Fragment Based Drug Discovery
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Fragment Based Drug Discovery
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Author : Steven Howard
language : en
Publisher: Royal Society of Chemistry
Release Date : 2015-07-03
Fragment Based Drug Discovery written by Steven Howard and has been published by Royal Society of Chemistry this book supported file pdf, txt, epub, kindle and other format this book has been release on 2015-07-03 with Medical categories.
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.
Fragment Based Drug Discovery
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Author : Daniel A. Erlanson
language : en
Publisher: John Wiley & Sons
Release Date : 2016-02-23
Fragment Based Drug Discovery written by Daniel A. Erlanson and has been published by John Wiley & Sons this book supported file pdf, txt, epub, kindle and other format this book has been release on 2016-02-23 with Medical categories.
From its origins as a niche technique more than 15 years ago, fragment-based approaches have become a major tool for drug and ligand discovery, often yielding results where other methods have failed. Written by the pioneers in the field, this book provides a comprehensive overview of current methods and applications of fragment-based discovery, as well as an outlook on where the field is headed. The first part discusses basic considerations of when to use fragment-based methods, how to select targets, and how to build libraries in the chemical fragment space. The second part describes established, novel and emerging methods for fragment screening, including empirical as well as computational approaches. Special cases of fragment-based screening, e. g. for complex target systems and for covalent inhibitors are also discussed. The third part presents several case studies from recent and on-going drug discovery projects for a variety of target classes, from kinases and phosphatases to targeting protein-protein interaction and epigenetic targets.
Fragment Based Drug Discovery
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Author : Edward R. Zartler
language : en
Publisher: John Wiley & Sons
Release Date : 2008-11-20
Fragment Based Drug Discovery written by Edward R. Zartler and has been published by John Wiley & Sons this book supported file pdf, txt, epub, kindle and other format this book has been release on 2008-11-20 with Science categories.
Fragment-based drug discovery (FBDD) is a new paradigm in drug discovery that utilizes very small molecules - fragments of larger molecules. It is a faster, cheaper, smarter way to do drug discovery, as shown by the number of pharmaceutical companies that have embraced this approach and the biotechnology companies who use fragments as their sole source of drug discovery. Fragment-Based Drug Discovery: A Practical Approach is a guide to the techniques and practice of using fragments in drug screening. The emphasis is on practical guidance, with procedures, case studies, practical tips, and contributions from industry. Topics covered include: an introduction to fragment based drug discovery, why using fragments is a more efficient process than predominant models, and what it means to have a successful FBDD effort. setting up an FBDD project library building and production NMR in fragment screening and follow up application of protein-ligand NOE matching to the rapid evaluation of fragment binding poses target immobilized NMR screening: validation and extension to membrane proteins in situ fragment-based medicinal chemistry: screening by mass spectrometry computational approaches to fragment and substructure discovery and evaluation virtual fragment scanning: current trends, applications and web based tools fragment-based lead discovery using covalent capture methods case study from industry: the identification of high affinity beta-secretase inhibitors using fragment-based lead generation With contributions from industry experts who have successfully set up an industrial fragment-based research program, Fragment-Based Drug Discovery: A Practical Approach offers essential advice to anyone embarking on drug discovery using fragments and those looking for a new approach to screening for drugs.
Fragment Based Drug Discovery And X Ray Crystallography
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Author : Thomas G. Davies
language : en
Publisher: Springer Science & Business Media
Release Date : 2012-01-23
Fragment Based Drug Discovery And X Ray Crystallography written by Thomas G. Davies and has been published by Springer Science & Business Media this book supported file pdf, txt, epub, kindle and other format this book has been release on 2012-01-23 with Science categories.
Introduction to Fragment-Based Drug Discovery, by Daniel A. Erlanson Fragment Screening Using X-Ray Crystallography, by Thomas G. Davies and Ian J. Tickle Hsp90 Inhibitors and Drugs from Fragment and Virtual Screening, by Stephen Roughley, Lisa Wright, Paul Brough, Andrew Massey and Roderick E. Hubbard Combining NMR and X-ray Crystallography in Fragment-Based Drug Discovery: Discovery of Highly Potent and Selective BACE-1 Inhibitors, by Daniel F. Wyss, Yu-Sen Wang, Hugh L. Eaton, Corey Strickland, Johannes H. Voigt, Zhaoning Zhu and Andrew W. Stamford Combining Biophysical Screening and X-Ray Crystallography for Fragment-Based Drug Discovery, by Michael Hennig, Armin Ruf and Walter Huber Targeting Protein–Protein Interactions and Fragment-Based Drug Discovery, by Eugene Valkov, Tim Sharpe, May Marsh, Sandra Greive and Marko Hyvönen Fragment Screening and HIV Therapeutics, by Joseph D. Bauman, Disha Patel and Eddy Arnold Fragment-Based Approaches and Computer-Aided Drug Discovery, by Didier Rognan
Fragment Based Drug Design
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Author : Lawrence C. Kuo
language : en
Publisher: Academic Press
Release Date : 2011-03-09
Fragment Based Drug Design written by Lawrence C. Kuo and has been published by Academic Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2011-03-09 with Medical categories.
There are numerous excellent reviews on fragment-based drug discovery (FBDD), but there are to date no hand-holding guides or protocols with which one can embark on this orthogonal approach to complement traditional high throughput screening methodologies. This Methods in Enzymology volume offers the tools, practical approaches, and hit-to-lead examples on how to conduct FBDD screens. The chapters in this volume cover methods that have proven to be successful in generating leads from fragments, including chapters on how to apply computational techniques, nuclear magnetic resonance, surface plasma resonance, thermal shift and binding assays, protein crystallography, and medicinal chemistry in FBDD. Also elaborated by experienced researchers in FBDD are sample preparations of fragments, proteins, and GPCR as well as examples of how to generate leads from hits. Offers the tools, practical approaches, and hit-to-lead examples on how to conduct FBDD screens The chapters in this volume cover methods that have proven to be successful in generating leads from fragments, including chapters on how to apply computational techniques, nuclear magnetic resonance, surface plasma resonance, thermal shift and binding assays, protein crystallography, and medicinal chemistry in FBDD
Fragment Based Approaches In Drug Discovery
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Author : Wolfgang Jahnke
language : en
Publisher: John Wiley & Sons
Release Date : 2006-12-13
Fragment Based Approaches In Drug Discovery written by Wolfgang Jahnke and has been published by John Wiley & Sons this book supported file pdf, txt, epub, kindle and other format this book has been release on 2006-12-13 with Science categories.
This first systematic summary of the impact of fragment-based approaches on the drug development process provides essential information that was previously unavailable. Adopting a practice-oriented approach, this represents a book by professionals for professionals, tailor-made for drug developers in the pharma and biotech sector who need to keep up-to-date on the latest technologies and strategies in pharmaceutical ligand design. The book is clearly divided into three sections on ligand design, spectroscopic techniques, and screening and drug discovery, backed by numerous case studies.
Fragment Based Methods In Drug Discovery
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Author : Anthony E. Klon
language : en
Publisher:
Release Date : 2015
Fragment Based Methods In Drug Discovery written by Anthony E. Klon and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 2015 with Biomedicine categories.
Annotation This volume covers the techniques necessary for a successful fragment-based drug design project, beginning from defining the problem in terms of preparing the protein model, identifying potential binding sites, and the consideration of various candidate fragments for simulation. The second part discusses the technical aspects that various methods have used to simulate fragment binding to a target protein by using Monte Carlo, molecular dynamics, and docking algorithms. After simulations, fragments are assembled into molecules using a variety of approaches, which are explored next. A discussion of design strategies and consideration of drug-like properties is included as part of the design process at this stage. Finally, several examples of successful fragment-based drug design projects are presented. Written for the "Methods in Molecular Biology" series, this work contains the kind of detailed description and implementation advice to encourage success in the lab.Practical and cutting-edge, "Fragment-Based Methodsin Drug Discovery" takes into account the great accomplishments in the field to provide an ideal guide for researchers continuing to investigate this exciting area of pharmacological study."
Structural Biology In Drug Discovery
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Author : Jean-Paul Renaud
language : en
Publisher: John Wiley & Sons
Release Date : 2020-01-09
Structural Biology In Drug Discovery written by Jean-Paul Renaud and has been published by John Wiley & Sons this book supported file pdf, txt, epub, kindle and other format this book has been release on 2020-01-09 with Medical categories.
With the most comprehensive and up-to-date overview of structure-based drug discovery covering both experimental and computational approaches, Structural Biology in Drug Discovery: Methods, Techniques, and Practices describes principles, methods, applications, and emerging paradigms of structural biology as a tool for more efficient drug development. Coverage includes successful examples, academic and industry insights, novel concepts, and advances in a rapidly evolving field. The combined chapters, by authors writing from the frontlines of structural biology and drug discovery, give readers a valuable reference and resource that: Presents the benefits, limitations, and potentiality of major techniques in the field such as X-ray crystallography, NMR, neutron crystallography, cryo-EM, mass spectrometry and other biophysical techniques, and computational structural biology Includes detailed chapters on druggability, allostery, complementary use of thermodynamic and kinetic information, and powerful approaches such as structural chemogenomics and fragment-based drug design Emphasizes the need for the in-depth biophysical characterization of protein targets as well as of therapeutic proteins, and for a thorough quality assessment of experimental structures Illustrates advances in the field of established therapeutic targets like kinases, serine proteinases, GPCRs, and epigenetic proteins, and of more challenging ones like protein-protein interactions and intrinsically disordered proteins
Making Fragments From Drugs
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Author : Vicki Nienaber
language : en
Publisher: Elsevier
Release Date : 2017-06-01
Making Fragments From Drugs written by Vicki Nienaber and has been published by Elsevier this book supported file pdf, txt, epub, kindle and other format this book has been release on 2017-06-01 with categories.
As a method that offers great benefits in terms of economic viability, rapidity of results and good success rates, fragment-based drug design has quickly been embraced by the drug discovery community. Combining strong coverage of foundational knowledge with expert tips and techniques, Starting simple and keeping it simple: How to make drugs from fragments is designed to provoke new ideas and discussion amongst seasoned professionals, whilst helping those in non-scientific roles to evaluate the opportunities and benefits of implementing fragment-based design at their organizations. Beginning with an introduction to the rules and metrics of fragment-based lead discovery and how to assess their usefulness, the book then reviews methods for prioritizing targets, designing fragment libraries and the potential for combining fragment-based methods with high-throughput screening for the benefit of both. Taking a practical approach to finding fragments is also discussed, followed by fragments finding their own binding sites. Methods for taking simple fragments and optimizing them to simple drug-like candidates are reviewed, followed by a practical overview of why fragments might not develop and optimize as expected. Readers will also learn how parallel processing can help streamline the fragment-to-lead process. The book concludes by asking if the processes and accumulated data can be simplified and standardized to increase the efficiency of fragment-based drug discovery. Under the expert guidance of its pioneering author, Starting simple and keeping it simple: How to Make Drugs From Fragments is both a practical tool for chemists and an accessible guide for their managers to the best ways to implement and optimize fragment-based drug design in their work. Discusses current methods and common issues associated with implementing and optimizing FBLD, supported by practical examples from industry experts Draws on the author's experience bridging academia and industry to present the key practical knowledge needed by relative new-comers to the technology in an accessible way Reviews the need for standardization and highlights implementation options
Structure Based Drug Discovery
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Author : Harren Jhoti
language : en
Publisher: Springer Science & Business Media
Release Date : 2007-05-24
Structure Based Drug Discovery written by Harren Jhoti and has been published by Springer Science & Business Media this book supported file pdf, txt, epub, kindle and other format this book has been release on 2007-05-24 with Science categories.
This book describes some of the most exciting developments for the discovery of new drugs, such as Fragment-based methods. It contains the latest developments in technologies that can be used to obtain the 3-D structures. This book includes experimental approaches using X-ray crystallography and NMR for Fragment-based screening as well as other biophysical methods for studying protein/ligand interactions.