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Synthesis And Characterization Of Peptide Macrocycles As Novel Bimodal Proteasome Inhibitors
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Book Synopsis Synthesis and Characterization of Peptide Macrocycles as Novel, Bimodal Proteasome Inhibitors by : David Lawrence Wilson
Download or read book Synthesis and Characterization of Peptide Macrocycles as Novel, Bimodal Proteasome Inhibitors written by David Lawrence Wilson and published by . This book was released on 2015 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: The proteasome is a large, multicatalytic protease found in all forms of life. The proteasome is instrumental in the regulation of many cellular pathways such as cell cycle arrest and cell proliferation. For this reason, proteasome inhibitors are of interest in drug development because of their ability to regulate the asynchronous cell cycles of cancers. In particular, multiple myeloma has been shown to be receptive to treatment with proteasome inhibitors. In this study, two novel macrocyclic peptidyl aldehyde proteasome inhibitors 11 and 12 are reported. The design of 11 and 12 was bioinspired by the natural product TMC-95A, a macrocyclic tripeptide shown to potently and selectively inhibit the proteasome. Compounds 11 and 12 were designed to test the effects of the peptide macrocycle on inhibitory strength and specificity. Both inhibitors were identical in sequence, however 12 incorporated a biaryl ether linkage to mimic the macrocyclic structure of TMC-95. Additionally, both inhibitors incorporated a C-terminal aldehyde designed to covalently bind the proteasome's catalytic threonine residue and hydrophobic side chains to target the chymotrypsin-like activity of the proteasome. In vitro testing of both inhibitors revealed them to be potent and specific inhibitors of the chymotrypsin-like activity of the proteasome (11, Ki = 33 nM, 12, Ki = 76 nM). It was found that there was no trend to suggest that the peptide macrocycle conferred increased specificity or binding. Ex vivo assays for 12 showed it to be metabolically stable, readily taken up by HeLa cells, and perform on par with the well characterized proteasome inhibitor MG-132. Finally, QM/MM studies suggested that the oxindole moiety found in the macrocycle of TMC-95A is essential for specificity for the chymotrypsin-like active site of the proteasome.
Book Synopsis Synthesis, Characterization, and Potency of Novel Bimodal Proteasome Inhibitors by : Frederick Michael Tomlin
Download or read book Synthesis, Characterization, and Potency of Novel Bimodal Proteasome Inhibitors written by Frederick Michael Tomlin and published by . This book was released on 2013 with total page 100 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Book Synopsis Peptide Macrocycles by : Matthew B. Coppock
Download or read book Peptide Macrocycles written by Matthew B. Coppock and published by Humana. This book was released on 2022-10-02 with total page 0 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.
Book Synopsis Structure-based Design and Synthesis of Bimodal Proteasome Inhibitors as Therapeutic Agents by : Zack Michael Strater
Download or read book Structure-based Design and Synthesis of Bimodal Proteasome Inhibitors as Therapeutic Agents written by Zack Michael Strater and published by . This book was released on 2014 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: The proteasome is a multicatalytic enzyme responsible for degrading damaged, misfolded, and uneeded intracellular proteins. Since many vital cellular pathways rely on the degradative function of the proteasome, its dysregulation is implicated in the pathology of several diseases, thus making it an attractive target for inhibition. Here we report two novel tetrapeptide aldehyde inhibitors based on the structure of natural product TMC-95A, a potent noncovalent inhibitor of the proteasome. Conversion of the carbonyl of the C-terminal residue to an aldehyde enabled these inhibitors to covalently bind to the catalytic Thr residue of the proteasome's active site. The P1 and P3 residues, which engage with the primary active site pockets, were varied to mimic TMC-95A and MG-132, a well known peptide aldehyde proteasome inhibitor. The combination of covalent and noncovalent mechanisms of binding to the active site allow these compounds to bimodally inhibit the proteasome. Additionally, the P2 and P4 residues of two of the inhibitors were cyclized via a biaryl ether moiety in order to mimic the synthetically inaccessible macrocycle found in TMC-95A. The compounds were then tested in vitro with 20S proteasome using fluorometric reversible kinetics. The two macrocyclic lead compounds were also compared to linear peptide aldehyde analogs that were prepared and tested in the same fashion to the macrocycles. The resulting inhibition constants were used to evaluate the effect of the macrocycle, the addition of the aldehyde functionality, and to compare the different amino acid sequences. The aldehyde was found to greatly increase potency compared to noncovalent inhibitors with a similar structure. The compounds with amino acid sequences similar to MG-132 were the most potent (Ki̳ = 33 nM, 76 nm) while the cyclic compounds were found to be slightly less potent than their linear analogues. These compounds were also tested with chymotrypsin, calpain, and cruzain to investigate their inhibitory specificity. The kinetic data demonstrated that the general structure of the inhibitors showed much greater affinity for the proteasome than for the other proteases tested.
Book Synopsis Self-Assembled Nanostructures by : Jin Zhang
Download or read book Self-Assembled Nanostructures written by Jin Zhang and published by Springer Science & Business Media. This book was released on 2006-04-11 with total page 327 pages. Available in PDF, EPUB and Kindle. Book excerpt: Nanostructures refer to materials that have relevant dimensions on the nanometer length scales and reside in the mesoscopic regime between isolated atoms and molecules in bulk matter. These materials have unique physical properties that are distinctly different from bulk materials. Self-Assembled Nanostructures provides systematic coverage of basic nanomaterials science including materials assembly and synthesis, characterization, and application. Suitable for both beginners and experts, it balances the chemistry aspects of nanomaterials with physical principles. It also highlights nanomaterial-based architectures including assembled or self-assembled systems. Filled with in-depth discussion of important applications of nano-architectures as well as potential applications ranging from physical to chemical and biological systems, Self-Assembled Nanostructures is the essential reference or text for scientists involved with nanostructures.
Book Synopsis Protein Self-Assembly by : Jennifer J. McManus
Download or read book Protein Self-Assembly written by Jennifer J. McManus and published by Humana. This book was released on 2020-08-08 with total page 266 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume explores experimental and computational approaches to measuring the most widely studied protein assemblies, including condensed liquid phases, aggregates, and crystals. The chapters in this book are organized into three parts: Part One looks at the techniques used to measure protein-protein interactions and equilibrium protein phases in dilute and concentrated protein solutions; Part Two describes methods to measure kinetics of aggregation and to characterize the assembled state; and Part Three details several different computational approaches that are currently used to help researchers understand protein self-assembly. 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. Thorough and cutting-edge, Protein Self-Assembly: Methods and Protocols is a valuable resource for researchers who are interested in learning more about this developing field.
Book Synopsis Ion Mobility-Mass Spectrometry by : Giuseppe Paglia
Download or read book Ion Mobility-Mass Spectrometry written by Giuseppe Paglia and published by Humana. This book was released on 2019-11-15 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book focuses on ion mobility-mass spectrometry (IM-MS) and informatics approaches to improve traditional analysis of molecules by providing fundamentals and protocols for exploiting the potential of state-of-the-art IM-MS technology for the most common analytical applications. The chapters have been organized into four parts, each dealing with a particular set of IM-MS applications: 1) metabolomics and lipidomics; 2) proteomics and glycomics; 3) imaging and ambient ionization IM-MS; and 4) bioinformatic solutions for analyzing IM-MS data and deriving CCS values. Written for the highly successful Methods in Molecular Biology series, 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. Authoritative and practical, Ion Mobility-Mass Spectrometry: Methods and Protocols serves as an ideal resource for scientists delving into the technique's unprecedented analytical advantages, enabling novel qualitative and quantitative applications for the analysis of complex biological samples.
Download or read book Macromolecules written by F Bovey and published by Elsevier. This book was released on 2012-12-02 with total page 566 pages. Available in PDF, EPUB and Kindle. Book excerpt: Macromolecules is an introductory book about macromolecules, specifically about the fundamental aspects of macromolecules, such as their nature, the ways they are formed, and their behavior. This book also focuses on the basics of macromolecules, which includes history, composition, and properties. The topics covered in this book include polymerization kinetics, chemical reactions, and degradation of macromolecules. This book also discusses biological molecules, including naturally occurring materials, synthetic macromolecules, and model compounds. Students majoring in chemistry or other related fields, such as materials engineering, will find this book very useful.
Book Synopsis Laboratory Manual for Principles of General Chemistry 10E for University of Maryland Baltimore City by : Dömling
Download or read book Laboratory Manual for Principles of General Chemistry 10E for University of Maryland Baltimore City written by Dömling and published by . This book was released on 2017-12-27 with total page 450 pages. Available in PDF, EPUB and Kindle. Book excerpt: By presenting the most successful experimental procedures for MCRs, this book is perfect for every bench chemists in pharmaceutical chemistry and graduate students alike. Written by Alexander Doemling, one of the leading experts with 25 years of laboratory experience.
Book Synopsis Topology of Polymers by : Koya Shimokawa
Download or read book Topology of Polymers written by Koya Shimokawa and published by Springer Nature. This book was released on 2019-12-06 with total page 81 pages. Available in PDF, EPUB and Kindle. Book excerpt: Plastics, films, and synthetic fibers are among typical examples of polymer materials fabricated industrially in massive quantities as the basis of modern social life. By comparison, polymers from biological resources, including proteins, DNAs, and cotton fibers, are essential in various processes in living systems. Such polymers are molecular substances, constituted by the linking of hundreds to tens of thousands of small chemical unit (monomer) components. Thus, the form of polymer molecules is frequently expressed by line geometries, and their linear and non-linear forms are believed to constitute the fundamental basis for their properties and functions. In the field of polymer chemistry and polymer materials science, the choice of macromolecules has continuously been extended from linear or randomly branched forms toward a variety of precisely controlled topologies by the introduction of intriguing synthetic techniques. Moreover, during the first decade of this century, a number of impressive breakthroughs have been achieved to produce an important class of polymers having a variety of cyclic and multicyclic topologies. These developments now offer unique opportunities in polymer materials design to create unique properties and functions based on the form, i.e., topology, of polymer molecules. The introduction and application of topological geometry (soft geometry) to polymer molecules is a crucial requirement to account for the basic geometrical properties of polymer chains uniquely flexible in nature, in contrast to small chemical compounds conceived upon Euclidian geometry (hard geometry) principles. Topological geometry and graph theory are introduced for the systematic classification and notation of the non-linear constructions of polymer molecules, including not only branched but also single cyclic and multicyclic polymer topologies. On that basis, the geometrical–topological relationship between different polymers having distinctive constructions is discussed. A unique conception of topological isomerism is thus formed, which contrasts with that of conventional constitutional and stereoisomerism occurring in small chemical compounds. Through the close collaboration of topology experts Shimokawa and Ishihara and the polymer chemist Tezuka, this monograph covers the fundamentals and selected current topics of topology applied in polymers and topological polymer chemistry. In particular, the aim is to provide novel insights jointly revealed through a unique interaction between mathematics (topology) and polymer materials science.
Book Synopsis Biomolecular Forms and Functions by : Manju Bansal
Download or read book Biomolecular Forms and Functions written by Manju Bansal and published by World Scientific. This book was released on 2013 with total page 515 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume is primarily a compilation of contributed articles representing the impact and application of Ramachandran's work on conformation analysis of biopolymers, as well as recent advances in macromolecular structural biology, involving diverse experimental and computational approaches. This volume is being published to coincide with a conference on "Biomolecular Forms and Functions: A celebration of 50 years of the Ramachandran Map" being held at the Indian Institute of Science, Bangalore, in January 2013.
Book Synopsis Coumarin and Its Derivatives by : Maria João Matos
Download or read book Coumarin and Its Derivatives written by Maria João Matos and published by Mdpi AG. This book was released on 2021-12-29 with total page 416 pages. Available in PDF, EPUB and Kindle. Book excerpt: Coumarins are widely distributed in nature and can be found in a large number of naturally occurring and synthetic bioactive molecules. The unique and versatile oxygen-containing heterocyclic structure makes them a privileged scaffold in Medicinal Chemistry. Many coumarin derivatives have been extracted from natural sources, designed, synthetized, and evaluated on different pharmacological targets. In addition, coumarin-based ion receptors, fluorescent probes, and biological stains are growing quickly and have extensive applications to monitor timely enzyme activity, complex biological events, as well as accurate pharmacological and pharmacokinetic properties in living cells. The extraction, synthesis, and biological evaluation of coumarins have become extremely attractive and rapidly developing topics. A large number of research and review papers have compiled information on this important family of compounds in 2020. Research articles, reviews, communications, and concept papers focused on the multidisciplinary profile of coumarins, highlighting natural sources, most recent synthetic pathways, along with the main biological applications and theoretical studies, were the main focus of this book. The huge and growing range of applications of coumarins described in this book is a demonstration of the potential of this family of compounds in Organic Chemistry, Medicinal Chemistry, and different sciences related to the study of natural products. This book includes 23 articles: 17 original papers and six review papers.
Book Synopsis Therapeutic Proteins by : C. Mark Smales
Download or read book Therapeutic Proteins written by C. Mark Smales and published by Springer Science & Business Media. This book was released on 2008-02-04 with total page 481 pages. Available in PDF, EPUB and Kindle. Book excerpt: With the recent completion of the sequencing of the human genome, it is widely anticipated that the number of potential new protein drugs and targets will escalate at an even greater rate than that observed in recent years. However, identification of a potential target is only part of the process in developing these new next generation protein-based “drugs” that are increasingly being used to treat human disease. Once a potential protein drug has been identified, the next rate-limiting step on the road to development is the production of sufficient authentic material for testing, charact- ization, clinical trials, and so on. If a protein drug does actually make it through this lengthy and costly process, methodology that allows the production of the protein on a scale large enough to meet demand must be implemented. Furthermore, large-scale production must not compromise the authenticity of the final product. It is also nec- sary to have robust methods for the purification, characterization, viral inactivation and continued testing of the authenticity of the final protein product and to be able to formulate it in a manner that retains both its biological activity and lends itself to easy administration. Therapeutic Proteins: Methods and Protocols covers all aspects of protein drug production downstream of the discovery stage. This volume contains contributions from leaders in the field of therapeutic protein expression, purification, characterization, f- mulation, and viral inactivation.
Book Synopsis Chemical Information Management by : Wendy A. Warr
Download or read book Chemical Information Management written by Wendy A. Warr and published by . This book was released on 1992 with total page 292 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Large Ions written by Tomas Baer and published by John Wiley & Sons. This book was released on 1996 with total page 208 pages. Available in PDF, EPUB and Kindle. Book excerpt: Recent advances in both experimental techniques and theoretical methodologies have meant that increasingly sophisticated studies concerning the formation, structures, energetics and reaction dynamics of state- or energy-selected molecular ions can now be performed. In order to better serve the ion chemistry and physics community, each volume of this series is dedicated to reviewing a specific topic, emphasizing new experimental and theoretical developments in the study of ions. The Wiley Series in Ion Chemistry and Physics will help stimulate new research directions and point to future opportunities in the field of ion chemistry and physics. This volume, the sixth in the series, concentrates on the area of large ions. The production, detection and analysis of large ions are areas which have taken on great importance in recent years, in particular in the biomedical and biochemical fields. The understanding of large ions presents unique and formidable challenges which are very different from those associated with the study of small ions. This volume focuses on some of the fundamental chemistry and physics associated with the behavior of large ions, with the contributors addressing the issues in a quantitative fashion, in order to elucidate clearly some of the key recent advances which have taken place. As such, Large Ions: Their Vaporization, Detection and Structural Analysis provides an excellent snapshot of current research in this fascinating and important area. The six chapters are written by some of the leading experts in the field, and together they will be of great interest to experts and newcomers, both of whom will benefit from the in-depth discussion of the latest methods and results.
Book Synopsis Molecules and Medicine by : E. J. Corey
Download or read book Molecules and Medicine written by E. J. Corey and published by John Wiley & Sons. This book was released on 2012-02-28 with total page 272 pages. Available in PDF, EPUB and Kindle. Book excerpt: Molecules and Medicine provides, for the first time ever, a completely integrated look at chemistry, biology, drug discovery, and medicine. It delves into the discovery, application, and mode of action of more than one hundred of the most significant molecules in use in modern medicine. Opening sections of the book provide a unique, clear, and concise introduction, which enables readers to understand chemical formulas.
Book Synopsis Transport Properties of Ions in Gases by : Edward A. Mason
Download or read book Transport Properties of Ions in Gases written by Edward A. Mason and published by Wiley-VCH. This book was released on 1988-08-09 with total page 584 pages. Available in PDF, EPUB and Kindle. Book excerpt: Presents thorough coverage of the transport properties of ions in gases. Starts from first principles, making this book useful to those new to the field as well as to experts. Describes the motions of ions in gases in electric fields, methods for measuring mobilities and diffusion coefficients, and pitfalls in measuring these quantities. Provides a detailed development of the theory of transport processes in the context of the kinetic theory of gases. Includes relevant experimental techniques and an index to experimental data.
