field explore the cutting-edge of nanopore technology for single molecule sensing, detection, and characterization. Divided into four convenient parts, this volume covers single molecule characterization techniques utilizing biological pores, methods for biomolecule characterization with nanoporous artificial membranes, computational studies of the biomolecule confined within the nanopore environment, as well as techniques that use novel materials in conjunction with nanopore sensing. Written for the highly successful Methods in Molecular BiologyTM series, this work provides the kind of detailed description and implementation advice that is crucial for achieving optimal results. Authoritative and state-of-the-art, Nanopore-Based Technology serves as an excellent representation of the present-day available techniques for biomolecule characterization with nanoporous membranes in order to guide researchers toward developing the next generation of technologies for fast and cheap DNA sequencing with practically no limitations on the read lengths.
Download or read book Macrolides written by Biljana Arsic and published by Walter de Gruyter GmbH & Co KG. This book was released on 2018-03-19 with total page 112 pages. Available in PDF, EPUB and Kindle. Book excerpt: Macrolide antibiotics represent a class of natural macrocyclic products, one of the most clinically important antibiotics. Unfortunately, the production and development of new macrolide antibiotics are not represented enough in the pharmaceutical industry today. The intention of the book is therefore not only to be a teaching tool for students and experts, but also to draw the attention of the general public to this extremely useful, cheap and relatively unharmful effective anti-macrobials, and potential anti-malarials. The authors introduce the different classes of macrolides and their derivatives, principles of their biological activity, their structure and interactions with biological targets as well as synthetic methods to produce new macrolide antibiotics of similar or improved properties. Special emphasis was put on conjugates of macrolides with nucleobases or nucleosides with numerous applications; among them the most important remains the attempt to overcome bacterial resistance.
Book Synopsis Fluorescent Nanodiamonds by : Huan-Cheng Chang
Download or read book Fluorescent Nanodiamonds written by Huan-Cheng Chang and published by John Wiley & Sons. This book was released on 2018-11-12 with total page 294 pages. Available in PDF, EPUB and Kindle. Book excerpt: The most comprehensive reference on fluorescent nanodiamond physical and chemical properties and contemporary applications Fluorescent nanodiamonds (FNDs) have drawn a great deal of attention over the past several years, and their applications and development potential are proving to be manifold and vast. The first and only book of its kind, Fluorescent Nanodiamonds is a comprehensive guide to the basic science and technical information needed to fully understand the fundamentals of FNDs and their potential applications across an array of domains. In demonstrating the importance of FNDs in biological applications, the authors bring together all relevant chemistry, physics, materials science and biology. Nanodiamonds are produced by powerful cataclysmic events such as explosions, volcanic eruptions and meteorite impacts. They also can be created in the lab by high-pressure high-temperature treatment of graphite or detonating an explosive in a reactor vessel. A single imperfection can give a nanodiamond a specific, isolated color center which allows it to function as a single, trapped atom. Much smaller than the thickness of a human hair, a nanodiamond can have a huge surface area that allows it to bond with a variety of other materials. Because of their non-toxicity, nanodiamonds may be useful in biomedical applications, such as drug delivery and gene therapy. The most comprehensive reference on a topic of rapidly increasing interest among academic and industrial researchers across an array of fields Includes numerous case studies and practical examples from many areas of research and industrial applications, as well as fascinating and instructive historical perspectives Each chapter addresses, in-depth, a single integral topic including the fundamental properties, synthesis, mechanisms and functionalisation of FNDs The first book published by the key patent holder with his research group in the field of FNDs Fluorescent Nanodiamonds is an important working resource for a broad range of scientists and engineers in industry and academia. It will also be a welcome reference for instructors in chemistry, physics, materials science, biology and related fields.
Book Synopsis Chemistry of Energetic Materials by : George A. Olah
Download or read book Chemistry of Energetic Materials written by George A. Olah and published by Academic Press. This book was released on 2012-12-02 with total page 225 pages. Available in PDF, EPUB and Kindle. Book excerpt: The study of energetic materials is emerging from one primarily directed toward practical interests to an advanced area of fundamental research, where state-of-the-art methods and theory are used side by side with modern synthetic methods. This timely book integrates the recent experimental, synthetic, and theoretical research of energetic materials. Editors George Olah and David Squire emphasize the importance of structure and mechanism in determining properties and performances. They also explore new spectrometric methods and synthetic approaches in this useful reference. - Discusses structural analysis by x-ray crystallography - Explains chemical dynamics by photofragmentation translational spectroscopy - Covers kinetic analysis by ultrafast absorption and emission spectroscopy - Details syntheses of polycyclic caged amines, fuel additives, and polynitro compounds - Examines computer-aided design of monopropellants - Includes contributions by two Nobel laureates and five members of the National Academy of Sciences
