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Peptide Macrocycles
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Book Synopsis Peptide Macrocycles by : Matthew B. Coppock
Download or read book Peptide Macrocycles written by Matthew B. Coppock and published by Humana. This book was released on 2021-11-02 with total page 469 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume explores the latest techniques and strategies used to study the field of peptide macrocycles. The chapters in this book ae organized into four parts: macrocycles synthesis, combinational library synthesis and screening, macrocycle characterization, and unique applications. Part One looks at a variety of peptide cyclization methodologies, and Part Two describes methods for the creation of peptide macrocycles libraries and their subsequent screening against biological targets of interest. Part Three discusses the study and characterization of peptide macrocycle-target interactions, and Part Four introduces unique applications for peptide macrocycles, from higher-order structure formation to post-synthetic functional modifications. Written in the highly successful Methods in Molecular Biology series format, 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. Cutting-edge and comprehensive, Peptide Macrocycles: Methods and Protocols is a valuable resource for both novice and expert researchers looking to learn more about this developing field.
Book Synopsis Practical Medicinal Chemistry with Macrocycles by : Eric Marsault
Download or read book Practical Medicinal Chemistry with Macrocycles written by Eric Marsault and published by John Wiley & Sons. This book was released on 2017-09-12 with total page 617 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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
Book Synopsis Peptide Macrocycles by : Matthew B. Coppock
Download or read book Peptide Macrocycles written by Matthew B. Coppock and published by . This book was released on 2021 with total page 469 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume explores the latest techniques and strategies used to study the field of peptide macrocycles. The chapters in this book ae organized into four parts: macrocycles synthesis, combinational library synthesis and screening, macrocycle characterization, and unique applications. Part One looks at a variety of peptide cyclization methodologies, and Part Two describes methods for the creation of peptide macrocycles libraries and their subsequent screening against biological targets of interest. Part Three discusses the study and characterization of peptide macrocycle-target interactions, and Part Four introduces unique applications for peptide macrocycles, from higher-order structure formation to post-synthetic functional modifications. Written in the highly successful Methods in Molecular Biology series format, 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. Cutting-edge and comprehensive, Peptide Macrocycles: Methods and Protocols is a valuable resource for both novice and expert researchers looking to learn more about this developing field.
Book Synopsis Practical Medicinal Chemistry with Macrocycles by : Eric Marsault
Download or read book Practical Medicinal Chemistry with Macrocycles written by Eric Marsault and published by John Wiley & Sons. This book was released on 2017-08-04 with total page 1094 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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
Book Synopsis Inhibitors of Protein–Protein Interactions by : Ali Tavassoli
Download or read book Inhibitors of Protein–Protein Interactions written by Ali Tavassoli and published by Royal Society of Chemistry. This book was released on 2020-12-07 with total page 357 pages. Available in PDF, EPUB and Kindle. Book excerpt: Protein-protein interactions (PPI) are at the heart of the majority of cellular processes, and are frequently dysregulated or usurped in disease. Given this central role, the inhibition of PPIs has been of significant interest as a means of treating a wide variety of diseases. However, there are inherent challenges in developing molecules capable of disrupting the relatively featureless and large interfacial areas involved. Despite this, there have been a number of successes in this field in recent years using both traditional drug discovery approaches and innovative, interdisciplinary strategies using novel chemical scaffolds. This book comprehensively covers the various aspects of PPI inhibition, encompassing small molecules, peptidomimetics, cyclic peptides, stapled peptides and macrocycles. Illustrated throughout with successful case studies, this book provides a holistic, cutting-edge view of the subject area and is ideal for chemical biologists and medicinal chemists interested in developing PPI inhibitors.
Download or read book Peptide Macrocycles written by Lei Liu and published by . This book was released on 2014 with total page 196 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Book Synopsis Macrocycles in Drug Discovery by : Jeremy I Levin
Download or read book Macrocycles in Drug Discovery written by Jeremy I Levin and published by Royal Society of Chemistry. This book was released on 2015 with total page 526 pages. Available in PDF, EPUB and Kindle. Book excerpt: This series provides a comprehensive resource for postgraduate students and for scientists in academia or industry wanting to learn topics outside their own areas of expertise.
Book Synopsis Synthesis and Characterization of Peptide Macrocycles as Novel, Bimodal Proteasome Inhibitors by : David Lawrence Wilson
Download or read book Synthesis and Characterization of Peptide Macrocycles as Novel, Bimodal Proteasome Inhibitors written by David Lawrence Wilson and published by . This book was released on 2015 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: The proteasome is a large, multicatalytic protease found in all forms of life. The proteasome is instrumental in the regulation of many cellular pathways such as cell cycle arrest and cell proliferation. For this reason, proteasome inhibitors are of interest in drug development because of their ability to regulate the asynchronous cell cycles of cancers. In particular, multiple myeloma has been shown to be receptive to treatment with proteasome inhibitors. In this study, two novel macrocyclic peptidyl aldehyde proteasome inhibitors 11 and 12 are reported. The design of 11 and 12 was bioinspired by the natural product TMC-95A, a macrocyclic tripeptide shown to potently and selectively inhibit the proteasome. Compounds 11 and 12 were designed to test the effects of the peptide macrocycle on inhibitory strength and specificity. Both inhibitors were identical in sequence, however 12 incorporated a biaryl ether linkage to mimic the macrocyclic structure of TMC-95. Additionally, both inhibitors incorporated a C-terminal aldehyde designed to covalently bind the proteasome's catalytic threonine residue and hydrophobic side chains to target the chymotrypsin-like activity of the proteasome. In vitro testing of both inhibitors revealed them to be potent and specific inhibitors of the chymotrypsin-like activity of the proteasome (11, Ki = 33 nM, 12, Ki = 76 nM). It was found that there was no trend to suggest that the peptide macrocycle conferred increased specificity or binding. Ex vivo assays for 12 showed it to be metabolically stable, readily taken up by HeLa cells, and perform on par with the well characterized proteasome inhibitor MG-132. Finally, QM/MM studies suggested that the oxindole moiety found in the macrocycle of TMC-95A is essential for specificity for the chymotrypsin-like active site of the proteasome.
Download or read book Cyclic Peptides written by Jesko Koehnke and published by Royal Society of Chemistry. This book was released on 2017-12-15 with total page 392 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book provides the reader with a comprehensive view of the state-of-the-art of cyclic peptides, from construction to utility in biology and drug discovery.
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 and published by John Wiley & Sons. This book was released on 2014-04-07 with total page 334 pages. 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.
Book Synopsis Anion Coordination Chemistry by : Kristin Bowman-James
Download or read book Anion Coordination Chemistry written by Kristin Bowman-James and published by John Wiley & Sons. This book was released on 2012-03-27 with total page 644 pages. Available in PDF, EPUB and Kindle. Book excerpt: Building on the pioneering work in supramolecular chemistry from the last 20 years or so, this monograph addresses new and recent approaches to anion coordination chemistry. Synthesis of receptors, biological receptors and metallareceptors, the energetics of anion binding, molecular structures of anion complexes, sensing devices are presented and computational studies addressed to aid with the understanding of the different driving forces responsible for anion complexation. The reader is promised an actual picture of the state of the art for this exciting and constantly evolving field of supramolecular anion coordination chemistry. The topics range from ion channels to selective sensors, making it attractive to all researchers and PhD students with an interest in supramolecular chemistry.
Book Synopsis Cucurbiturils and Related Macrocycles by : Kimoon Kim
Download or read book Cucurbiturils and Related Macrocycles written by Kimoon Kim and published by Royal Society of Chemistry. This book was released on 2019-11-06 with total page 572 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book provides a complete overview of cucurbituril chemistry, covering fundamental aspects including history, synthesis and host-guest chemistry.
Book Synopsis Middle Molecular Strategy by : Koichi Fukase
Download or read book Middle Molecular Strategy written by Koichi Fukase and published by Springer Nature. This book was released on 2021-07-13 with total page 357 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book highlights recently discovered aspects of “middle-size molecules,” focusing on (1) their unique bio-functions on the basis of derivatives and conjugates of natural products, saccharides, peptides, and nucleotides; (2) the synthesis of structurally complex natural products; (3) special synthetic methods for π-conjugated functional molecules; and (4) novel synthetic methods using flow chemistry. Given its scope, the book is of interest to industrial researchers and graduate students in the fields of organic chemistry, medicinal chemistry, and materials science.
Book Synopsis New Methods to Prepare Complex Macrocyclic Peptidomimetics Directly from Unprotected Peptides by : Kenneth Victor Lawson
Download or read book New Methods to Prepare Complex Macrocyclic Peptidomimetics Directly from Unprotected Peptides written by Kenneth Victor Lawson and published by . This book was released on 2014 with total page 720 pages. Available in PDF, EPUB and Kindle. Book excerpt: Peptidomimetic macrocycles are valuable research tools and serve as lead compounds in drug discovery. We have developed two synthetic methods to access distinct isomeric macrocycles from a given peptide sequence; internal palladium(0)-catalyzed allylation, and large-ring forming Friedel-Crafts alkylation. These methods utilize a lipophilic template designed to impart favorable drug-like properties to the composite macrocycles relative to their linear peptide precursors. Structurally diverse macrocyclic peptidomimetics derived from these methods have the potential to identify small molecules effective against challenging targets involved in exposed protein surfaces.
Book Synopsis Supramolecular Protein Chemistry by : Peter B Crowley
Download or read book Supramolecular Protein Chemistry written by Peter B Crowley and published by Royal Society of Chemistry. This book was released on 2020-12-09 with total page 329 pages. Available in PDF, EPUB and Kindle. Book excerpt: Building on decades of “host-guest” research, recent years have seen a surge of activity in water-soluble supramolecular receptors for protein recognition and assembly. Progress has been particularly rich in the area of calixarenes, cucurbiturils and molecular tweezers. Emerging applications include controlled protein assembly in solution, crystal engineering, supramolecular control of catalysis (both in vitro and in vivo), as well as novel mechanisms of protein-interaction inhibition with relevance to amyloids and disease. One challenge at the interface of supramolecular chemistry and protein science is to increase interaction and collaboration between chemists and biochemists/structural biologists.This book addresses the exciting interface of supramolecular chemistry and protein science. Chapters cover supramolecular approaches to protein recognition, assembly and regulation. Principles outlined will highlight the opportunities that are readily accessible to collaborating chemists and biochemists, enriching the breadth and scope of this multidisciplinary field. Supramolecular Protein Chemistry will be of particular interest to graduate students and researchers working in supramolecular chemistry, protein science, self-assembly, biomaterials, biomedicine and biotechnology.
Book Synopsis Modern Supramolecular Chemistry by : François Diederich
Download or read book Modern Supramolecular Chemistry written by François Diederich and published by John Wiley & Sons. This book was released on 2008-03-17 with total page 419 pages. Available in PDF, EPUB and Kindle. Book excerpt: Written by internationally acclaimed experts, this handy volume covers all major classes of supramolecular compounds. Chapters include cyclophanes, resorcinarene and calixarene synthesis, supramolecular metallomacrocycles and macrocycle synthesis, rotaxane and catenane synthesis, cucurbiturils and porphyrins, as well as macrocyclic drugs. Each chapter contains experimental procedures allowing fast access to this type of synthetic chemistry.
Book Synopsis Peptide Therapeutics by : Seetharama D. Jois
Download or read book Peptide Therapeutics written by Seetharama D. Jois and published by Springer Nature. This book was released on 2022-09-26 with total page 321 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.
