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Peptide Chemistry and Drug Design

Peptide Chemistry and Drug Design
Author: Ben M. Dunn
Publisher: John Wiley & Sons
Total Pages: 336
Release: 2015-02-02
Genre: Medical
ISBN: 1118995287

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This book focuses on peptides as drugs, a growing area ofpharmaceutical research and development. It helps readers solveproblems of discovering, developing, producing, and deliveringpeptide-based drugs. • Identifies promising new areas in peptide drugdiscovery • Includes chapters on discovery from natural sources,metabolic modification, and drug delivery • Overviews separation methods and techniques foranalysis, bond formation, and purification • Offers readers both a professional reference and atext or resource for graduate-level students


Peptide-based Drug Discovery

Peptide-based Drug Discovery
Author: Ved Srivastava
Publisher: Royal Society of Chemistry
Total Pages: 589
Release: 2017-06-22
Genre: Science
ISBN: 1788011716

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With potentially high specificity and low toxicity, biologicals offer promising alternatives to small-molecule drugs. Peptide therapeutics have again become the focus of innovative drug development efforts backed up by a resurgence of venture funds and small biotechnology companies. What does it take to develop a peptide-based medicine? What are the key challenges and how are they overcome? What are emerging therapeutics for peptide modalities? This book answers these questions with a holistic story from molecules to medicine, combining the themes of design, synthesis and clinical applications of peptide-based therapeutics and biomarkers. Chapters are written and edited by leaders in the field from industry and academia and they cover the pharmacokinetics of peptide therapeutics, attributes necessary for commercially successful metabolic peptides, medicinal chemistry strategies for the design of peptidase-resistant peptide analogues, disease classes for which peptide therapeutic are most relevant, and regulatory issues and guidelines. The critical themes covered provide essential background information on what it takes to develop peptide-based medicine from a chemistry perspective and views on the future of peptide drugs. This book will be a valuable resource not only as a reference book for the researcher engaged in academic and pharmaceutical setting, from basic research to manufacturing and from organic chemistry to biotechnology, but also a valuable resource to graduate students to understand discovery and development process for peptide-based medicine.


Peptide Therapeutics

Peptide Therapeutics
Author: Ved Srivastava
Publisher: Royal Society of Chemistry
Total Pages: 572
Release: 2019-08-28
Genre: Science
ISBN: 1788014332

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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.


Peptidomimetics in Organic and Medicinal Chemistry

Peptidomimetics in Organic and Medicinal Chemistry
Author: Antonio Guarna
Publisher: John Wiley & Sons
Total Pages: 334
Release: 2014-03-14
Genre: Science
ISBN: 1118683145

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A peptidomimetic is a small protein-like chain designed to mimic a peptide with adjusted molecular properties such as enhanced stability or biological activity. It is a very powerful approach for the generation of small-molecule-based drugs as enzyme inhibitors or receptor ligands. Peptidomimetics in Organic and Medicinal Chemistry outlines the concepts and synthetic strategies underlying the building of bioactive compounds of a peptidomimetic nature. Topics covered include the chemistry of unnatural amino acids, peptide- and scaffold-based peptidomimetics, amino acid-side chain isosteres, backbone isosteres, dipeptide isosteres, beta-turn peptidomimetics, proline-mimetics as turn inducers, cyclic scaffolds, amino acid surrogates, and scaffolds for combinatorial chemistry of peptidomimetics. Case studies in the hit-to-lead process, such as the development of integrin ligands and thrombin inhibitors, illustrate the successful application of peptidomimetics in drug discovery.


Peptide Drug Discovery and Development

Peptide Drug Discovery and Development
Author: Miguel Castanho
Publisher: John Wiley & Sons
Total Pages: 547
Release: 2011-10-24
Genre: Medical
ISBN: 3527636749

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Filling a real knowledge gap, this handbook and ready reference is both modern and forward-looking in its emphasis on the "bench to bedside" translational approach to drug development. Clearly structured into three major parts, the book stakes out the boundaries of peptide drug development in the preclinical as well as clinical stages. The first part provides a general background and focuses on the characteristic strengths and weaknesses of peptide drugs. The second section contains five cases studies of peptides from diverse therapeutic fields, and the lessons to be learned from them, while the final part looks at new targets and opportunities, discussing several drug targets and diseases for which peptide drugs are currently being developed.


Peptide-Based Drug Design

Peptide-Based Drug Design
Author: Laszlo Otvos
Publisher: Humana Press
Total Pages: 0
Release: 2010-11-19
Genre: Medical
ISBN: 9781617378690

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Due to their high specificity and low toxicity profile, peptides have once again become central to the development of new drugs. In Peptide-Based Drug Design: Methods and Protocols, expert researchers provide a handbook which offers a selection of research and production tools suitable for transforming a promising protein fragment or stand-alone native peptide into a pharmaceutically acceptable composition. The volume delves into contemporary, cutting-edge subjects such as hit isolation and target validation, computer-aided design, sequence modifications to satisfy pharmacologists, in vivo stability and imaging, and the actual production of difficult sequences. Written in the highly successful Methods in Molecular BiologyTM series format, chapters include readily reproducible, step-by-step laboratory protocols, lists of materials, and the Notes section, which highlights tips on troubleshooting and avoiding known pitfalls. Comprehensive and up-to-date, Peptide-Based Drug Design: Methods and Protocols shows its subject to be an independent science on the rise, and provides scientists with a clear, concise guide for continuing this vital research.


Peptide and Protein Design for Biopharmaceutical Applications

Peptide and Protein Design for Biopharmaceutical Applications
Author: Knud Jensen
Publisher: John Wiley & Sons
Total Pages: 306
Release: 2009-09-01
Genre: Science
ISBN: 9780470749715

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Peptides serve as effective drugs in the clinic today. However the inherent drawbacks of peptide structures can limit their efficacy as drugs. To overcome this researchers are developing new methods to create ‘tailor-made’ peptides and proteins with improved pharmacological properties. Design of Peptides and Proteins provides an overview of the experimental and computational methods for peptide and protein design, with an emphasis on specific applications for therapeutics and biomedical research. Topics covered include: Computer modeling of peptides and proteins Peptidomimetics Design and synthesis of cyclic peptides Carbohydrates in peptide and protein design De novo design of peptides and proteins Medical development applications An extended case study – the design of insulin variants Design of Peptides and Proteins presents the state-of-the-art of this exciting approach for therapeutics, with contributions from international experts. It is an essential resource for academic and industrial scientists in the fields of peptide and protein drug design, biomedicine, biochemistry, biophysics, molecular modelling, synthetic organic chemistry and medicinal/pharmaceutical chemistry.


Peptide Therapeutics

Peptide Therapeutics
Author: Seetharama D. Jois
Publisher: Springer Nature
Total Pages: 321
Release: 2022-09-26
Genre: Medical
ISBN: 3031045440

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This book explains how peptide-based drug design works, what steps are needed to develop a peptide-based therapeutic, and challenges in synthesis as well as regulatory issues. It covers the design concept of peptide therapeutics from fundamental principles using structural biology and computational approaches. The chapters are arranged in a linear fashion. A fresh graduate or a scientist who works on small molecules can use this to follow the design and development of peptide therapeutics to use as understanding the basic concepts. Each chapter is written by experts from academia as well as industry. Rather than covering extensive literature, the book provides concepts of design, synthesis, delivery, as well as regulatory affairs and manufacturing of peptides in a systematic way with examples in each case. The book can be used as a reference for a pharmaceutical or biomedical scientist or graduate student who wants to pursue their career in peptide therapeutics. Some chapters will be written as a combination of basic principles and protocol so that scientists can adopt these methods to their research work. The examples provided can be used to perform peptide formulation considerations for the designed peptides. The book has nine chapters, and each chapter can be read as an independent unit on a particular concept.


Application of Peptide-Based Prodrug Chemistry in Drug Development

Application of Peptide-Based Prodrug Chemistry in Drug Development
Author: Arnab De
Publisher: Springer Science & Business Media
Total Pages: 89
Release: 2012-08-18
Genre: Medical
ISBN: 1461448751

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Macromolecular (specifically peptide-based) drugs could potentially be highly effective medicines. However they have a relatively short duration of action and variable therapeutic index. An example of such a peptide is Glucagon-like Peptide I which could potentially be used as a revolutionary drug for diabetes. This is because it stimulates insulin only when the blood glucose level is high thereby reducing the risk of hypoglycemia (a significant disadvantage of using insulin is that an insulin overdose is the single most potent cause of life-threatening hypoglycemia). However it’s short duration of action (half-life of 2 minutes in plasma) precludes its therapeutic use. In this volume, the use of novel therapeutics like GLP1 as an alternative to tradition insulin-based drugs in diabetes is described. Application of Peptide-Based Prodrug Chemistry in Drug Development elucidates the traditional concept of prodrugs as “specialized non-toxic protective groups used in a transient manner to alter or to eliminate certain limiting properties in the parent small molecule” (IUPAC definition). It goes on to provide insight into how prodrugs of peptides (with GLP1 as an example) could be appropriately used to extend the biological half life, broaden the therapeutic index of macromolecules and improve the pharmacodynamics of such drugs. Author explains the logic behind designing peptide prodrugs, synthetic procedures and bioassays to examine the conversion of the prodrug to the drug under therapeutic conditions. The prodrugs described slowly convert to the parent drug at physiological conditions of 37C and pH 7.2 driven by their inherent chemical instability without the need of any enzymatic cleavage. The diketopiperazine and diketomorpholine (DKP and DMP) strategies for prodrug conversion are demonstrated in detail with special emphasis on the chemical flexibility that it offers to develop prodrugs with variable time actions. This book will be of useful to chemists, biochemists, medicinal chemists, biologists and people in the medical profession (doctors). It may be used in undergraduate classes but will certainly help post-graduate students and advanced professionals. The author is grateful to Prof. Richard DiMarchi (Standiford H. Cox Professor of Chemistry and the Linda & Jack Gill Chair in Biomolecular Sciences at Indiana University) for valuable suggestions. The foreword for the book has been written by Prof. Jean Martinez, (Legion d'Honneur awarded by the French Republic; Professor of Chemistry and Medicinal Chemistry of the University of Montpellier, France; and Chairman of European Peptide Society, 2002-2010).


De Novo Peptide Design

De Novo Peptide Design
Author: Vibin Ramakrishnan
Publisher: Academic Press
Total Pages: 297
Release: 2022-09-17
Genre: Science
ISBN: 0323985432

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De novo Peptide Design: Principles and Applications presents the latest developments in the fields of therapeutic peptides and bio-nanotechnology. The title focuses on the design of peptides, particularly how peptides may be tailored to specific functions. It includes computational and experimental protocols to assist in the design of peptides. Sections cover the basics of protein and peptide structure, modeling and simulation, solid phase peptide synthesis, peptide-based antibiotics, drug delivery, peptide nanomaterials, aromatic interactions directing nano-assembly, protein/peptide aggregation, therapeutic interventions against protein/peptide aggregation diseases, peptide based hydrogels, computational tools and algorithms for peptide design, and experimental protocols in peptide chemistry. In addition, the book covers key aspects in peptide design, providing a solution for researchers working within the 'peptidic universe' to create new therapeutic agents. Gives comprehensive coverage, including peptide design, modeling, synthesis and applications Presents emerging topics in the design of peptide-based therapeutics Details the latest developments in the fields of therapeutic peptides and bio-nanotechnology Considers peptide design and the tailoring of peptides to specific functions Offers computational tools and algorithms for peptide design and experimental protocols for peptide chemistry