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Peptidomimetics Protocols

2010-10-28 Science
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Release : 2010-10-28
Genre : Science
Kind : eBook
Book Rating : 595/5 ( reviews)

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Book Synopsis Peptidomimetics Protocols by : Wieslaw M. Kazmierski

Download or read book Peptidomimetics Protocols written by Wieslaw M. Kazmierski. This book was released on 2010-10-28. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Peptide Characterization and Application Protocols

2010-11-19 Science
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Release : 2010-11-19
Genre : Science
Kind : eBook
Book Rating : 375/5 ( reviews)

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Book Synopsis Peptide Characterization and Application Protocols by : Gregg B. Fields

Download or read book Peptide Characterization and Application Protocols written by Gregg B. Fields. This book was released on 2010-11-19. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Peptidomimetics in Organic and Medicinal Chemistry

2014-03-14 Science
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Release : 2014-03-14
Genre : Science
Kind : eBook
Book Rating : 145/5 ( reviews)

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Book Synopsis Peptidomimetics in Organic and Medicinal Chemistry by : Antonio Guarna

Download or read book Peptidomimetics in Organic and Medicinal Chemistry written by Antonio Guarna. This book was released on 2014-03-14. Available in PDF, EPUB and Kindle. Book excerpt: 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 Synthesis

2019-12-27 Science
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Release : 2019-12-27
Genre : Science
Kind : eBook
Book Rating : 263/5 ( reviews)

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Book Synopsis Peptide Synthesis by : Waleed M. Hussein

Download or read book Peptide Synthesis written by Waleed M. Hussein. This book was released on 2019-12-27. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Combinatorial Peptide Library Protocols

2008-02-02 Science
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Release : 2008-02-02
Genre : Science
Kind : eBook
Book Rating : 715/5 ( reviews)

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Book Synopsis Combinatorial Peptide Library Protocols by : Shmuel Cabilly

Download or read book Combinatorial Peptide Library Protocols written by Shmuel Cabilly. This book was released on 2008-02-02. Available in PDF, EPUB and Kindle. Book excerpt: 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.

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