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Design And Synthesis Of Novel Amino Acids And Their Use In Synthesis Of B Turn Mimetics And Their Incorporation Into Biological Active Peptides Phd
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Book Synopsis Design and Synthesis of Novel Amino Acids and Their Use in Synthesis of B-Turn Mimetics and Their Incorporation Into Biological Active Peptides (PHD). by : Xuyuan Gu
Download or read book Design and Synthesis of Novel Amino Acids and Their Use in Synthesis of B-Turn Mimetics and Their Incorporation Into Biological Active Peptides (PHD). written by Xuyuan Gu and published by . This book was released on with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Book Synopsis PART I. DESIGN AND SYNTHESIS OF BICYCLIC INTERNAL BETA-TURN MIMETICS AND THEIR INCORPORATION INTO BIOLOGICALLY ACTIVE LIGANDS; PART II. SYNTHESIS OF CYCLIC PEPTIDES BY RING. by :
Download or read book PART I. DESIGN AND SYNTHESIS OF BICYCLIC INTERNAL BETA-TURN MIMETICS AND THEIR INCORPORATION INTO BIOLOGICALLY ACTIVE LIGANDS; PART II. SYNTHESIS OF CYCLIC PEPTIDES BY RING. written by and published by . This book was released on 2010 with total page 604 pages. Available in PDF, EPUB and Kindle. Book excerpt: Beta-Turns in many biologically active peptides are important secondary structural elements which are critical for their biological activities. Hence, it is not surprising that beta-turn based pharmacophore design including beta-turn mimetics has become a central topic in medicinal chemistry in addition to alpha-helix or helical peptides. One of the advantages of such beta-turn mimetics is that they can better control torsion angles of the backbone of peptides and to some degree dihedral angles chi (X). These beta-turn mimicking scaffolds are designed to have a higher avidity for the acceptor by overcoming what otherwise is the inherent entropic cost paid for beta-turn formation upon binding to the acceptor. Among different synthetic strategies to bicyclic structures as beta-turn mimetics, consecutive formation of bicyclic structures using tandem acid-catalyzed N-acyliminium ion cyclization is attractive since this methodology was well established in the synthesis of natural product alkaloids. 1,3,6,8-Substituted tetrahydro-2H-pyrazino[1,2-a]pyrimidine-4,7-diones were designed and synthesized as internal beta-turn mimetics through an acid-catalyzed tandem acyliminium ion cyclization. Its development and synthesis are decribed in Chapter 2 to Chapter 4. Its application toward the development and synthesis of a small molecule ligand for melanocortin receptors is described in Chapter 5. In addition, the development of peptidomimetics for opioid receptors is explained in Chapter 6. On the other hand, a dicarba analogue having opioid receptor agonist, and dicarba analogues for MCRs were synthesized through solid phase synthesis including a ring closing metathesis reaction using Grubbs' catalyst (I) in Chapter 8.
Book Synopsis The Design and Synthesis of Novel -substituted Amino Acids, Bicyclic Dipeptide Mimetics, and Their Incorporation Into Cholecystokinin/opioid Chimeric Peptides (PHD). by : John M. Ndungu
Download or read book The Design and Synthesis of Novel -substituted Amino Acids, Bicyclic Dipeptide Mimetics, and Their Incorporation Into Cholecystokinin/opioid Chimeric Peptides (PHD). written by John M. Ndungu and published by . This book was released on with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Book Synopsis Biologically Active Peptides by : David B. Weiner
Download or read book Biologically Active Peptides written by David B. Weiner and published by CRC Press. This book was released on 1993-11-04 with total page 382 pages. Available in PDF, EPUB and Kindle. Book excerpt: Investigation into basic and advanced peptide design, synthesis, evaluation and utilization. New therapeutic approaches from experimental systems.
Book Synopsis Peptide Synthesis and Applications by : John Howl
Download or read book Peptide Synthesis and Applications written by John Howl and published by Springer Science & Business Media. This book was released on 2008-02-02 with total page 263 pages. Available in PDF, EPUB and Kindle. Book excerpt: Hands-on experts describe in step-by-step detail the key methodologies of contemporary peptide synthesis and illustrate their numerous applications. The techniques presented include protocols for chemical ligation, the synthesis of cyclic and phosphotyrosine-containing peptides, lipoamino acid- and sugar-conjugated peptides, and peptide purification and analyses. Additional chapters detail methodologies and instrumentation for high-throughput peptide synthesis, many different applications of peptides as novel research tools and biological probes, and the design and application of fluorescent substrate-based peptides that can be used to determine the selectivity and activity of peptidases. A practical guide to the identification of proteins using mass spectrometric analyses of peptide mixtures is also included.
Book Synopsis The DESIGN AND SYNTHESIS OF NOVEL UNNATURAL AMINO ACIDS AND THE DESIGN AND SYNTHESIS OF PEPTIDES & PEPTIDOMIMETICS CONTAINING UNNATURAL AMINO ACIDS FOR THE STUDY OF G-PROTEIN COUPLED RECEPTORS. by :
Download or read book The DESIGN AND SYNTHESIS OF NOVEL UNNATURAL AMINO ACIDS AND THE DESIGN AND SYNTHESIS OF PEPTIDES & PEPTIDOMIMETICS CONTAINING UNNATURAL AMINO ACIDS FOR THE STUDY OF G-PROTEIN COUPLED RECEPTORS. written by and published by . This book was released on 2010 with total page 454 pages. Available in PDF, EPUB and Kindle. Book excerpt: Nature has gifted peptides as important modulators in the human body, but these types of molecules often have not been favored when we were looking for therapeutic agents. The poor bioavailability, fast degradation and until recent high manufacturing costs of some bioactive peptides lowered their potential usage in the health industry. Under these circumstances, unnatural amino acids were developed as indispensible tools providing enormous support to peptide science. By incorporating proper unnatural amino acids into a peptide or protein, we now can significantly improve peptide's or protein's half-life, cell permeability, bio-distribution, etc. In addition, their potency and receptor/acceptor selectivity could also be enhanced. Site-specific modifications of peptides and proteins under physiological conditions with the use of unnatural amino acids also have been made easier with the advance of biotechnology. Therefore, my research described in this dissertation contributes to the efforts in the development of novel unnatural amino acids. In particular, I have focused on novel methods in the synthesis of anti beta-functionalized gamma, delta-unsaturated amino acids. These amino acids have special interests in peptide chemistry: they can provide conformational constraints to the peptide 3D structures; the beta-functionalization allows the introduction of pharmaceutically interesting side chain groups; and the terminal double bond which is orthogonal to peptide synthesis provides access to further chemical modifications. Two general methodologies for the synthesis of both racemic and optically active anti beta-functionalized gamma, delta--unsaturated amino acids were developed by using the thio-Claisen rearrangement (TCR) reaction. Excellent diastereoselectivies and enantioselectivities were obtained when C2-symmetric chiral auxiliaries were selected to control the stereochemistry outcome. The mechanism and the scope of the TCR reaction were also studied, showing unique advantages in the preparation of these biological interesting amino acids. Another effort of developing angiotensin II type 1 (AT1) receptor biased peptide ligands is also documented in this dissertation. The AT1 receptor is a 7-transmembrane G-protein coupled receptor, which recent researches have shown could be activated through a beta-arrestins only, but G-protein independent, pathway. We synthesized 12 analogs of Sar1,Ile4,Ile8-AngII (SII), and tested them in biological assays, and obtained valuable information for further "perfect" biased ligands design.
Book Synopsis Biologically Active Peptides by : David B. Weiner
Download or read book Biologically Active Peptides written by David B. Weiner and published by CRC Press. This book was released on 2023-07-28 with total page 377 pages. Available in PDF, EPUB and Kindle. Book excerpt: Investigation into basic and advanced peptide design, synthesis, evaluation and utilization. New therapeutic approaches from experimental systems.
Book Synopsis Synthesis of Novel Amino Acids and Use of Peptides & Peptidomimetics Containing Unnatural Amino Acids for the Development of Selective Melanocortin Peptide Antagonists and for the Study of Melanocortin Receptor Signaling by : Hongchang Qu
Download or read book Synthesis of Novel Amino Acids and Use of Peptides & Peptidomimetics Containing Unnatural Amino Acids for the Development of Selective Melanocortin Peptide Antagonists and for the Study of Melanocortin Receptor Signaling written by Hongchang Qu and published by . This book was released on 2007 with total page 366 pages. Available in PDF, EPUB and Kindle. Book excerpt: Unnatural amino acids are indispensible tools, not only for the elucidation of molecular mechanisms during the study of the complicated biological system, but also for the development of novel peptide and protein drugs with better efficacy and lower toxicity. Beta-substituted gamma, delta-unsaturated amino acids have been shown to be an important type of novel amino acid because of the terminal double bond which can be converted to many other functionalities. The methodology for the synthesis of syn-beta-substituted gamma, delta-unsaturated amino acids has been developed. However, there is no satisfactory general method for the synthesis of anti-beta-substituted gamma, delta-unsaturated amino acids. Therefore, a general methodology was developed by using the Eschenmoser-Claisen rearrangement for the synthesis of both racemic and optically active anti-beta-substituted gamma, delta-unsaturated amino acids. This rearrangement is highly diastereoselective and good asymmetric induction was obtained with a relatively small C2-symmetric chiral auxiliary (2R,5R)-dimethylpyrrolidine. In an effort to design peptide antagonists that are selective for human melanocortin 4 receptor, highly constrained trans and cis 4-guanidinium proline derivatives were synthesized and incorporated in various melanotropin analogues designed to mimic the endogenous hMC1,4R selective antagonist hASIP (Agouti Signaling Protein) central loop. Biologicalassays show that some of these analogues are highly selective for hMC1R and/or hMC4R with partial agonist or antagonist activities due to a new beta-turn structure induced by the presence of the constrained amino acids. According to molecular modeling studies, the lowest energy conformations of these selective analogues resemble the NMR solution structure of the hASIP central loop. Therefore, a new template was developed for the rational design of novel selective melanotropin analogues that may have therapeutic potential. To further understand the molecular mechanisms of hMC4R signaling upon agonist activation, an hMC4R selective nonpeptide agonist THIQ and its fluorescent dye labeled derivatives were needed to compare to peptide agonist MTII with regard to receptor phosphorylation, internalization, etc. An improved synthetic method was developed for the efficient synthesis of THIQ. A method for the synthesis of TRITC labeled THIQ derivatives was also developed.
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 2020-08-18 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 Synthesis of Novel Amino Acids with Incorporation Into Peptides and Synthesis of Peptides with Novel Aggregation States by : Scott Michael Cowell
Download or read book Synthesis of Novel Amino Acids with Incorporation Into Peptides and Synthesis of Peptides with Novel Aggregation States written by Scott Michael Cowell and published by . This book was released on 1996 with total page 148 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Book Synopsis Peptide Applications in Biomedicine, Biotechnology and Bioengineering by : Sotirios Koutsopoulos
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
Book Synopsis Peptide and Protein Design for Biopharmaceutical Applications by : Knud Jensen
Download or read book Peptide and Protein Design for Biopharmaceutical Applications written by Knud Jensen and published by John Wiley & Sons. This book was released on 2009-09-01 with total page 306 pages. Available in PDF, EPUB and Kindle. Book excerpt: Peptides serve as effective drugs in the clinic today. However the inherent drawbacks of peptide structures can limit their efficacy as drugs. To overcome this researchers are developing new methods to create ‘tailor-made’ peptides and proteins with improved pharmacological properties. Design of Peptides and Proteins provides an overview of the experimental and computational methods for peptide and protein design, with an emphasis on specific applications for therapeutics and biomedical research. Topics covered include: Computer modeling of peptides and proteins Peptidomimetics Design and synthesis of cyclic peptides Carbohydrates in peptide and protein design De novo design of peptides and proteins Medical development applications An extended case study – the design of insulin variants Design of Peptides and Proteins presents the state-of-the-art of this exciting approach for therapeutics, with contributions from international experts. It is an essential resource for academic and industrial scientists in the fields of peptide and protein drug design, biomedicine, biochemistry, biophysics, molecular modelling, synthetic organic chemistry and medicinal/pharmaceutical chemistry.
Book Synopsis Studies on Chemical Synthesis of Peptides: Efficient Synthetic Methods for β-Amino Acids, Azides, Amino Acid Hydroxamates and Esters by : Vasanthakumar Ganga Ramu
Download or read book Studies on Chemical Synthesis of Peptides: Efficient Synthetic Methods for β-Amino Acids, Azides, Amino Acid Hydroxamates and Esters written by Vasanthakumar Ganga Ramu and published by GRIN Verlag. This book was released on 2011-10-17 with total page 186 pages. Available in PDF, EPUB and Kindle. Book excerpt: Doctoral Thesis / Dissertation from the year 2004 in the subject Chemistry - Organic Chemistry, Bangalore University / Central College (Department of Studies in Chemistry), language: English, abstract: The importance of ß-amino acids has been focused, particularly in the past few decades. They are found as components of many biologically active peptidic and nonpeptidic natural products with antibiotic, antifungal, cytotoxic, and other pharmacological properties. ß-Amino acids are produced in humans, animals, microorganisms, marine organisms, and plants either in free state or as part of a peptide or depsipeptide. The importance of nonpeptidic ß-amino acids has been nfocused particularly on the ß-lactam antibiotics, since naturally occurring penicillin derivatives have been discovered as broad antibiotic active agents. Over the years, a large number of these compounds have been prepared and tested, and a variety of new ß-lactam ring systems have been introduced such as cephems, cephalosporins, oxacephems, penems, carbapenems, oxapenams as well as monocyclic and polycyclic ring systems. ß-Amino acids have been known to play an important role in primary and secondary metabolism also. [...]
Book Synopsis The Design and Synthesis of Peptide Turn Mimetics by : Peter Joseph Cassidy
Download or read book The Design and Synthesis of Peptide Turn Mimetics written by Peter Joseph Cassidy and published by . This book was released on 1998 with total page 658 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Book Synopsis The Design and Synthesis of [beta]-amino Acids by : John Francis Mehlmann
Download or read book The Design and Synthesis of [beta]-amino Acids written by John Francis Mehlmann and published by . This book was released on 2000 with total page 34 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Book Synopsis Principles of Peptide Synthesis by : M. Bodanszky
Download or read book Principles of Peptide Synthesis written by M. Bodanszky and published by Springer Science & Business Media. This book was released on 2012-12-06 with total page 320 pages. Available in PDF, EPUB and Kindle. Book excerpt: A look at the shelves of a major library awakens doubts in the author of this small volume about the importance of writing a new introduction to peptide synthesis. This rather narrow area of bio-organic chemistry already has received considerable attention. A whole series of books deals with the synthesis of peptides. Some of these are textbooks written to support lecture courses on peptide synthesis. Others try to help the beginner, otherwise well versed in organic chemistry, to embark on some experimental project that requires the construction of peptide chains. Not less useful are the monographs which were compiled to aid the adept practitioner and to provide him with references to the growing literature of a very active field. Is there any need for a new book on peptide synthesis? Should we add a new volume to an already impressive and certainly useful series? The answer is not obvious. The author has already participated in two similar en deavors. The first edition! of "Peptide Synthesis", with M. A. Ondetti as coauthor, was meant to serve as an introduction for the beginner. It was rather well received by researchers who joined the field of peptide chemistry and were looking for initiation. While working on the 2 second edition with Drs. Klausner and Ondetti, we became painfully aware of the impossibility of the task.
Download or read book Peptides written by Channa Basava and published by Springer Science & Business Media. This book was released on 1994-04 with total page 340 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.
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