Structure and Function in Peptides with Natural and Non-natural Backbones PDF Download
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Author: Jonathan Robert Lai
Publisher:
ISBN:
Category :
Languages : en
Pages : 422
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Book Description
Author: Jonathan Robert Lai
Publisher:
ISBN:
Category :
Languages : en
Pages : 422
Get Book Here
Book Description
Author:
Publisher:
ISBN: 9780815332183
Category : Cells
Languages : en
Pages : 0
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Book Description
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
Author:
Publisher:
ISBN: 9781339160450
Category :
Languages : en
Pages : 452
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Book Description
Cyclic peptides are structurally complex molecules with the potential to access challenging biological targets. Although many cyclic peptides exhibit poor pharmacokinetic properties, a few have structural features that allow them to passively permeate cell membranes and achieve high oral bioavailability. It is well established that intramolecular hydrogen bonds and N-methylation play important roles in the passive permeability of cyclic peptides, but other structural features have been explored less extensively. In order to design synthetic peptides with better pharmacokinetic and physicochemical properties a deeper understanding of the relationship between structure and function is necessary. Cyclic peptide natural products contain a variety of non-proteinogenic structural elements such as D-amino acids, gamma-amino acids, beta-hydroxlation, and an enrichment in beta-branched amino acids; all of which may impart to the peptide scaffolds favorable physicochemical properties. To determine the effects of these non-proteinogenic structural motifs on the passive permeability of peptidic macrocycles, a series of 14 cyclic hexapeptide stereoisomers containing gamma-amino acids was synthesized and assessed for permeability, solubility, lipophilicity, and oral bioavailability. Using a combination of NMR and computational modeling, the solution structures of 5 macrocycles were determined. The compounds with more intramolecular hydrogen bonds tended to be more permeable, and one compound was found to be 21% orally bioavailable in rat. The relative effects of steric occlusion by beta-branched residues, N-methylation, and aliphatic carbon count on cyclic peptide permeability were explored using multiple scaffolds. In a series of 17 sanguinamide A analogs, steric occlusion by beta-branched residues was determined to have a minimal effect on passive permeability compared to that of N-methylation and scaffold lipophilicity, which were used to increase the permeability of the scaffold 15-fold. One analog was found to exhibit both high passive permeability and solubility. This behavior was attributed to the solvent-dependent backbone flexibility observed in NMR and molecular dynamics experiments. Finally, the bioactivity and permeability of a set of trimethylated cyclic hexapeptides was explored. Two new passively permeable macrocycles with different pattens of N-methylation and stereochemistry were developed and a side chain variant disrupted cell growth in several organisms.
Author:
Publisher: Academic Press
ISBN: 0128007974
Category : Science
Languages : en
Pages : 404
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Book Description
Advances in Botanical Research publishes in-depth and up-to-date reviews on a wide range of topics in plant sciences. Currently in its 76th volume, the series features several reviews by recognized experts on all aspects of plant genetics, biochemistry, cell biology, molecular biology, physiology and ecology. - Publishes in-depth and up-to-date reviews on a wide range of topics in plant sciences - Contains commentary by recognized experts on all aspects of plant genetics, biochemistry, cell biology, molecular biology, physiology, and ecology - This volume features reviews of the fast moving field of plant cyclotides
Author:
Publisher: Academic Press
ISBN: 0080921639
Category : Science
Languages : en
Pages : 334
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Book Description
By combining the tools of organic chemistry with those of physical biochemistry and cell biology, Non-Natural Amino Acids aims to provide fundamental insights into how proteins work within the context of complex biological systems of biomedical interest. The critically acclaimed laboratory standard for 40 years, Methods in Enzymology is one of the most highly respected publications in the field of biochemistry. Since 1955, each volume has been eagerly awaited, frequently consulted, and praised by researchers and reviewers alike. With more than 400 volumes published, each Methods in Enzymology volume presents material that is relevant in today's labs -- truly an essential publication for researchers in all fields of life sciences. - Demonstrates how the tools and principles of chemistry combined with the molecules and processes of living cells can be combined to create molecules with new properties and functions found neither in nature nor in the test tube - Presents new insights into the molecular mechanisms of complex biological and chemical systems that can be gained by studying the structure and function of non-natural molecules - Provides a "one-stop shop" for tried and tested essential techniques, eliminating the need to wade through untested or unreliable methods
Author: Astrid Sigel
Publisher: Walter de Gruyter GmbH & Co KG
ISBN: 3110434334
Category : Science
Languages : en
Pages : 596
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Book Description
Volume 17, entitled Lead: Its Effects on Environment and Health of the series Metal Ions in Life Sciences centers on the interrelations between biosystems and lead. The book provides an up-to-date review of the bioinorganic chemistry of this metal and its ions; it covers the biogeochemistry of lead, its use (not only as gasoline additive) and anthropogenic release into the environment, its cycling and speciation in the atmosphere, in waters, soils, and sediments, and also in mammalian organs. The analytical tools to determine and to quantify this toxic element in blood, saliva, urine, hair, etc. are described. The properties of lead(II) complexes formed with amino acids, peptides, proteins (including metallothioneins), nucleobases, nucleotides, nucleic acids, and other ligands of biological relevance are summarized for the solid state and for aqueous solutions as well. All this is important for obtaining a coherent picture on the properties of lead, its effects on plants and toxic actions on mammalian organs. This and more is treated in an authoritative and timely manner in the 16 stimulating chapters of Volume 17, which are written by 36 internationally recognized experts from 13 nations. The impact of this recently again vibrant research area is manifested in nearly 2000 references, over 50 tables and more than 100 illustrations (half in color). Lead: Its Effects on Environment and Health is an essential resource for scientists working in the wide range from material sciences, inorganic biochemistry all the way through to medicine including the clinic ... not forgetting that it also provides excellent information for teaching.
Author:
Publisher: Elsevier
ISBN: 0443218153
Category : Science
Languages : en
Pages : 400
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Book Description
Peptide Chemical Tools for Modulating Biology, Volume 698 in the esteemed Methods in Enzymology series, highlights new advances in the field, with this new volume presenting interesting topics on Peptide tools that target telomere maintenance, Molecular Design of Peptide Therapeutics, Sulfonyl peptide tools for modulating biology, Peptide tools for targeting the Crk/CrkL-p130Cas axis, Quorum sensing peptide tools, In vivo stability and BBB penetration of peptide tools, and Oligo-benzamide-based peptide mimicking tools for modulating biology. - Provides the authority and expertise of leading contributors from an international board of authors - Presents the latest release in Methods in Enzymology - Updated release includes the latest information on Peptide Chemical Tools for Modulating Biology
Author: Antonio Guarna
Publisher: John Wiley & Sons
ISBN: 1119950600
Category : Science
Languages : en
Pages : 334
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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.
Author: Pierre Rousselot-pailley
Publisher: World Scientific
ISBN: 9811261679
Category : Science
Languages : en
Pages : 520
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Book Description
Peptides and proteins are crucial biomolecules in life. The manifold functions they carry out range from molecular recognition and signaling to catalysis and immune response. However, the native systems are limited to a reduced toolbox of chemical functionalities as well as tridimensional structures. Widening these toolboxes could pave the way to engineer peptides and proteins with enhanced properties compared to their native counterparts and/or with structures and functions unprecedented in Nature. Advances in the chemical and biological synthesis of peptides and proteins, in computational tools, in molecular biology and in high-throughput screening methods are making this realm possible.This book aims to give an overview of the last developments in the field of peptide and protein engineering. It comprises a collection of chapters that span from the production of simple non-proteinogenic building blocks and peptidic scaffolds of different sizes and structures to more complex systems including peptide-based nanomaterials, enzymes and artificial metalloenzymes. Different strategies are described where chemical and biological tools have been developed and combined to attain the desired properties and sought functionalities.The diverse systems described in this book highlight the progress in this important field and represent the starting points for the development of functional biomolecules, biomaterials and hybrid systems capable of addressing key societal challenges of our times in relevant areas such health, environment and energy.
