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

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.

Peptides

Peptides
Author: Bernd Gutte
Publisher: Elsevier
Total Pages: 527
Release: 1995-10-24
Genre: Science
ISBN: 0080538592

In recent years, research has shown the importance of peptides in neuroscience, immunology, and cell biology. Active research programs worldwide are now engaged in developing peptide-based drugs and vaccines using modification of natural peptides and proteins, design of artificial peptides and peptide mimetics, and screening of peptide and phage libraries. In this comprehensive book, the authors discuss peptide synthesis and application within the context of their increasing importance to the pharmaceutical industry. Peptides: Synthesis, Structures, and Applications explores the broad growth of information in modern peptide synthetic methods and the structure-activity relationships of synthetic polypeptides. - The history of peptide chemistry - Amide formation, deprotection, and disulfide formation in peptide synthesis - Solid-phase peptide synthesis - a-helix formation by peptides in water - Stability and dynamics of peptide conformation - An overview of structure-function studies of peptide hormones - Neuropeptides:peptide and nonpeptide analogs - Reversible inhibitors of serine proteinases - Design of polypeptides - Current capabilities and future possibilities of soluble chemical combinatorial libraries - Epitope mapping with peptides - Synthesis and applications of branched peptides in immunological methods and vaccines

Chemical Approaches to the Synthesis of Peptides and Proteins

Chemical Approaches to the Synthesis of Peptides and Proteins
Author: Paul Lloyd-Williams
Publisher: CRC Press
Total Pages: 306
Release: 2020-08-18
Genre: Cooking
ISBN: 1000151689

Organic chemists working on the synthesis of natural products have long found a special challenge in the preparation of peptides and proteins. However, more reliable, more efficient synthetic preparation methods have been developed in recent years. This reference evaluates the most important synthesis methods available today, and also considers methods that show promise for future applications. This text describes the state of the art in efficient synthetic methods for the synthesis of both natural and artificial large peptide and protein molecules. Subjects include an introduction to basic topics, linear solid-phase synthesis of peptides, peptide synthesis in solution, convergent solid-phase synthesis, methods for the synthesis of branched peptides, formation of disulfide bridges, and more. The book emphasizes strategies and tactics that must be considered for the successful synthesis of peptides.

Conformation in Biology and Drug Design

Conformation in Biology and Drug Design
Author: Sidney Udenfriend
Publisher: Elsevier
Total Pages: 516
Release: 2014-05-10
Genre: Science
ISBN: 1483218007

The Peptides: Analysis, Synthesis, Biology, Volume 7: Conformation in Biology and Drug Design focuses on the analysis of peptides, emphasizing the use of physical methods in peptide conformational analysis and the relationship of conformational properties of peptides to biological properties. This book consists of nine chapters. Chapter 1 provides a brief overview of the perspective on the application of physical methods to peptide conformational analysis. The use of circular dichroism (CD) spectroscopy to examine the conformational properties of peptides in solution is elaborated in Chapter 2, while the use of fluorescence spectroscopy to examine the special relationships of aromatic side-chain groups to one another is discussed in Chapter 3. In Chapter 4, the use of various theoretical methods to calculate the conformations of peptides is described. The methods used to stimulate peptide conformations and dynamics are outlined in Chapter 5. The last four chapters examine various aspects of the use of nuclear magnetic resonance (NMR) in peptide conformational analysis. This volume is suitable for biologists, specialists, and researchers interested in peptides and proteins.

Peptide Synthesis

Peptide Synthesis
Author: Miklos Bodanszky
Publisher: John Wiley & Sons
Total Pages: 230
Release: 1976
Genre: Science
ISBN: