The Design of Covalent-Based Inhibitors

The Design of Covalent-Based Inhibitors PDF Author:
Publisher: Academic Press
ISBN: 0128232463
Category : Science
Languages : en
Pages : 300

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Book Description
Annual Report on Medicinal Chemistry series, highlights new advances in the field with this new volume presenting interesting chapters. Each chapter is written by an international board of authors. - Provides the authority and expertise of leading contributors from an international board of authors - Presents the latest release in the Annual Report on Medicinal Chemistry series - Updated release includes the latest information on The Design of Covalent-Based Inhibitors

The Design of Covalent-Based Inhibitors

The Design of Covalent-Based Inhibitors PDF Author:
Publisher: Academic Press
ISBN: 0128232463
Category : Science
Languages : en
Pages : 300

Get Book Here

Book Description
Annual Report on Medicinal Chemistry series, highlights new advances in the field with this new volume presenting interesting chapters. Each chapter is written by an international board of authors. - Provides the authority and expertise of leading contributors from an international board of authors - Presents the latest release in the Annual Report on Medicinal Chemistry series - Updated release includes the latest information on The Design of Covalent-Based Inhibitors

Biomedical Chemistry

Biomedical Chemistry PDF Author: Nuno Vale
Publisher: Walter de Gruyter GmbH & Co KG
ISBN: 3110468751
Category : Science
Languages : en
Pages : 361

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Book Description
Biomedical Chemistry provides readers with an understanding of how fundamental chemical concepts are used to combat some diseases. The authors explain the interdisciplinary relationship of chemistry with biology, physics, pharmacy and medicine. The results of chemical research can be applied to understand chemical processes in cells and in the body, and new methods for drug transportation. Also, basic chemical ideas and determination of disease etiology are approached by developing techniques to ensure optimum interaction between drugs and human cells. This Book is an excellent resource for students and researchers in health-related fields with frontier topics in medicinal and pharmaceutical chemistry, organic chemistry and biochemistry.

Activity-Based Protein Profiling

Activity-Based Protein Profiling PDF Author: Benjamin F. Cravatt
Publisher: Springer
ISBN: 3030111431
Category : Medical
Languages : en
Pages : 420

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Book Description
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.

Structure-based Design of Drugs and Other Bioactive Molecules

Structure-based Design of Drugs and Other Bioactive Molecules PDF Author: Arun K. Ghosh
Publisher: John Wiley & Sons
ISBN: 3527333657
Category : Medical
Languages : en
Pages : 474

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Book Description
Drug design is a complex, challenging and innovative research area. Structure-based molecular design has transformed the drug discovery approach in modern medicine. Traditionally, focus has been placed on computational, structural or synthetic methods only in isolation. This one-of-akind guide integrates all three skill sets for a complete picture of contemporary structure-based design. This practical approach provides the tools to develop a high-affinity ligand with drug-like properties for a given drug target for which a high-resolution structure exists. The authors use numerous examples of recently developed drugs to present "best practice" methods in structurebased drug design with both newcomers and practicing researchers in mind. By way of a carefully balanced mix of theoretical background and case studies from medicinal chemistry applications, readers will quickly and efficiently master the basic skills of successful drug design. This book is aimed at new and active medicinal chemists, biochemists, pharmacologists, natural product chemists and those working in drug discovery in the pharmaceutical industry. It is highly recommended as a desk reference to guide students in medicinal and chemical sciences as well as to aid researchers engaged in drug design today.

Handbook of In Vivo Chemistry in Mice

Handbook of In Vivo Chemistry in Mice PDF Author: Katsunori Tanaka
Publisher: John Wiley & Sons
ISBN: 3527344322
Category : Science
Languages : en
Pages : 560

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Book Description
Provides timely, comprehensive coverage of in vivo chemical reactions within live animals This handbook summarizes the interdisciplinary expertise of both chemists and biologists performing in vivo chemical reactions within live animals. By comparing and contrasting currently available chemical and biological techniques, it serves not just as a collection of the pioneering work done in animal-based studies, but also as a technical guide to help readers decide which tools are suitable and best for their experimental needs. The Handbook of In Vivo Chemistry in Mice: From Lab to Living System introduces readers to general information about live animal experiments and detection methods commonly used for these animal models. It focuses on chemistry-based techniques to develop selective in vivo targeting methodologies, as well as strategies for in vivo chemistry and drug release. Topics include: currently available mouse models; biocompatible fluorophores; radionuclides for radiodiagnosis/radiotherapy; live animal imaging techniques such as positron emission tomography (PET) imaging; magnetic resonance imaging (MRI); ultrasound imaging; hybrid imaging; biocompatible chemical reactions; ligand-directed nucleophilic substitution chemistry; biorthogonal prodrug release strategies; and various selective targeting strategies for live animals. -Completely covers current techniques of in vivo chemistry performed in live animals -Describes general information about commonly used live animal experiments and detection methods -Focuses on chemistry-based techniques to develop selective in vivo targeting methodologies, as well as strategies for in vivo chemistry and drug release -Places emphasis on material properties required for the development of appropriate compounds to be used for imaging and therapeutic purposes in preclinical applications Handbook of In Vivo Chemistry in Mice: From Lab to Living System will be of great interest to pharmaceutical chemists, life scientists, and organic chemists. It will also appeal to those working in the pharmaceutical and biotechnology industries.

Fragment-Based Drug Discovery

Fragment-Based Drug Discovery PDF Author: Steven Howard
Publisher: Royal Society of Chemistry
ISBN: 1782625658
Category : Medical
Languages : en
Pages : 314

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Book Description
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.

Inhibitors of Protein–Protein Interactions

Inhibitors of Protein–Protein Interactions PDF Author: Ali Tavassoli
Publisher: Royal Society of Chemistry
ISBN: 178801569X
Category : Science
Languages : en
Pages : 357

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Book Description
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.

Accounts in Drug Discovery

Accounts in Drug Discovery PDF Author: Joel Charles Barrish
Publisher: Royal Society of Chemistry
ISBN: 1849731268
Category : Medical
Languages : en
Pages : 397

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Book Description
Accounts in Drug Discovery describes recent case studies in medicinal chemistry with a particular emphasis on how the inevitable problems that arise during any project can be surmounted or overcome. The Editors cover a wide range of therapeutic areas and medicinal chemistry strategies, including lead optimization starting from high-throughput screening "hits" as well as rational, structure-based design. The chapters include "follow-ons" and "next generation" compounds that aim to improve upon first-generation agents. This volume surveys the range of challenges commonly faced by medicinal chemistry researchers, including the optimization of metabolism and pharmacokinetics, toxicology, pharmaceutics and pharmacology, including proof-of-concept in the clinic for novel biological targets. The case studies include medicinal chemistry stories on recently approved and marketed drugs, but also chronicle "near-misses", i.e. exemplary compounds that may have proceeded well into the clinic but for various reasons did not result in a successful registration. As the vast majority of projects fail prior to registration, much can be learned from such narratives. By sharing a wide range of drug discovery experiences and information across the community of medicinal chemists in both industry and academia, the Editors believe that these accounts will provide insights into the art of medicinal chemistry as it is currently practiced and will help to serve the needs of active medicinal chemists.

Fragment-based Approaches in Drug Discovery

Fragment-based Approaches in Drug Discovery PDF Author: Wolfgang Jahnke
Publisher: John Wiley & Sons
ISBN: 3527608605
Category : Science
Languages : en
Pages : 391

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Book Description
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 Drug Discovery

Fragment-based Drug Discovery PDF Author: Daniel A. Erlanson
Publisher: John Wiley & Sons
ISBN: 352733775X
Category : Medical
Languages : en
Pages : 524

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Book Description
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.