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Author : Flora Paula Bunga
Publisher :
ISBN 13 :
Total Pages : 0 pages
Book Rating : 4.:/5 (111 download)
Download or read book Synthesis of Cyclic Peptide Natural Products and Peptidomimetics written by Flora Paula Bunga and published by . This book was released on 2015 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Author : Flora Bunga
Publisher :
ISBN 13 :
Total Pages : pages
Book Rating : 4.:/5 (16 download)
Download or read book Synthesis of Cyclic Peptide Natural Products and Peptidomimetics written by Flora Bunga and published by . This book was released on 2015 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt:
Author : Antonio Guarna
Publisher : John Wiley & Sons
ISBN 13 : 1118683145
Total Pages : 334 pages
Book Rating : 4.1/5 (186 download)
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 2014-03-14 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.
Author : Jesko Koehnke
Publisher : Royal Society of Chemistry
ISBN 13 : 1788013778
Total Pages : 392 pages
Book Rating : 4.7/5 (88 download)
Download or read book Cyclic Peptides written by Jesko Koehnke and published by Royal Society of Chemistry. This book was released on 2017-12-14 with total page 392 pages. Available in PDF, EPUB and Kindle. Book excerpt: Cyclic peptides are increasingly employed as chemical tools in biology and drug discovery. They have gained a lot of interest as alternative sources of new drugs to traditional small molecules. This book introduces cyclic peptides and provides a thorough overview of biosynthetic and fully synthetic approaches to their preparation. Following an introduction to cyclic peptides, biosynthetic and traditional chemical routes to cyclic peptides are reviewed. Due to their size, their synthesis is not trivial. Recent advances in the incorporation of novel structural units are presented in addition to how synthesis and biological methods can be combined. The chemical analysis of this molecular class is also discussed. Furthermore, chapters detail the progression of cyclic peptides as tools in biology and as potential drugs, providing a future vision of their importance. In total, this book provides the reader with a comprehensive view of the state-of-the-art of cyclic peptides, from construction to possible clinical utility. This book will be an essential resource for students, researchers and scientists within industry in medicinal, bioorganic, natural product and analytical chemistry fields.
Author : Donald Chang
Publisher : Academic Press
ISBN 13 : 0323145019
Total Pages : 592 pages
Book Rating : 4.3/5 (231 download)
Download or read book Guide to Electroporation and Electrofusion written by Donald Chang and published by Academic Press. This book was released on 1991-12-11 with total page 592 pages. Available in PDF, EPUB and Kindle. Book excerpt: Guide to Electroporation and Electrofusion is designed to cover all relevant topics pertaining to both electroporation and electrofusion. Divided into four major parts, the book covers fundamental aspects, as well as more advance aspects of the electroporation-electrofusion relationship. The book first covers the basic principles and fundamentals by presenting the most recent theoretical and experimental studies from various fields, such as physics, chemistry, and biology. Next, the book tackles the applications of electroporation and electrofusion in biology, such as transferring, manipulating, and transforming genetic materials. In the third section, the book discusses experimental protocols to serve as a guide when performing experiments using electroporation and electrofusion. The final section discusses the instruments needed to effectively perform an experiment that involves electroporation and electrofusion. This book will be of great used to both novice and advanced researchers whose work involves electroporation and electrofusion, as it provides comprehensive information regarding these topics.
Author : A. Abell
Publisher : Elsevier
ISBN 13 : 0080552625
Total Pages : 321 pages
Book Rating : 4.0/5 (85 download)
Download or read book Advances in Amino Acid Mimetics and Peptidomimetics written by A. Abell and published by Elsevier. This book was released on 1997-11-19 with total page 321 pages. Available in PDF, EPUB and Kindle. Book excerpt: Peptidomimetics are compounds which mimic the biological activity of peptides while offering the advantages of increased bioavailability, biostability, bioefficiency, and bioselectivity against the natural biological target of the parent peptide. Examples of peptidomimetics have been isolated as natural products, synthesized as libraries from novel subunits, and designed on the basis of X-ray crystallographic studies and through an intricate knowledge of the biological mode of action of natural peptides. They offer challenging synthetic targets and are increasingly important medicinal agents and biological probes. As a consequence, peptidomimetics embrace much of what is modern medicinal and organic chemistry. This volume highlights some recent and exciting developments in the area.
Author : Eric Marsault
Publisher : John Wiley & Sons
ISBN 13 : 1119092906
Total Pages : 1094 pages
Book Rating : 4.1/5 (19 download)
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
Author : Hanna Hong
Publisher :
ISBN 13 :
Total Pages : pages
Book Rating : 4.:/5 (11 download)
Download or read book Total Synthesis of Novel Bioactive Cyclic Peptide Natural Products written by Hanna Hong and published by . This book was released on 2016 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt:
Author : Hanae Benelkebir
Publisher :
ISBN 13 :
Total Pages : pages
Book Rating : 4.:/5 (824 download)
Download or read book Synthesis of Cyclic Peptide Natural Products and Inhibitors of Histone Modifying Enzymes written by Hanae Benelkebir and published by . This book was released on 2011 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt: Natural products have been the source of numerous leads for several drugs. As these natural products are often isolated in small quantities, it is necessary to produce them synthetically to allow testing for biological activity. Furthermore, synthesis allows the preparation of unnatural analogues for SAR studies. Cyclic peptides represent an important family of biologically active natural products. The hepta- and octacyclopeptides sanguinamide A and sanguinamide B were recently isolated in submicromolar amounts by the Molinski group. The lack of material prevented biological evaluation of the natural products. For this reason and to confirm the structural elucidation we have targeted the total synthesis of sanguinamides. In addition to two proline residues, sanguinamides A and B include heterocycles and natural L-amino acid residues. We have completed the total syntheses of sanguinamides A and B; however the synthetic rotamers differed in both cases from the natural rotamers. We have investigated the influence of macrocyclisation on cis/trans conformational preference of the proline residues for the synthesis of sanguinamide A. We attempted several isomerisations and calculated the relative energies of the different sanguinamide conformers. [D-Ile]-Sanguinamide A, Cys(tBu) analogue of sanguinamide A and the synthetic sanguinamide B displayed antibacterial activity while the synthetic trans, trans-sanguinamide A displayed mild tyrosine kinase inhibitory activity. While extracted stylissamide A showed inhibition of translation during the elongation step, even though being structurally identical to the natural product, the synthetic compound prepared by macrocyclisation from a linear precursor was found to be totally inactive. Histones undergo different types of covalent modifications on the N-terminal tails such as acetylation, phosphorylation and methylation. Histone modification is a major mechanism of regulation in gene expression, replication and repair. Deregulation of histone modifications leads to cancer progression and therefore, inhibitors of enzymes which are able to catalyse the addition and removal of these epigenetic marks have therapeutic potential for treating cancer. An enzyme of particular interest is the family of zinc-dependent histone deacetylases (HDACs) that remove acetyl groups from acetylated lysine residues. Depsipeptides were prepared as HDAC inhibitors. We will ii present our total synthesis of largazole along with a range of analogues and discuss the SAR obtained from HDAC and cell proliferation assays. We elucidated the stereochemistry of burkholdac B by total synthesis of three diastereomers. The diastereomers made along with the natural product were tested as HDAC inhibitors. We are interested in inhibitors of lysine-specific demethylase 1 (LSD1) which is a different kind of epigenetic enzyme involved in demethylation of histone proteins in chromatin. Tranylcypromine is known to be an LSD1 inhibitor. Analogues of PCPA have been synthesised in order to explore the structure-activity relationships of this inhibitor. Analogues were also prepared and tested as LSD1 inhibitors.
Author : Sotirios Koutsopoulos
Publisher : Woodhead Publishing
ISBN 13 : 0081007426
Total Pages : 655 pages
Book Rating : 4.0/5 (81 download)
Download or read book Peptide Applications in Biomedicine, Biotechnology and Bioengineering written by Sotirios Koutsopoulos and published by Woodhead Publishing. This book was released on 2017-11-16 with total page 655 pages. Available in PDF, EPUB and Kindle. Book excerpt: Peptide Applications in Biomedicine, Biotechnology and Bioengineering summarizes the current knowledge on peptide applications in biomedicine, biotechnology and bioengineering. After a general introduction to peptides, the book addresses the many applications of peptides in biomedicine and medical technology. Next, the text focuses on peptide applications in biotechnology and bioengineering and reviews of peptide applications in nanotechnology. This book is a valuable resource for biomaterial scientists, polymer scientists, bioengineers, mechanical engineers, synthetic chemists, medical doctors and biologists. Presents a self-contained work for the field of biomedical peptides Summarizes the current knowledge on peptides in biomedicine, biotechnology and bioengineering Covers current and potential applications of biomedical peptides
Author : Serge Zaretsky
Publisher :
ISBN 13 :
Total Pages : pages
Book Rating : 4.:/5 (133 download)
Download or read book Disrupted Ugi Reaction written by Serge Zaretsky and published by . This book was released on 2015 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt: Cyclization is a technique often employed in the design of therapeutic agents and molecular probes to increase a molecule's affinity and selectivity towards enzyme or receptor target. Recent efforts have yielded a new method of piperazinone formation and peptide cyclization using unprotected aziridine aldehydes. The counterintuitive combination of a nucleophile and an electrophile in one molecule facilitates stitching of amino acids or linear peptides at high concentrations, thereby reducing reaction times. The scope of this reaction has been investigated with a variety of amino acids and peptides. The results differ from the initial studies and a new mechanism has been proposed that takes into account the substrate-dependent reactivity and formation of side-products. A variety of functionalization reactions, through aziridine ring-opening, have been reported. The ring-opened products have exhibited unique structural properties which have been investigated by ab initio calculations, X-ray crystallography, and NMR spectroscopy. Finally, the elements of scaffold design and aziridine ring-opening chemistry have been applied to the creation of inhibitors for Calpain, a disease-causing protease.
Author : Paul Lloyd-Williams
Publisher : CRC Press
ISBN 13 : 9780849391422
Total Pages : 306 pages
Book Rating : 4.3/5 (914 download)
Download or read book Chemical Approaches to the Synthesis of Peptides and Proteins written by Paul Lloyd-Williams and published by CRC Press. This book was released on 1997-04-23 with total page 306 pages. Available in PDF, EPUB and Kindle. Book excerpt: Organic chemists working on the synthesis of natural products have long found a special challenge in the preparation of peptides and proteins. However, more reliable, more efficient synthetic preparation methods have been developed in recent years. This reference evaluates the most important synthesis methods available today, and also considers methods that show promise for future applications. This text describes the state of the art in efficient synthetic methods for the synthesis of both natural and artificial large peptide and protein molecules. Subjects include an introduction to basic topics, linear solid-phase synthesis of peptides, peptide synthesis in solution, convergent solid-phase synthesis, methods for the synthesis of branched peptides, formation of disulfide bridges, and more. The book emphasizes strategies and tactics that must be considered for the successful synthesis of peptides.
Author : Matthew B. Coppock
Publisher : Humana
ISBN 13 : 9781071616888
Total Pages : 469 pages
Book Rating : 4.6/5 (168 download)
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.
Author : Carmen Avendaño
Publisher : Elsevier
ISBN 13 : 0444626670
Total Pages : 767 pages
Book Rating : 4.4/5 (446 download)
Download or read book Medicinal Chemistry of Anticancer Drugs written by Carmen Avendaño and published by Elsevier. This book was released on 2015-06-11 with total page 767 pages. Available in PDF, EPUB and Kindle. Book excerpt: Medicinal Chemistry of Anticancer Drugs, Second Edition, provides an updated treatment from the point of view of medicinal chemistry and drug design, focusing on the mechanism of action of antitumor drugs from the molecular level, and on the relationship between chemical structure and chemical and biochemical reactivity of antitumor agents. Antitumor chemotherapy is a very active field of research, and a huge amount of information on the topic is generated every year. Cytotoxic chemotherapy is gradually being supplemented by a new generation of drugs that recognize specific targets on the surface or inside cancer cells, and resistance to antitumor drugs continues to be investigated. While these therapies are in their infancy, they hold promise of more effective therapies with fewer side effects. Although many books are available that deal with clinical aspects of cancer chemotherapy, this book provides a sorely needed update from the point of view of medicinal chemistry and drug design. Presents information in a clear and concise way using a large number of figures Historical background provides insights on how the process of drug discovery in the anticancer field has evolved Extensive references to primary literature
Author : Ashraf Brik
Publisher : John Wiley & Sons
ISBN 13 : 3527346600
Total Pages : 626 pages
Book Rating : 4.5/5 (273 download)
Download or read book Total Chemical Synthesis of Proteins written by Ashraf Brik and published by John Wiley & Sons. This book was released on 2021-06-08 with total page 626 pages. Available in PDF, EPUB and Kindle. Book excerpt: How to synthesize native and modified proteins in the test tube With contributions from a panel of experts representing a range of disciplines, Total Chemical Synthesis of Proteins presents a carefully curated collection of synthetic approaches and strategies for the total synthesis of native and modified proteins. Comprehensive in scope, this important reference explores the three main chemoselective ligation methods for assembling unprotected peptide segments, including native chemical ligation (NCL). It includes information on synthetic strategies for the complex polypeptides that constitute glycoproteins, sulfoproteins, and membrane proteins, as well as their characterization. In addition, important areas of application for total protein synthesis are detailed, such as protein crystallography, protein engineering, and biomedical research. The authors also discuss the synthetic challenges that remain to be addressed. This unmatched resource: Contains valuable insights from the pioneers in the field of chemical protein synthesis Presents proven synthetic approaches for a range of protein families Explores key applications of precisely controlled protein synthesis, including novel diagnostics and therapeutics Written for organic chemists, biochemists, biotechnologists, and molecular biologists, Total Chemical Synthesis of Proteins provides key knowledge for everyone venturing into the burgeoning field of protein design and synthetic biology.
Author : Zigang Li
Publisher : John Wiley & Sons
ISBN 13 : 3527343458
Total Pages : 242 pages
Book Rating : 4.5/5 (273 download)
Download or read book Cyclized Helical Peptides written by Zigang Li and published by John Wiley & Sons. This book was released on 2021-06-21 with total page 242 pages. Available in PDF, EPUB and Kindle. Book excerpt: An important and timely guide to the progress being made on constrained helical peptides Constraint helical peptides have emerged as a solution to target previously undruggable protein-protein interactions, which feature large and complex surfaces. Cyclized Helical Peptides: Synthesis, Properties and Therapeutic Applications offers a review of the most current methodologies of constructing constrained helices. The authors noted experts on the topic include the information on the fundamental features of cyclized helical peptides and discuss their limitations. The book summarizes and explores the effects of chemical methods constructing helical peptides on helicity, binding affinity, cell penetration, and nonspecific toxicity. The book examines the therapeutic applications of the constraint helices and includes comparison with existing small molecule modulators or antibodies. Designed as a useful resource for both those outside and inside the field. Those new to the field will find a comprehensive introduction to cyclized helical peptide and those inside the field will find a deeper understanding of the topic. This important book: Offers a practical introduction to constrained helical peptides Includes all aspects of constrained helical peptides Includes information on the most recent methods that have emerged Presents a guide to help solve practical problems in the field Written for academics, pharmaceutical professional, Cyclized Helical Peptides is a comprehensive guide to the developments of constrained helical peptides.
Author : Channa Basava
Publisher : Springer Science & Business Media
ISBN 13 : 1461581761
Total Pages : 417 pages
Book Rating : 4.4/5 (615 download)
Download or read book Peptides written by Channa Basava and published by Springer Science & Business Media. This book was released on 2012-12-06 with total page 417 pages. Available in PDF, EPUB and Kindle. Book excerpt: A successful seientific career requires constant effort on the part of the seientist. If such a career is to be achieved by seientists in developing countries where the faeilities are not easily available, even more dedication is required. Dr. K. M. Sivanandaiah, having completed a successful career in the field of peptide chemistry, is such a seientist. Being weIl aware of the limited research facilities available in India, we are extraordinarily appreciative of Professor Sivanandaiah's dedication to the advancement of science. As a Professor of Chemistry and, until his retirement in 1992, the Head of the Department of Studies in Chemistry at Bangalore University, India, he not only devoted much of his time to his students, teaching basic organic chemistry, but was also able to contribute to the field of peptide chemistry. After completing 25 years of service at Central College, Bangalore, where he was admired as an outstanding teacher, Professor Sivanandaiah is still active in research. He is now Professor Emeritus and continues to contribute to the field of peptides. As former students of Professor Sivanandaiah, we felt that publishing a book containing articles related to the design, synthesis, conformation, and biological activity of peptides and written by eminent scientists in the field of peptide research would be a fitting tribute to his role in the field of bioorganic chemistry.
