Piperidine Based Drug Discovery

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Piperidine-Based Drug Discovery

Author : Ruben Vardanyan
Publisher : Elsevier
ISBN 13 : 0128134283
Total Pages : 358 pages
Book Rating : 4.1/5 (281 download)

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Book Synopsis Piperidine-Based Drug Discovery by : Ruben Vardanyan

Download or read book Piperidine-Based Drug Discovery written by Ruben Vardanyan and published by Elsevier. This book was released on 2017-06-12 with total page 358 pages. Available in PDF, EPUB and Kindle. Book excerpt: Piperidine-Based Drug Discovery outlines the complexities of Piperidine scaffold use in drug discovery, including derivative chemistry, structural properties, methods of synthesis and practical implementations. Piperidine scaffolds are the cornerstones of over 70 commercialized drugs (including multiple blockbusters). Designed as a guide for both experts and students working in this and related areas, it is hoped that this volume will encourage and inspire the continued design and development of novel pharmaceuticals based on Piperidine and its derivatives. Heterocyclic compounds are of central importance to medicinal chemistry, as demonstrated by the high percentage of marketable drugs that feature heterocyclic fragments in their structures. As starting points for drug discovery they offer a broad range of attractive properties, and a detailed understanding of the particular characteristics of each is of great benefit to researchers. The most commonly used heterocycle among US FDA approved pharmaceuticals, Piperidine is an extremely important building block in the synthesis of medicinal agents. This heterocycle and its derivatives exhibit a number of important functionalities and have been employed variously as CNS modulators, antiaggregants, anticoagulants, antihistamines, anti-cancer drugs and analgesics. Explores this extremely important heterocycle to a high level of detail Describes synthesis methods for 70 current drugs based on Piperidine scaffolds Gives drug designers all the key knowledge required to develop new drugs utilizing Piperidine Provides pharmacologists a solid overview of the chemical background of existing Piperidine-based drugs

Privileged Structures in Drug Discovery

Author : Larry Yet
Publisher : John Wiley & Sons
ISBN 13 : 1118145666
Total Pages : 560 pages
Book Rating : 4.1/5 (181 download)

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Book Synopsis Privileged Structures in Drug Discovery by : Larry Yet

Download or read book Privileged Structures in Drug Discovery written by Larry Yet and published by John Wiley & Sons. This book was released on 2018-03-27 with total page 560 pages. Available in PDF, EPUB and Kindle. Book excerpt: A comprehensive guide to privileged structures and their application in the discovery of new drugs The use of privileged structures is a viable strategy in the discovery of new medicines at the lead optimization stages of the drug discovery process. Privileged Structures in Drug Discovery offers a comprehensive text that reviews privileged structures from the point of view of medicinal chemistry and contains the synthetic routes to these structures. In this text, the author—a noted expert in the field—includes an historical perspective on the topic, presents a practical compendium to privileged structures, and offers an informed perspective on the future direction for the field. The book describes the up-to-date and state-of-the-art methods of organic synthesis that describe the use of privileged structures that are of most interest. Chapters included information on benzodiazepines, 1,4-dihydropyridines, biaryls, 4-(hetero)arylpiperidines, spiropiperidines, 2-aminopyrimidines, 2-aminothiazoles, 2-(hetero)arylindoles, tetrahydroisoquinolines, 2,2-dimethylbenzopyrans, hydroxamates, and bicyclic pyridines containing ring-junction nitrogen as privileged scaffolds in medicinal chemistry. Numerous, illustrative case studies document the current use of the privileged structures in the discovery of drugs. This important volume: Describes the drug compounds that have successfully made it to the marketplace and the chemistry associated with them Offers the experience from an author who has worked in many therapeutic areas of medicinal chemistry Details many of the recent developments in organic chemistry that prepare target molecules Includes a wealth of medicinal chemistry case studies that clearly illustrate the use of privileged structures Designed for use by industrial medicinal chemists and process chemists, academic organic and medicinal chemists, as well as chemistry students and faculty, Privileged Structures in Drug Discovery offers a current guide to organic synthesis methods to access the privileged structures of interest, and contains medicinal chemistry case studies that document their application.

Drug Discovery with Privileged Building Blocks

Author : Jie Jack Li
Publisher : CRC Press
ISBN 13 : 1000416011
Total Pages : 320 pages
Book Rating : 4.0/5 (4 download)

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Book Synopsis Drug Discovery with Privileged Building Blocks by : Jie Jack Li

Download or read book Drug Discovery with Privileged Building Blocks written by Jie Jack Li and published by CRC Press. This book was released on 2021-10-21 with total page 320 pages. Available in PDF, EPUB and Kindle. Book excerpt: Drug Discovery with Privileged Building Blocks traces back PharmaBlock’s founding philosophy of designing privileged building blocks. High-quality building blocks are crucial not only to biological activities of different molecules but also to ADMET properties, which eventually will impact the success rate of drug discovery projects. A thorough study of how building blocks perform in drug molecules and a regular analysis of new building block structures in the latest researches have proven to be a fruitful strategy to generate novel building blocks. Using this strategy, PharmaBlock has supplied the drug industry with a great number of building blocks, which are increasingly being adopted by drug hunters, and these are identified in this book. Each chapter may be read and studied without learning the previous chapters. This book will be a good starting point for novice medicinal chemists, and veteran medicinal chemists will find it useful as well. Key Feature The book covers privileged building blocks appearing most frequently on patents for novel drugs. The latest relevant tactics are explained in the context of drug design and medicinal chemistry. Key synthesis, especially large-scale synthesis, is described. The most recent literature references are cited.

Successful Drug Discovery, Volume 1

Author : János Fischer
Publisher : John Wiley & Sons
ISBN 13 : 3527336850
Total Pages : 258 pages
Book Rating : 4.5/5 (273 download)

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Book Synopsis Successful Drug Discovery, Volume 1 by : János Fischer

Download or read book Successful Drug Discovery, Volume 1 written by János Fischer and published by John Wiley & Sons. This book was released on 2015-05-04 with total page 258 pages. Available in PDF, EPUB and Kindle. Book excerpt: The first volume of the book series "Successful Drug Discovery" is focusing on new drug discoveries during the last decade, from established drugs to recently introduced drugs of all kinds: small-molecule-, peptide-, and protein-based drugs. The role of serendipity is analyzed in some very successful drugs where the research targets of the lead molecule and the drug are different. Phenotypic and target-based drug discovery approaches are discussed from the viewpoint of pioneer drugs and analogues. This volume gives an excellent overview of insulin analogues including a discussion of the properties of rapid-acting and long-acting formulations of this important hormone. The major part of the book is devoted to case histories of new drug discoveries described by their key inventors. Eight case histories range across many therapeutic fields. The goal of this book series is to help the participants of the drug research community with a reference book series and to support teaching in medicinal chemistry with case histories and review articles of new drugs.

Structure-based Design of Drugs and Other Bioactive Molecules

Author : Arun K. Ghosh
Publisher : John Wiley & Sons
ISBN 13 : 3527333657
Total Pages : 474 pages
Book Rating : 4.5/5 (273 download)

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Book Synopsis Structure-based Design of Drugs and Other Bioactive Molecules by : Arun K. Ghosh

Download or read book Structure-based Design of Drugs and Other Bioactive Molecules written by Arun K. Ghosh and published by John Wiley & Sons. This book was released on 2014-08-11 with total page 474 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Progress in Drug Research

Author : Ernst Jucker
Publisher : Springer Science & Business Media
ISBN 13 : 9783764360283
Total Pages : 314 pages
Book Rating : 4.3/5 (62 download)

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Book Synopsis Progress in Drug Research by : Ernst Jucker

Download or read book Progress in Drug Research written by Ernst Jucker and published by Springer Science & Business Media. This book was released on 1999 with total page 314 pages. Available in PDF, EPUB and Kindle. Book excerpt: Progress in Drug Research is a prestigious book series which provides extensive expert-written reviews on a wide spectrum of highly topical areas in current pharmaceutical and pharmacological research. It serves as an important source of information for researchers concerned with drug research and all those who need to keep abreast of the many recent developments in the quest for new and better medicines.

Fragment-Based Drug Discovery

Author : Steven Howard
Publisher : Royal Society of Chemistry
ISBN 13 : 1849739080
Total Pages : 314 pages
Book Rating : 4.8/5 (497 download)

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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 2015-07-03 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.

Heterocyclic Chemistry in Drug Discovery

Author : Jie Jack Li
Publisher : John Wiley & Sons
ISBN 13 : 1118148908
Total Pages : 0 pages
Book Rating : 4.1/5 (181 download)

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Book Synopsis Heterocyclic Chemistry in Drug Discovery by : Jie Jack Li

Download or read book Heterocyclic Chemistry in Drug Discovery written by Jie Jack Li and published by John Wiley & Sons. This book was released on 2013-04-15 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: Enables researchers to fully realize the potential to discover new pharmaceuticals among heterocyclic compounds Integrating heterocyclic chemistry and drug discovery, this innovative text enables readers to understand how and why these two fields go hand in hand in the effective practice of medicinal chemistry. Contributions from international leaders in the field review more than 100 years of findings, explaining their relevance to contemporary drug discovery practice. Moreover, these authors have provided plenty of practical guidance and tips based on their own academic and industrial laboratory experience, helping readers avoid common pitfalls. Heterocyclic Chemistry in Drug Discovery is ideal for readers who want to fully realize the almost limitless potential to discover new and effective pharmaceuticals among heterocyclic compounds, the largest and most varied family of organic compounds. The book features: Several case studies illustrating the role and application of 3, 4, 5, and 6+ heterocyclic ring systems in drug discovery Step-by-step descriptions of synthetic methods and practical techniques Examination of the physical properties for each heterocycle, including NMR data and quantum calculations Detailed explanations of the complexity and intricacies of reactivity and stability for each class of heterocycles Heterocyclic Chemistry in Drug Discovery is recommended as a textbook for organic and medicinal chemistry courses, particularly those emphasizing heterocyclic chemistry. The text also serves as a guide for medicinal and process chemists in the pharmaceutical industry, offering them new insights and new paths to explore for effective drug discovery.

The Combinatorial Index

Author : Barry A. Bunin
Publisher : Elsevier
ISBN 13 : 0080542409
Total Pages : 341 pages
Book Rating : 4.0/5 (85 download)

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Book Synopsis The Combinatorial Index by : Barry A. Bunin

Download or read book The Combinatorial Index written by Barry A. Bunin and published by Elsevier. This book was released on 1998-04-15 with total page 341 pages. Available in PDF, EPUB and Kindle. Book excerpt: With the explosion of combinatorial solid-phase methods, access to information has become one of the main barriers facing a synthetic chemist who is contemplating a combinatorial approach to a medicinal chemistry problem. The Combinatorial Index is an answer to that problem. This compendium of methods from the primary literature provides quick and convenient access to reliable synthetic transformations as well as information on linkers and analytical methods. Each synthetic procedure is preceded by a section entitled"Points of Interest,"which highlights the strengths and weaknesses of the various studies. The index also covers the use of solution-based synthesis for the generation of molecular diversity. Organized for rapid retrieval of published information on classes of synthetic transformations, linkers, and analytical methods Serves as a laboratory manual for bench chemists Includes a chapter on linkers to assist in choice of linking strategy Discusses strengths and limitations of the various methods Contains a structural index showing functional group transformations in solid-phase synthesis

Privileged Scaffolds in Medicinal Chemistry

Author : Stefan Bräse
Publisher : Royal Society of Chemistry
ISBN 13 : 1782620303
Total Pages : 486 pages
Book Rating : 4.7/5 (826 download)

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Book Synopsis Privileged Scaffolds in Medicinal Chemistry by : Stefan Bräse

Download or read book Privileged Scaffolds in Medicinal Chemistry written by Stefan Bräse and published by Royal Society of Chemistry. This book was released on 2015-11-20 with total page 486 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book addresses the various classes of privileged scaffolds and covers the history of their discovery and use.

Drug-like Properties: Concepts, Structure Design and Methods

Author : Li Di
Publisher : Elsevier
ISBN 13 : 0080557619
Total Pages : 549 pages
Book Rating : 4.0/5 (85 download)

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Book Synopsis Drug-like Properties: Concepts, Structure Design and Methods by : Li Di

Download or read book Drug-like Properties: Concepts, Structure Design and Methods written by Li Di and published by Elsevier. This book was released on 2010-07-26 with total page 549 pages. Available in PDF, EPUB and Kindle. Book excerpt: Of the thousands of novel compounds that a drug discovery project team invents and that bind to the therapeutic target, typically only a fraction of these have sufficient ADME/Tox properties to become a drug product. Understanding ADME/Tox is critical for all drug researchers, owing to its increasing importance in advancing high quality candidates to clinical studies and the processes of drug discovery. If the properties are weak, the candidate will have a high risk of failure or be less desirable as a drug product. This book is a tool and resource for scientists engaged in, or preparing for, the selection and optimization process. The authors describe how properties affect in vivo pharmacological activity and impact in vitro assays. Individual drug-like properties are discussed from a practical point of view, such as solubility, permeability and metabolic stability, with regard to fundamental understanding, applications of property data in drug discovery and examples of structural modifications that have achieved improved property performance. The authors also review various methods for the screening (high throughput), diagnosis (medium throughput) and in-depth (low throughput) analysis of drug properties. Serves as an essential working handbook aimed at scientists and students in medicinal chemistry Provides practical, step-by-step guidance on property fundamentals, effects, structure-property relationships, and structure modification strategies Discusses improvements in pharmacokinetics from a practical chemist's standpoint

Synthesis of Essential Drugs

Author : Ruben Vardanyan
Publisher : Elsevier
ISBN 13 : 008046212X
Total Pages : 635 pages
Book Rating : 4.0/5 (84 download)

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Book Synopsis Synthesis of Essential Drugs by : Ruben Vardanyan

Download or read book Synthesis of Essential Drugs written by Ruben Vardanyan and published by Elsevier. This book was released on 2006-03-10 with total page 635 pages. Available in PDF, EPUB and Kindle. Book excerpt: Synthesis of Essential Drugs describes methods of synthesis, activity and implementation of diversity of all drug types and classes. With over 2300 references, mainly patent, for the methods of synthesis for over 700 drugs, along with the most widespread synonyms for these drugs, this book fills the gap that exists in the literature of drug synthesis. It provides the kind of information that will be of interest to those who work, or plan to begin work, in the areas of biologically active compounds and the synthesis of medicinal drugs. This book presents the synthesis of various groups of drugs in an order similar to that traditionally presented in a pharmacology curriculum. This was done with a very specific goal in mind – to harmonize the chemical aspects with the pharmacology curriculum in a manner useful to chemists. Practically every chapter begins with an accepted brief definition and description of a particular group of drugs, proposes their classification, and briefly explains the present model of their action. This is followed by a detailed discussion of methods for their synthesis. Of the thousands of drugs existing on the pharmaceutical market, the book mainly covers generic drugs that are included in the WHO’s Essential List of Drugs. For practically all of the 700+ drugs described in the book, references (around 2350) to the methods of their synthesis are given along with the most widespread synonyms. Synthesis of Essential Drugs is an excellent handbook for chemists, biochemists, medicinal chemists, pharmacists, pharmacologists, scientists, professionals, students, university libraries, researchers, medical doctors and students, and professionals working in medicinal chemistry. * Provides a brief description of methods of synthesis, activity and implementation of all drug types* Includes synonyms* Includes over 2300 references

Opioids and Their Receptors

Author : Mariana Spetea
Publisher : MDPI
ISBN 13 : 3036500464
Total Pages : 358 pages
Book Rating : 4.0/5 (365 download)

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Book Synopsis Opioids and Their Receptors by : Mariana Spetea

Download or read book Opioids and Their Receptors written by Mariana Spetea and published by MDPI. This book was released on 2020-12-18 with total page 358 pages. Available in PDF, EPUB and Kindle. Book excerpt: The interest in opioids such as morphine, the prototypical opioid ligand, has been maintained through the years. The identification of endogenous opioids and their receptors (mu, delta, kappa, and nociceptin), molecular cloning, and the elucidation of the crystal structures of opioid receptors represent key milestones in opioid research. The opioid system modulates numerous pharmacological responses, with therapeutic (i.e., analgesia) and detrimental side effects (i.e., addiction). The medical use and misuse of opioids have dramatically increased, leading to the 21st century opioid crisis. This book presents recent developments in opioid drug discovery, specifically in the medicinal chemistry and pharmacology of new ligands targeting the opioid receptors as effective and safe therapeutics for human diseases. Furthermore, it draws a special attention to advancing concepts and strategies in opioid drug discovery to mitigate opioid liabilities. The diversity among the discussed topics is a testimony to the complexity of the opioid system, which results from the expression, regulation, and functional role of ligands and receptors. The array of multidisciplinary research areas illustrates the rapidly developing basic research and translational activities in opioid drug discovery. This book will serve as a useful reference while also stimulating continued research in the chemistry and pharmacology of opioids and their receptors, with the prospect of developing improved therapies for human diseases, but also improving health and quality of life in general.

Pyridines: from lab to production

Author : Eric F.V. Scriven
Publisher : Academic Press
ISBN 13 : 0123852366
Total Pages : 582 pages
Book Rating : 4.1/5 (238 download)

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Book Synopsis Pyridines: from lab to production by : Eric F.V. Scriven

Download or read book Pyridines: from lab to production written by Eric F.V. Scriven and published by Academic Press. This book was released on 2013-01-08 with total page 582 pages. Available in PDF, EPUB and Kindle. Book excerpt: Provides a synthetic armory of tools to aid the practicing chemist by reviewing the most reliable historical methods alongside new methods/ Written by scientists who have actually used these in synthesis. By emphasizing tricks and tips to optimize reactions for the best yields and purity, which are often missing from the primary literature, this book provides another dimension for the synthetic chemist. A combined academic and industrial approach evaluates the best methods for different scales of reaction and discusses practical tips (e.g. when to stop a reaction early to maximize purity or when to re-use side products). Chapters also assess whether to make or source starting materials, how to connect them and what are the best synthetic routes. The book is designed to be a stand-alone reference, but also provides cross references to leading reviews and the Comprehensive Heterocyclic Chemistry reference works for those who want to learn more. Reviews tried and tested practical methods to help the reader select the best method for their research Includes tips, tricks and hints to enable the reader to get the best yield or cleanest product out of their reaction for synthesising or transforming a pyridine derivative Written by both academic researchers and industry leaders this provides a unique view of how to get the most out of a reaction no matter what scale you are running this on

Synthetic Methods in Drug Discovery

Author : David C Blakemore
Publisher : Royal Society of Chemistry
ISBN 13 : 178262791X
Total Pages : 517 pages
Book Rating : 4.7/5 (826 download)

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Book Synopsis Synthetic Methods in Drug Discovery by : David C Blakemore

Download or read book Synthetic Methods in Drug Discovery written by David C Blakemore and published by Royal Society of Chemistry. This book was released on 2016-07-15 with total page 517 pages. Available in PDF, EPUB and Kindle. Book excerpt: Building on key reactions presented in Volume 1, Synthetic Methods in Drug Discovery Volume 2 covers a range of important reaction types including organometallic chemistry, fluorination approaches and asymmetric methods as well as new and exciting areas such as Csp2-Csp3 couplings, catalytic amide bond forming reactions, hydrogen borrowing chemistry and methods to access novel motifs and monomers. This book provides both academic and industrial perspectives on key reactions giving the reader an excellent overview of the techniques used in modern synthesis. Reaction types are conveniently framed in the context of their value to industry and the challenges and limitations of methodologies are discussed with relevant illustrative examples. Moreover, key opportunities in expanding chemical space are presented, including the increasingly important syntheses that introduce three-dimensional molecular shape. Edited and authored by leading scientists from both academia and industry, this book will be a valuable reference for all chemists involved in drug discovery as well as postgraduate students in medicinal chemistry.

Structural Biology in Drug Discovery

Author : Jean-Paul Renaud
Publisher : John Wiley & Sons
ISBN 13 : 1118900502
Total Pages : 1367 pages
Book Rating : 4.1/5 (189 download)

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Book Synopsis Structural Biology in Drug Discovery by : Jean-Paul Renaud

Download or read book Structural Biology in Drug Discovery written by Jean-Paul Renaud and published by John Wiley & Sons. This book was released on 2020-01-09 with total page 1367 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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

Peptide Therapeutics

Author : Ved Srivastava
Publisher : Royal Society of Chemistry
ISBN 13 : 1788014332
Total Pages : 572 pages
Book Rating : 4.7/5 (88 download)

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Book Synopsis Peptide Therapeutics by : Ved Srivastava

Download or read book Peptide Therapeutics written by Ved Srivastava and published by Royal Society of Chemistry. This book was released on 2019-08-28 with total page 572 pages. Available in PDF, EPUB and Kindle. Book excerpt: Peptide therapy has become a key strategy in innovative drug development, however, one of the potential barriers for the development of novel peptide drugs in the clinic is their deficiencies in clearly defined chemistry, manufacturing and controls (CMC) strategy from clinical development to commercialization. CMC can often become a rate-limiting step due to lack of knowledge and lack of a formal policy or guidelines on CMC for peptide-based drugs. Regulators use a risk-based approach, reviewing applications on a case-by-case basis. Peptide Therapeutics: Strategy and Tactics for Chemistry, Manufacturing, and Controls covers efficient manufacturing of peptide drug substances, a review of the process for submitting applications to the regulatory authority for drug approval, a holistic approach for quality attributes and quality control from a regulatory perspective, emerging analytical tools for the characterisation of impurities, and the assessment of stability. This book is an essential reference work for students and researchers, in both academia and industry, with an interest in learning about CMC, and facilitating development and manufacture of peptide-based drugs.