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Chemical Structure And Antibacterial Activity Of Some Analogues Of Natural Amino Acids And Peptides
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Book Synopsis Chemical Structure and Antibacterial Activity of Some Analogues of Natural Amino Acids and Peptides by : Themis Askounis Klotz
Download or read book Chemical Structure and Antibacterial Activity of Some Analogues of Natural Amino Acids and Peptides written by Themis Askounis Klotz and published by . This book was released on 1951 with total page 76 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Book Synopsis Amino Acids, Peptides and Proteins by : J S Davies
Download or read book Amino Acids, Peptides and Proteins written by J S Davies and published by Royal Society of Chemistry. This book was released on 2007-10-31 with total page 455 pages. Available in PDF, EPUB and Kindle. Book excerpt: Amino Acids, Peptides and Proteins comprises a comprehensive review of significant developments at this biology/chemistry interface. Each volume of this Specialist Periodical Report opens with an overview of amino acids and their applications. Work on peptides is reviewed over several chapters, ranging from current trends in their synthesis and conformational and structural analysis, to peptidomimetics and the discovery of peptide-related molecules in nature. The application of advanced techniques in structural elucidation is incorporated into all chapters, whilst periodic chapters on metal complexes of amino acids, peptides and beta-lactams extend the scope of coverage. Efficient searching of specialist topics is facilitated by the sub-division of chapters into discrete subject areas, allowing annual trends to be monitored. Researchers in the pharmaceutical and allied industries, and at the biology/chemistry interface in academia will find this an indispensable reference source. Specialist Periodical Reports provide systematic and detailed review coverage in major areas of chemical research. Compiled by teams of leading experts in their specialist fields, this series is designed to help the chemistry community keep current with the latest developments in their field. Each volume in the series is published either annually or biennially and is a superb reference point for researchers. www.rsc.org/spr
Book Synopsis Amino Acids, Peptides and Proteins by : Maxim Ryadnov
Download or read book Amino Acids, Peptides and Proteins written by Maxim Ryadnov and published by Royal Society of Chemistry. This book was released on 2017-11-29 with total page 338 pages. Available in PDF, EPUB and Kindle. Book excerpt: Amino Acids, Peptides and Proteins comprises a comprehensive and critical review of significant developments at the biology and chemistry interface. Compiled by leading researchers in their subject, this volume incorporates current trends and emerging areas in topics such as magnetic resonance studies of membrane active peptides, proteins and peptides for the diagnosis and therapy of Leishmania donovani parasite infections and advances in the design of ligands interacting with proteases causing infectious respiratory syndrome. Appealing broadly to researchers in academia and industry, it will be of great benefit to any researcher wanting a succinct reference on developments in this area now and looking to the future.
Book Synopsis Polypeptoids as Simplified Analogues of Antimicrobial Peptides by : Pedro Javier Salas Ambrosio
Download or read book Polypeptoids as Simplified Analogues of Antimicrobial Peptides written by Pedro Javier Salas Ambrosio and published by . This book was released on 2021 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: Antimicrobial peptides (AMP) are an interesting family of natural peptides mainly produced by microorganisms to eliminate their bacterial competitors. AMPs have demonstrated their effectiveness against all types of micro-organisms: the efficacy of AMPs is explained by their ability to destabilize membranes, a physicochemical property linked to their amphiphilic character. Until now, the industrial development of AMPs in pharmacy remains limited and their sensitivity to proteases prevents their therapeutic administration by oral route. By reproducing their chemical composition or certain structural characteristics, polymeric analogues have been proposed to try to overcome these limitations, such as amino acid polymers which are biodegradable and biocompatible.This Ph.D. work presents the preparation of new antimicrobial copolypeptoids by ring-opening polymerization (ROP) of N-alkylated-N-carboxyanhydrides (NNCA) bearing hydrophobic and cationic substituents. These NNCAs monomers bearing hydrophobic alkyl groups (methyl, isopropyl, cyclohexyl, benzyl, p-nitrobenzyl and methylthioethyl) or alkyl precursors of cationic units (Cbz-aminoethyl and Cbz-aminobutyl) were prepared in two synthetic steps: 1) reductive amination with glyoxylic acid, 2) cyclization into NNCA via the Leuchs method through the introduction of N-Boc protection. This methodology enabled us to prepare 9 monomers whose polymerization was studied: we first determined the kinetics of the ROP reactions in DMF and we implemented copolymerization reactions by mixing the NNCA monomers. Using this methodology, we developed a variety of copolypeptoids consisting of cationic and hydrophobic units at various ratios and designed copolymers with different macromolecular architectures such as linear-drug conjugates, cyclic structures or star-like structures.According to the WHO, bacterial infections caused by resistant germs have reached very high levels of incidence worldwide, being responsible for a worrying mortality. One of the most problematic pathogens is Clostridioides difficile, a Gram-positive bacterium responsible for pseudomembranous colitis, a nosocomial infection that is frequently lethal in elderly patients. Current treatment consists in antibiotics that often present recurrences. The goal of this Ph.D. thesis was to develop a medicinal chemistry approach to design antimicrobial copolypeptoids capable of killing this pathogen. First, we prepared libraries of linear copolymers in order to study the structure-antimicrobial activity relationships (SAR) varying the nature of the side chains, the nature of the initiator, the degree of polymerization, enabling us to define a first series of active compounds whose minimum inhibitory concentrations (MIC) were determined towards C. difficile as well as their cytotoxicity on Caco-2 intestinal epithelial cells. In a second step, we prepared a series of cyclic copolypeptoids by developing a new methodology: the ring-expansion polymerization using LiHMDS. This new synthesis enabled us to access macrocyclic polymers and vary the hydrophobic content and microstructure of the peptoid copolymers, to perform a second SAR study with respect to antimicrobial tests on C. difficile. Finally, we extended our study to other macromolecular architectures: star-like copolymers and antibiotic drug conjugates. Overall, SAR studies showed that linear and cyclic copolymers with random microstructure, containing N-benzyl and N-aminobutyl groups exhibited the most interesting antibacterial activity against C. difficile. Finally, antibacterial assays on other bacteria allowed us to evaluate a preliminary antibacterial spectrum of action.
Book Synopsis Total Synthesis of Naturally Occurring Antimicrobial Peptides by : Buzhe Xu
Download or read book Total Synthesis of Naturally Occurring Antimicrobial Peptides written by Buzhe Xu and published by . This book was released on 2019 with total page 231 pages. Available in PDF, EPUB and Kindle. Book excerpt: This thesis describes the first total synthesis of naturally occurring lanthipeptide tikitericin, as well as its N-terminal truncated analogues. The thesis also explores the total chemical synthesis of the lipopeptide antibiotic daptomycin and analogues along with evaluation of their antibacterial activity. Tikitericin is a newly described lanthipeptide characterized by four intramolecular thioether linked (methyl)lanthionine bridges. It was isolated from the New Zealand extremophilic microorganism Thermogemmatispora strain T81, collected at Tikitere (Hell's Gate), Rotorua. However, the chemical and biological properties of tikitericin haven't been established due to the limited amount of natural product isolated. This thesis describes the first total synthesis of tikitericin via Fmoc-solid-phase peptide synthesis (SPPS). The key noncanonical (methyl)lanthionine residues were synthesized in solution phase via an improved synthetic route and subsequently assembled to construct the peptide backbone using Fmoc-SPPS. N-Terminal truncated analogues of tikitericin were also prepared in order to evaluate the contribution of each sequential ring of the polycyclic lanthipeptide to the antibacterial activity. Daptomycin is a cyclic lipodepsipeptide natural product, exhibiting potent antimicrobial activity against highly resistant Gram-positive pathogens such as methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococci (VRE), and several species of Streptococci. Previous chemoenzymatic synthesis, semi-synthesis, and combinatorial biosynthesis only produced a very limited number of daptomycin analogues, leaving much of the chemical space unexplored. A de novo solid-phase synthesis of daptomycin via Boc chemistry was achieved. The challenging ester bond formation between the nonproteinogenic amino acid kynurenine was achieved by esterification of a threonine residue with a protected tryptophan. Subsequent late-stage on-resin ozonolysis, inspired by the biomimetic pathway, afforded the kynurenine residue directly. Synthetic daptomycin possessed potent antimicrobial activity against S. aureus, while five other daptomycin analogues containing (2R,3R)-3-methylglutamic acid, (2S,4S)-4-methylglutamic acid or canonical glutamic acid at position twelve prepared using this new methodology were all inactive; clearly establishing that the (2S,3R)-3-methylglutamic acid plays a key role in the antimicrobial activity of daptomycin.
Book Synopsis Biomembrane Structures by : Parvez I. Haris
Download or read book Biomembrane Structures written by Parvez I. Haris and published by IOS Press. This book was released on 1998 with total page 288 pages. Available in PDF, EPUB and Kindle. Book excerpt: Biological membranes play a significant role in a range of biological processes such as ion-transport and signal transduction. Over the years much effort has been devoted towards developing an understanding of biomembrane structure. The study of this subject is now reaching an important stage. This is because at last the full three-dimensional structure of certain membrane proteins is beginning to be resolved. In the past three-dimensional structures of membrane proteins were difficult to obtain as only two dimensional crystals were available. In recent years satisfactory crystals have been obtained and X-ray diffraction techniques have been applied. This has led to the three dimensional structures of the photosynthetic reaction centres, porins and more recently the structure of cytochrome oxidase. Of course not all membrane proteins are readily crystallisable and some are not even available in sufficient quantities to obtain the necessary crystals or to carry out biophysical experiments. In some cases e.g. the voltage-gated potassium ion channel membrane proteins their structure has been proposed mainly on the basis of molecular biology methods. This has prompted the search for alternative approaches for characterising biomembrane structure. Molecular biological studies are providing a wealth of information on a number of different membrane proteins. Combining the information derived from such studies with molecular modelling is becoming extremely useful for relating structure to function. Development of other approaches include synthesis and structure- function analysis of peptides corresponding to functionally important domains of membrane proteins. This book presents a series of Chapters discussing how a combination of molecular biological, biophysical and theoretical (molecular modelling) techniques are helping us to obtain a much clearer picture of biomembrane structure. After an introductory Chapter on the Principles of membrane Protein Structure, the book is divided into two sections; one dealing with crystallographic approaches and the other non-crystallographic approaches such as NMR, AFM, SPR and FTIR spectroscopy. Chapters dealing with the recently solved crystal structure of cytochrome oxidase and bacteriorhodopsin are presented. The book contains contributions from leading membrane scientists describing their latest studies. It provides an up to date coverage of the developments in the field of biomembranes with particular emphasis on membrane proteins.
Download or read book Biomembranes written by Robert B. Gennis and published by Springer Science & Business Media. This book was released on 2013-04-17 with total page 549 pages. Available in PDF, EPUB and Kindle. Book excerpt: New textbooks at all levels of chemistry appear with great regularity. Some fields like basic biochemistry, organic reaction mechanisms, and chemical thermody namics are well represented by many excellent texts, and new or revised editions are published sufficiently often to keep up with progress in research. However, some areas of chemistry, especially many of those taught at the graduate level, suffer from a real lack of up-to-date textbooks. The most serious needs occur in fields that are rapidly changing. Textbooks in these subjects usually have to be written by scientists actually involved in the research which is advancing the field. It is not often easy to persuade such individuals to set time aside to help spread the knowledge they have accumulated. Our goal, in this series, is to pinpoint areas of chemistry where recent progress has outpaced what is covered in any available textbooks, and then seek out and persuade experts in these fields to produce relatively concise but instructive introductions to their fields. These should serve the needs of one semester or one quarter graduate courses in chemistry and biochemistry. In some cases, the availability of texts in active research areas should help stimulate the creation of new courses.
Book Synopsis Antimicrobial Peptides by : Katsumi Matsuzaki
Download or read book Antimicrobial Peptides written by Katsumi Matsuzaki and published by Springer. This book was released on 2019-04-12 with total page 304 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book presents an overview of antimicrobial peptides (AMPs), their mechanisms of antimicrobial action, other activities, and various problems that must still be overcome regarding their clinical application. Divided into four major parts, the book begins with a general overview of AMPs (Part I), and subsequently discusses the various mechanisms of antimicrobial action and methods for researching them (Part 2). It then addresses a range of activities other than antimicrobial action, such as cell penetration, antisepsis, anticancer, and immunomodulatory activities (Part 3), and explores the prospects of clinical application from various standpoints such as the selective toxicity, design, and discovery of AMPs (Part 4). A huge number of AMPs have been discovered in plants, insects, and vertebrates including humans, and constitute host defense systems against invading pathogenic microorganisms. Consequently, many attempts have been made to utilize AMPs as antibiotics. AMPs could help to solve the urgent problem of drug-resistant bacteria, and are also promising with regard to sepsis and cancer therapy. Gathering a wealth of information, this book will be a bible for all those seeking to develop antibiotics, anti-sepsis, or anticancer agents based on AMPs.
Book Synopsis Nisin and Novel Lantibiotics by : G. Jung
Download or read book Nisin and Novel Lantibiotics written by G. Jung and published by Springer Science & Business Media. This book was released on 1991-12-31 with total page 518 pages. Available in PDF, EPUB and Kindle. Book excerpt: Proceedings of the First International Workshop on Lantibiotics, April 15-18, 1991, Physikzentrum Bad Honnef, F.R.G.
Book Synopsis The Amphipathic Helix by : Richard M. Epand
Download or read book The Amphipathic Helix written by Richard M. Epand and published by CRC Press. This book was released on 1993-07-09 with total page 422 pages. Available in PDF, EPUB and Kindle. Book excerpt: The Amphipathic Helix is a comprehensive volume discussing amphipathic helices in systems as diverse as serum lipoproteins, lung surfactant, cytotoxic peptides, ion channels, mitochondrial targeting, peptide hormones, G proteins, T-cell recognition, DNA binding proteins, and antifreeze proteins. The book also includes general introductory material that defines amphipathic helices, discusses methods to identify amphipathic helical segments from the amino acid sequence of a protein, illustrates how amphipathic helices can be used in the de novo design of peptide and protein structures, and describes how these helices stabilize protein structures. There is also a section on techniques to determine helix orientation in a membrane environment using polarized attenuated total reflection infrared spectroscopy or solid state NMR spectroscopy. Recent developments on all these topics have been discussed by leading experts in this reference for researchers and students in biochemistry, biophysics, and pharmacology.
Book Synopsis Biologically Active Peptides by : Fidel Toldra
Download or read book Biologically Active Peptides written by Fidel Toldra and published by Academic Press. This book was released on 2021-06-17 with total page 819 pages. Available in PDF, EPUB and Kindle. Book excerpt: Biologically Active Peptides: From Basic Science to Applications for Human Health stands as a comprehensive resource on bioactive peptide science and applications. With contributions from more than thirty global experts, topics discussed include bioactive peptide science, structure-activity relationships, best practices for their study and production, and their applications. In the interdisciplinary field of bioactive peptides, this book bridges the gap between basic peptide chemistry and human physiology, while reviewing recent advances in peptide analysis and characterization. Methods and technology-driven chapters offer step-by-step guidance in peptide preparation from different source materials, bioactivity assays, analysis and identification of bioactive peptides, encoding bioactive peptides. Later, applications across disease areas and medical specialties are examined in-depth, including the use of bioactive peptides in treating obesity, diabetes, osteoporosis, mental health disorders, food allergies, and joint health, among other disorders, as well as bioactive peptides for sensory enhancement, sports and clinical nutrition, lowering cholesterol, improving cardiovascular health, and driving advances in biotechnology. Discusses the latest advances in bioactive peptide chemistry, functionality and analysis Offers step-by-step instruction in applying new technologies for peptide extraction, protection, production and encoding, as well as employing bioactive peptide sequencing and bioactivity assays in new research Effectively links basic peptide chemistry, human biology and disease Features chapter contributions from international experts across disciplines and applications
Book Synopsis Chemical Synthesis of Peptides by : Fernando Albericio
Download or read book Chemical Synthesis of Peptides written by Fernando Albericio and published by Wiley. This book was released on 2020-03-13 with total page 300 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Book Synopsis Chemical Approaches to the Synthesis of Peptides and Proteins by : Paul Lloyd-Williams
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.
Book Synopsis The World of Peptides by : Theodor Wieland
Download or read book The World of Peptides written by Theodor Wieland and published by Springer Science & Business Media. This book was released on 2012-12-06 with total page 311 pages. Available in PDF, EPUB and Kindle. Book excerpt: Almost two centuries ago proteins were recognized as the primary materials (proteios = primary) oflife, but the significance and wide role of peptides (from pepsis = digestion) in practically all life pro cesses has only become apparent in the last few decades. Biologi cally active peptides are now being discovered at rapid intervals in the brain and in other organs including the heart, in the skin of amphibians and many other tissues. Peptides and peptide-like compounds are found among toxins and antibiotics. It is unlikely that this process, an almost explosive broadening of the field, will come to a sudden halt. By now it is obvious that Nature has used the combination of a small to moderate number of amino acids to generate a great variety of agonists with specific and often highly sophisticated functions. Thus, peptide chemistry must be regarded as a discipline in its own right, a major branch of biochemistry, fairly separate from the chemistry of proteins. Because of the important role played by synthesis both in the study and in the practical preparation of peptides, their area can be considered as belonging to bio-organic chemistry as well. The already overwhelming and still increasing body of know ledge renders an account of the history of peptide chemistry more and more difficult. It appears therefore timely to look back, to take stock and to recall the important stages in the development of a new discipline.
Book Synopsis Medicinal Natural Products by : Paul M. Dewick
Download or read book Medicinal Natural Products written by Paul M. Dewick and published by John Wiley & Sons. This book was released on 2002-01-03 with total page 524 pages. Available in PDF, EPUB and Kindle. Book excerpt: This guide covers classes of natural products in medicine, whether derived from plants, micro-organisms or animals. Structured according to biosynthetic pathway, it is written from a chemistry-based approach.
Book Synopsis Chemical Epigenetics by : Antonello Mai
Download or read book Chemical Epigenetics written by Antonello Mai and published by Springer Nature. This book was released on 2020-03-31 with total page 569 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book presents an authoritative review of the most significant findings about all the epigenetic targets (writers, readers, and erasers) and their implication in physiology and pathology. The book also covers the design, synthesis and biological validation of epigenetic chemical modulators, which can be useful as novel chemotherapeutic agents. Particular attention is given to the chemical mechanisms of action of these molecules and to the drug discovery prose which allows their identification. This book will appeal to students who want to know the extensive progresses made by epigenetics (targets and modulators) in the last years from the beginning, and to specialized scientists who need an instrument to quickly search and check historical and/or updated notices about epigenetics.
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
