Development of [alpha/beta]-peptide Foldamer Tertiary and Quaternary Structure

Development of [alpha/beta]-peptide Foldamer Tertiary and Quaternary Structure PDF Author: Joshua Lloyd Price
Publisher:
ISBN:
Category :
Languages : en
Pages : 372

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Development of [alpha/beta]-peptide Foldamer Tertiary and Quaternary Structure

Development of [alpha/beta]-peptide Foldamer Tertiary and Quaternary Structure PDF Author: Joshua Lloyd Price
Publisher:
ISBN:
Category :
Languages : en
Pages : 372

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Development of [alpha]-helix-like [alpha]/[beta]/[upsilon] Foldamers

Development of [alpha]-helix-like [alpha]/[beta]/[upsilon] Foldamers PDF Author:
Publisher:
ISBN:
Category :
Languages : en
Pages : 0

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Book Description
Helical peptidomimetics that contain non-natural amino acid residues, such as beta- and gamma-amino acid residues, are less prone to proteolytic degradation than are conventional peptides (composed exclusively of alpha-amino acid residues). However, the additional backbone atoms in beta- and gamma-residues relative to alpha-residues may increase backbone flexibility, and thereby increase the entropic penalty upon binding to a protein partner, resulting in decreased affinity for the targets. Ring-constrained beta- and gamma-amino acids have been developed to address this problem by pre-organizing the residues for helical conformations. This thesis details development of alpha-helix-like alpha/beta/gamma foldamers containing cyclic and/or acyclic beta- and gamma-amino acid residues. Chapters 2 and 3 discuss biophysical investigations of helical alpha/beta/gamma-peptides. Studies of the ring-constrained beta- and gamma-residues' effects on the helicity of alpha/beta/gamma-peptides suggest that beta(3)- and gamma(4)- amino acid residues differ in their intrinsic tendencies to adopt helical secondary structure, with gamma(4)-residues displaying a higher propensity than beta(3)- residues. Different acyclic gamma-residues, and different patterns of alpha, beta and gamma residues in the backbone have been explored. The results show that as long as cyclically constrained beta-amino acids are incorporated into alpha/beta/gamma-peptides, the alpha/beta/gamma-peptide helical propensity is not very sensitive to the nature of the acyclic gamma-amino acids used (although gamma(4)-amino acids are the best helix-adopting acyclic residues) or the pattern of residues within the backbone. Chapter 4 discusses efforts to establish an alpha + alpha/beta/gamma coiled-coil system for use in thermodynamic analysis of alpha + alpha/beta/gamma coiled-coil folding propensities. Chapter 5 discusses efforts toward developing functional alpha/beta/gamma-peptides to modulate apoptosis-regulating protein-protein interactions.

Designing [alpha]/[beta]-peptide Foldamers to Target Diverse Protein Surfaces

Designing [alpha]/[beta]-peptide Foldamers to Target Diverse Protein Surfaces PDF Author:
Publisher:
ISBN:
Category :
Languages : en
Pages : 1146

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Foldamers

Foldamers PDF Author: Stefan Hecht
Publisher: John Wiley & Sons
ISBN: 3527611487
Category : Science
Languages : en
Pages : 456

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Book Description
This truly comprehensive treatise of foldamers, from synthesis to applications in bio-, material-, and nanoscience is at once an introduction to the topic, while providing in-depth accounts on various aspects clearly aimed at the specialist. The book is clearly structured, with the first part concentrating on structure and foldamer design concepts, while the second part covers functional aspects from properties to applications. The international team of expert authors provides overviews of synthetic approaches as well as analytical techniques.

Supramolecular Chemistry in Water

Supramolecular Chemistry in Water PDF Author: Stefan Kubik
Publisher: John Wiley & Sons
ISBN: 3527814930
Category : Science
Languages : en
Pages : 781

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Book Description
Provides deep insight into the concepts and recent developments in the area of supramolecular chemistry in water Written by experts in their respective field, this comprehensive reference covers various aspects of supramolecular chemistry in water?from fundamental aspects to applications. It provides readers with a basic introduction to the current understanding of the properties of water and how they influence molecular recognition, and examines the different receptor types available in water and the types of substrates that can be bound. It also looks at areas to where they can be applied, such as materials, optical sensing, medicinal imaging, and catalysis. Supramolecular Chemistry in Water offers five major sections that address important topics like water properties, molecular recognition, association and aggregation phenomena, optical detection and imaging, and supramolecular catalysis. It covers chemistry and physical chemistry of water; water-mediated molecular recognition; peptide and protein receptors; nucleotide receptors; carbohydrate receptors; and ion receptors. The book also teaches readers all about coordination compounds; self-assembled polymers and gels; foldamers; vesicles and micelles; and surface-modified nanoparticles. In addition, it provides in-depth information on indicators and optical probes, as well as probes for medical imaging. -Covers, in a timely manner, an emerging area in chemistry that is growing more important every day -Addresses topics such as molecular recognition, aggregation, catalysis, and more -Offers comprehensive coverage of everything from fundamental aspects of supramolecular chemistry in water to its applications -Edited by one of the leading international scientists in the field Supramolecular Chemistry in Water is a one-stop-resource for all polymer chemists, catalytic chemists, biochemists, water chemists, and physical chemists involved in this growing area of research.

The Development of Novel Β-peptide Foldamers

The Development of Novel Β-peptide Foldamers PDF Author: Bayard Robert Huck
Publisher:
ISBN:
Category :
Languages : en
Pages : 404

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Synthetic and Enzymatic Modifications of the Peptide Backbone

Synthetic and Enzymatic Modifications of the Peptide Backbone PDF Author:
Publisher: Academic Press
ISBN: 0128212543
Category : Science
Languages : en
Pages : 640

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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

Inhibitors of Protein–Protein Interactions

Inhibitors of Protein–Protein Interactions PDF Author: Ali Tavassoli
Publisher: Royal Society of Chemistry
ISBN: 178801569X
Category : Science
Languages : en
Pages : 357

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Book Description
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.

Fuzziness

Fuzziness PDF Author: Monika Fuxreiter
Publisher: Springer Science & Business Media
ISBN: 1461406595
Category : Medical
Languages : en
Pages : 210

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Book Description
Detailed characterization of fuzzy interactions will be of central importance for understanding the diverse biological functions of intrinsically disordered proteins in complex eukaryotic signaling networks. In this volume, Peter Tompa and Monika Fuxreiter have assembled a series of papers that address the issue of fuzziness in molecular interactions. These papers provide a broad overview of the phenomenon of fuzziness and provide compelling examples of the central role played by fuzzy interactions in regulation of cellular signaling processes and in viral infectivity. These contributions summarize the current state of knowledge in this new field and will undoubtedly stimulate future research that will further advance our understanding of fuzziness and its role in biomolecular interactions.

G Protein-Coupled Receptors

G Protein-Coupled Receptors PDF Author: Jesus Giraldo
Publisher: Royal Society of Chemistry
ISBN: 1849733449
Category : Science
Languages : en
Pages : 549

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Book Description
G protein-coupled receptors (GPCRs) are the largest family of cell-surface receptors, with more than 800 members identified thus far in the human genome. They regulate the function of most cells in the body, and represent approximately 3% of the genes in the human genome. These receptors respond to a wide variety of structurally diverse ligands, ranging from small molecules, such as biogenic amines, nucleotides and ions, to lipids, peptides, proteins, and even light. Ligands (agonists and antagonists) acting on GPCRs are important in the treatment of numerous diseases, including cardiovascular and mental disorders, retinal degeneration, cancer, and AIDS. It is estimated that these receptors represent about one third of the actual identified targets of clinically used drugs. The determination of rhodopsin crystal structure and, more recently, of opsin, 1 and 2 adrenergic and A2A adenosine receptors provides both academia and industry with extremely valuable data for a better understanding of the molecular determinants of receptor function and a more reliable rationale for drug design. GPCR structure and function constitutes a hot topic. The book, which lies between the fields of chemical biology, molecular pharmacology and medicinal chemistry, is divided into three parts. The first part considers what receptor structures tell us about the mechanism of receptor activation. Part II focuses on receptor function. It discusses what the data from biophysical and mutational studies, and the analysis of the interactions of the receptor with ligands and regulator proteins, tell us about the process of signal transduction. The final part, on modelling and simulation, details new insights on the link between structure and mechanism and their implications in drug design.