Practical Medicinal Chemistry with Macrocycles


Book Description

Including case studies of macrocyclic marketed drugs and macrocycles in drug development, this book helps medicinal chemists deal with the synthetic and conceptual challenges of macrocycles in drug discovery efforts. Provides needed background to build a program in macrocycle drug discovery –design criteria, macrocycle profiles, applications, and limitations Features chapters contributed from leading international figures involved in macrocyclic drug discovery efforts Covers design criteria, typical profile of current macrocycles, applications, and limitations




Privileged Scaffolds in Medicinal Chemistry


Book Description

This book addresses the various classes of privileged scaffolds and covers the history of their discovery and use.







Amino Acids, Peptides and Proteins


Book Description

In an ever-increasing domain of activity, Amino Acids, Peptides and Proteins provides an annual compilation of the world's research effort into this important area of biological chemistry. Comprising a comprehensive review of significant developments at this biology/chemistry interface, each volume opens with an overview of amino acids and their applications. Work on peptides is reviewed over several chapters, ranging from current trends in their synthesis and conformational and structural analysis, to peptidomimetics and the discovery of peptide-related molecules in nature. The application of advanced techniques in structural elucidation is incorporated into all chapters, whilst periodic chapters on metal complexes of amino acids, peptides and beta-lactams extend the scope of coverage. Efficient searching of specialist topics is facilitated by the sub-division of chapters into discrete subject areas, allowing annual trends to be monitored. All researchers in the pharmaceutical and allied industries, and at the biology/chemistry interface in academia will find this an indispensable reference source. Volume 36 covers literature published during 2003.




Peptidomimetics in Organic and Medicinal Chemistry


Book Description

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.




Synthetic and Enzymatic Modifications of the Peptide Backbone


Book Description

Methods in Enzymology 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 Methods of Enzymology series Updated release includes the latest information on the Synthetic and Enzymatic Modifications of the Peptide Backbone




Chemical Epigenetics


Book Description

This book presents an authoritative review of the most significant findings about all the epigenetic targets (writers, readers, and erasers) and their implication in physiology and pathology. The book also covers the design, synthesis and biological validation of epigenetic chemical modulators, which can be useful as novel chemotherapeutic agents. Particular attention is given to the chemical mechanisms of action of these molecules and to the drug discovery prose which allows their identification. This book will appeal to students who want to know the extensive progresses made by epigenetics (targets and modulators) in the last years from the beginning, and to specialized scientists who need an instrument to quickly search and check historical and/or updated notices about epigenetics.




Peptides: The Wave of the Future


Book Description

This volume contains the proceedings of the Second International Peptide Symposium and the Seventeenth American Peptide Symposium, held on 9-14 June, 2001, at the Town and Country Resort in San Diego, California. The biennial meeting was held under the auspices of the American Peptide Society. In addition to the main Symposium, we were honored to have the Merrifield Satellite Symposium, honoring Bruce Merrifield's accomplishments on his 80th birthday. Over 1250 participants from around the world attended the lectures, posters, and exhibits. Reflecting the international nature of the Symposium, there were participants from 37 countries in attendance. In addition to the 75 plenary lectures, there were over 575 poster presentations, and 70 commercial exhibits as well as booths from the American, Australian, Chinese, European, and Japanese Peptide Societies. These proceedings include plenary lectures and oral and poster presentations collected from a wide diversity of topics providing a truly comprehensive and up-to-date overview of the field of peptide science. This publication contains essential reference information for researchers active in peptide science.




Peptide Synthesis and Applications


Book Description

Hands-on experts describe in step-by-step detail the key methodologies of contemporary peptide synthesis and illustrate their numerous applications. The techniques presented include protocols for chemical ligation, the synthesis of cyclic and phosphotyrosine-containing peptides, lipoamino acid- and sugar-conjugated peptides, and peptide purification and analyses. Additional chapters detail methodologies and instrumentation for high-throughput peptide synthesis, many different applications of peptides as novel research tools and biological probes, and the design and application of fluorescent substrate-based peptides that can be used to determine the selectivity and activity of peptidases. A practical guide to the identification of proteins using mass spectrometric analyses of peptide mixtures is also included.




Biologically Active Peptides


Book Description

Investigation into basic and advanced peptide design, synthesis, evaluation and utilization. New therapeutic approaches from experimental systems.