[PDF] Peptidomimetics Protocols eBook

Author : Wieslaw M. Kazmierski
Publisher : Humana Press
Page : 549 pages
File Size : 12,87 MB
Release : 2010-10-28
Category : Science
ISBN : 9781617370595

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Many physiologically important receptors and enzymes are regulated by their endogenous ligands and inhibitors. Nature chose to utilize these p- tides as chemical switches since they can be efficiently synthesized and - graded in cells, thus providing an immediate response to a fast changing environment. Such properties, so critical in cell survival, make peptides less than ideal drug candidates. Other frequently desired properties in drug m- ecules include oral bioavailability, the ability to cross membranes, including the blood-brain barrier, and sufficient stability for administration 1-2 times a day. In spite of these obstacles, some natural peptides and proteins are ind- putably successful medicines and have become drugs of choice. Further - vances in peptide-based pharmaceuticals are critically dependent on both new delivery methods and new chemical approaches to the conversion of these molecules to druglike entities. In addition, peptides are also the natural sta- ing points for optimization of their pharamacological and chemical prop- ties, which may lead to superior drugs. Peptidomimetics Protocols deals with both aspects of peptide pharmaceuticals, through the tools of modern s- thetic and medicinal chemistry. The last decade has witnessed a steady stream of new synthetic approaches to peptide mimetics, compounds that replace phy- ologically vulnerable peptide functionalities with chemical modules of - creased stability and cellular penetration. The chapters have been written by both academic and industrial chemists, and focus on the practical synthetic preparation of peptide mimetics.

Author : Gregg B. Fields
Publisher : Humana Press
Page : 342 pages
File Size : 16,44 MB
Release : 2010-11-19
Category : Science
ISBN : 9781617376375

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This book is dedicated to the characterization of peptides and their applications for the study of biochemical systems. The contributing authors are all leaders in the field of peptide research. Part I, Characterization, presents the most recent advances in select analytical techniques. Part II, Application, presents a variety of specific applications for synthetic peptides. This book is an indispensable aid in the pursuit of new directions in peptide research.

Author : Antonio Guarna
Publisher : John Wiley & Sons
Page : 334 pages
File Size : 44,42 MB
Release : 2014-03-14
Category : 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.

Author : Waleed M. Hussein
Publisher : Humana
Page : 0 pages
File Size : 39,34 MB
Release : 2019-12-27
Category : Science
ISBN : 9781071602263

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This book provides a variety of procedures for synthetically producing peptides and their derivatives, ensuring the kind of precision that is of paramount importance for successful synthesis. Numerous techniques relevant to drugs and vaccines are explored, such as conjugation and condensation methodologies. Written for the highly successful Methods in Molecular Biology series, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls. Authoritative and practical, Peptide Synthesis: Methods and Protocols serves as an essential guide to the many crucial processes that will allow researchers to efficiently prepare, purify, characterize, and use peptides for chemical, biochemical, and biological studies.

Author : Shmuel Cabilly
Publisher : Springer Science & Business Media
Page : 320 pages
File Size : 26,19 MB
Release : 2008-02-02
Category : Science
ISBN : 1592595715

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During the course of evolution, an imbalance was created between the rate of vertebrate genetic adaptation and that of the lower forms of living organisms, such as bacteria and viruses. This imbalance has given the latter the advantage of generating, relatively quickly, molecules with unexpected structures and features that carry a threat to vertebrates. To compensate for their weakness, vertebrates have accelerated their own evolutionary processes, not at the level of whole organism, but in specialized cells containing the genes that code for antibody molecules or for T-cell receptors. That is, when an immediate requirement for molecules capable of specific interactions arose, nature has preferred to speed up the mode of Darwinian evolution in pref- ence to any other approach (such as the use of X-ray diffraction studies and computergraphic analysis). Recently, Darwinian rules have been adapted for test tube research, and the concept of selecting molecules having particular characteristics from r- dom pools has been realized in the form of various chemical and biological combinatorial libraries. While working with these libraries, we noticed the interesting fact that when combinatorial libraries of oligopeptides were allowed to interact with different selector proteins, only the actual binding sites of these proteins showed binding properties, whereas the rest of the p- tein surface seemed "inert. " This seemingly common feature of protein- having no extra potential binding sites--was probably selected during evolution in order to minimize nonspecific interactions with the surrounding milieu.

Author : Nir Qvit
Publisher : Academic Press
Page : 792 pages
File Size : 34,10 MB
Release : 2022-09-22
Category : Science
ISBN : 0128204478

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Peptide and Peptidomimetic Therapeutics: From Bench to Beside offers applied, evidence-based instruction on developing and applying peptide therapeutics in disease treatment, driving drug discovery, and improving patient care. Here, researchers, clinicians and students will find tools to harness the full power of peptides and peptidomimetics and improve bioavailability, stability, efficiency and selectivity of new therapeutics and their application in treatment plans. More than 20 leaders in the field share their approaches for identifying and advancing peptide and peptidomimetic therapeutics. Topics examined run from "bench to bedside," beginning with fundamental peptide science, protein-protein interactions and peptide synthesis. Later chapters examine modes for peptide drug delivery, including cell penetration peptide and peptidomimetic delivery, as well as the targeting of specific disease types, peptide therapeutics as applied to infectious disease, cancer, metabolic disorders, neurodegenerative disorders, and skin disorders, and antiparasitic and immunosuppressive peptidomimetics. Helps researchers and clinicians harness the full of power of peptides and peptidomimetics in their daily work and drug discovery Features chapters running from “bench to bedside , providing a thorough grounding in fundamental peptide science, drug delivery methods, and targeting of specific disease types Features chapter contributions from international leaders in peptide science and drug development

Author : Thomas Simonson
Publisher : Humana
Page : 427 pages
File Size : 10,34 MB
Release : 2022-03-18
Category : Science
ISBN : 9781071618547

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This volume details current and new computational methodologies to study peptides. Chapters guide readers through antimicrobial peptides, foldability, amyloid sheet formation, membrane-active peptides, organized peptide assemblies, protein-peptide interfaces, prediction of peptide-MHC complexes, advanced free energy simulations for peptide binding, and methods for high throughput peptide or miniprotein design. Written in the format of the highly successful Methods in Molecular Biology series, each chapter includes an introduction to the topic, lists necessary materials, software, and reagents, includes tips on troubleshooting and known pitfalls, and step-by-step, readily reproducible protocols. Authoritative and cutting-edge, Computational Peptides Science: Methods and Protocols aims to provide concepts, methods, and guidelines to help both novices and experienced workers benefit from today's new opportunities and challenges.

Author : Mikhail Soloviev
Publisher : Humana Press
Page : 396 pages
File Size : 46,90 MB
Release : 2010-04-29
Category : Science
ISBN : 9781607615378

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Despite being known and studied for years, peptides have never before attracted enough attention to necessitate the invention of the term "peptidomics" in order to specify the study of the complement of peptides from a cell, organelle, tissue or organism. In Peptidomics: Methods and Protocols, expert researchers present a comprehensive range of analytical techniques for the analysis of the peptide contents of complex biological samples with an emphasis often on higher throughput techniques, suitable for the analysis of large numbers of peptides typically present in the peptidomes. Encompassing a number of species ranging from bacteria to man, the methods presented intensively cover topics such as organism handling, tissue and organ dissection, cellular and subcellular fractionation, peptide extraction, fractionation and purification, structural characterization, molecular cloning, and sequence analysis. Written in the highly successful Methods in Molecular BiologyTM series format, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and notes on troubleshooting and avoiding known pitfalls. Comprehensive and cutting-edge, Peptidomics: Methods and Protocols brings this ten year old field fully up-to-date in order to inspire novices and experts alike with the easy-to-follow practical advice needed to set up and carry out analysis of the peptide contents of complex biological samples.