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cleavable linkers in chemical biology: Chemical Proteomics Gerard Drewes, Marcus Bantscheff, 2011-11-08 The multidisciplinary science of chemical proteomics studies how small molecules of synthetic or natural origin bind to proteins and modulate their function. In Chemical Proteomics: Methods and Protocols, expert researchers in the field provide key techniques to investigate chemical proteomics focusing on analytical strategies, how probes are generated, techniques for the discovery of small molecule targets and the probing of target function, and small molecule ligand and drug discovery. Written in the highly successful Methods in Molecular BiologyTM series format, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and key tips on troubleshooting and avoiding known pitfalls. Authoritative and practical, Chemical Proteomics : Methods and Protocols seeks to provide methodologies that will contribute to a wider application of chemical proteomics methods in biochemical and cell biological laboratories. |
cleavable linkers in chemical biology: Linker Strategies in Solid-Phase Organic Synthesis Peter Scott, 2009-10-13 Linker design is an expanding field with an exciting future in state-of-the-art organic synthesis. Ever-increasing numbers of ambitious solution phase reactions are being adapted for solid-phase organic chemistry and to accommodate them, large numbers of sophisticated linker units have been developed and are now routinely employed in solid-phase synthesis. Linker Strategies in Solid-Phase Organic Synthesis guides the reader through the evolution of linker units from their genesis in solid-supported peptide chemistry to the cutting edge diversity linker units that are defining a new era of solid phase synthesis. Individual linker classes are covered in easy to follow chapters written by international experts in their respective fields and offer a comprehensive guide to linker technology whilst simultaneously serving as a handbook of synthetic transformations now possible on solid supports. Topics include: the principles of solid phase organic synthesis electrophile and nucleophile cleavable linker units cyclative cleavage as a solid phase strategy photocleavable linker units safety-catch linker units enzyme cleavable linker units T1 and T2 –versatile triazene linker groups hydrazone linker units benzotriazole linker units phosphorus linker units sulfur linker units selenium and tellurium linker units sulfur, oxygen and selenium linker units cleaved by radical processes silicon and germanium linker units boron and stannane linker units bismuth linker units transition metal carbonyl linker units linkers releasing olefins or cycloolefins by ring-closing metathesis fluorous linker units solid-phase radiochemistry The book concludes with extensive linker selection tables, cataloguing the linker units described in this book according to the substrate liberated upon cleavage and conditions used to achieve such cleavage, enabling readers to choose the right linker unit for their synthesis. Linker Strategies in Solid-Phase Organic Synthesis is an essential guide to the diversity of linker units for organic chemists in academia and industry working in the broad areas of solid-phase organic synthesis and diversity oriented synthesis, medicinal chemists in the pharmaceutical industry who routinely employ solid-phase chemistry in the drug discovery business, and advanced undergraduates, postgraduates, and organic chemists with an interest in leading-edge developments in their field. |
cleavable linkers in chemical biology: Activity-Based Proteomics Herman S. Overkleeft, Bogdan I. Florea, 2018-07-10 This volume focuses on explorative activity-based proteomics, biomedical applications of activity-based proteomics, and chemical strategies in activity-based proteomics providing a concise overview of activity-based protein profiling. 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. Authoritative and cutting-edge, Activity-Based Proteomics: Methods and Protocols aims to ensure successful results in the further study of this vital field. |
cleavable linkers in chemical biology: Antibody-Drug Conjugates Laurent Ducry, 2016-08-23 Antibody-drug conjugates (ADCs) represent a promising therapeutic approach for cancer patients by combining the antigen-targeting specificity of monoclonal antibodies (mAbs) with the cytotoxic potency of chemotherapeutic drugs. In Antibody-Drug Conjugates, expert researchers provide detailed protocols for many of the key ADC techniques necessary for working in the field. These chapters and methodologies are aimed at the key tasks necessary to identify a suitable target, properly design the mAb, the linker and the payload, as well as to conjugate them in a reproducible and scalable fashion. Written in the highly successful Methods in Molecular BiologyTM format, these detailed chapters include the kind of practical implementation advice that guarantees quality results. Authoritative and timely, Antibody-Drug Conjugates aims to further drive ADC development and thus help toward improving cancer treatments of the future. |
cleavable linkers in chemical biology: Bioconjugate Techniques Greg T. Hermanson, 2010-07-26 Bioconjugate Techniques, 2nd Edition, is the essential guide to the modification and cross linking of biomolecules for use in research, diagnostics, and therapeutics. It provides highly detailed information on the chemistry, reagent systems, and practical applications for creating labeled or conjugate molecules. It also describes dozens of reactions with details on hundreds of commercially available reagents and the use of these reagents for modifying or cross linking peptides and proteins, sugars and polysaccharides, nucleic acids and oligonucleotides, lipids, and synthetic polymers. A one-stop source for proven methods and protocols for synthesizing bioconjugates in the lab Step-by-step presentation makes the book an ideal source for researchers who are less familiar with the synthesis of bioconjugates More than 600 figures that visually describe the complex reactions associated with the synthesis of bioconjugates Includes entirely new chapters on the latest areas in the field of bioconjugation as follows: Microparticles and nanoparticlesSilane coupling agentsDendrimers and dendronsChemoselective ligationQuantum dotsLanthanide chelatesCyanine dyesDiscrete PEG compoundsBuckyballs,fullerenes, and carbon nanotubesMass tags and isotope tagsBioconjugation in the study of protein interactions |
cleavable linkers in chemical biology: Antibody-Drug Conjugates Kenneth J. Olivier, Jr., Sara A. Hurvitz, 2016-11-14 Providing practical and proven solutions for antibody-drug conjugate (ADC) drug discovery success in oncology, this book helps readers improve the drug safety and therapeutic efficacy of ADCs to kill targeted tumor cells. • Discusses the basics, drug delivery strategies, pharmacology and toxicology, and regulatory approval strategies • Covers the conduct and design of oncology clinical trials and the use of ADCs for tumor imaging • Includes case studies of ADCs in oncology drug development • Features contributions from highly-regarded experts on the frontlines of ADC research and development |
cleavable linkers in chemical biology: New Frontiers in Chemical Biology Mark E. Bunnage, 2011 This book highlights the new frontiers in chemical biology and describes their impact and future potential in drug discovery. |
cleavable linkers in chemical biology: Cancer Drug Delivery Systems Based on the Tumor Microenvironment Yasuhiro Matsumura, David Tarin, 2020-01-07 This book proposes the importance of new systems of drug design and delivery based on cancer pathophysiology in addition to cancer molecular and cellular biology. The current studies based on molecular and cellular biology while ignoring pathophysiology and pharmacology may be leading the development of antitumor drugs in the wrong direction and wasting a lot of money. Although there have been numerous reports of genetic and phenotypic changes in tumors, a large body of pathological and clinical evidence supports the conclusion that there are no pivotal changes in tumor cells that distinguish them consistently and reliably from normal dividing cells. Unlike using antibiotics against bacterial infection, therefore, anticancer agents (ACAs) need to be delivered selectively to tumor tissues and should be kept there long enough to reproduce the concentrations they reach in the Petri dish, which is a closed space where the cytocidal effects of any anticancer agents (ACAs) including molecular targeting agents are very strong. In the body, however, administered ACAs are cleared with the passage of time. Furthermore, most human cancers possess abundant stroma that hinders the penetration of drugs into the tumor microenvironment. Therefore, to overcome these difficulties, novel drug delivery systems have been designed, such as nanoparticles and ACA conjugated antibodies to stromal components and to cancer cell surface antigens. These advances are described in this book after the first section, which describes core features of the pathophysiology of the cancer microenvironment, on which these new developments are based. |
cleavable linkers in chemical biology: Cytotoxic Payloads for Antibody–Drug Conjugates David E Thurston, Paul J M Jackson, 2019-07-11 Antibody–drug conjugates (ADCs) represent one of the most promising and exciting areas of anticancer drug discovery. Five ADCs are now approved in the US and EU [i.e., ado-trastuzumab emtansine (KadcylaTM), brentuximab vedotin (AdcetrisTM), inotuzumab ozogamicin (BesponsaTM), gemtuzumab ozogamicin (MylotargTM) and moxetumomab pasudotox-tdfk (Lumoxiti®)] and over 70 others are in various stages of clinical development, with impressive interim results being reported for many. The technology is based on the concept of delivering a cytotoxic payload selectively to cancer cells by attaching it to an antibody targeted to antigens on the cell surfaces. This approach has several advantages including the ability to select patients as likely responders based on the presence of antigen on the surface of their cancer cells and a wider therapeutic index, given that ADC targeting enables a more efficient delivery of cytotoxic agents to cancer cells than can be achieved by conventional chemotherapy, thus minimising systemic toxicity. Although there are many examples of antibodies that have been developed for this purpose, along with numerous linker technologies used to attach the cytotoxic agent to the antibody, there is presently a relatively small number of payload molecules in clinical use. The purpose of this book is to describe the variety of payloads used to date, along with a discussion of their advantages and disadvantages and to provide information on novel payloads at the research stage that may be used clinically in the future. |
cleavable linkers in chemical biology: Avidin-biotin Technology Meir Wilchek, Edward A. Bayer, 1990 The avidin-biotin complex has been used for isolation (affinity chromatography), localization (affinity cytochemistry, cell cytometry, and blotting technology), and diagnostics (immunoassay, histopathology, and gene probes). Recently, usage of the system has been extended to include other areas. This volume covers these new applications and methodologies including hybridoma technology, bioaffinity sensors, affinity targeting, and drug delivery, as well as cross-linking, immobilization, and fusogenic studies. |
cleavable linkers in chemical biology: Concepts and Case Studies in Chemical Biology Herbert Waldmann, Petra Janning, 2014-06-30 Retaining the proven didactic concept of the successful Chemical Biology - Learning through Case Studies, this sequel features 27 new case studies, reflecting the rapid growth in this interdisciplinary topic over the past few years. Edited by two of the world's leading researchers in the field, this textbook introduces students and researchers to the modern approaches in chemical biology, as well as important results, and the techniques and methods applied. Each chapter presents a different biological problem taken from everyday lab work, elucidated by an international team of renowned scientists. With its broad coverage, this is a valuable source of information for students, graduate students, and researchers working on the borderline between chemistry, biology, and biochemistry. |
cleavable linkers in chemical biology: Proteomics for Biological Discovery Timothy D. Veenstra, John R. Yates, III, 2006-06-12 Written by recognized experts in the study of proteins, Proteomics for Biological Discovery begins by discussing the emergence of proteomics from genome sequencing projects and a summary of potential answers to be gained from proteome-level research. The tools of proteomics, from conventional to novel techniques, are then dealt with in terms of underlying concepts, limitations and future directions. An invaluable source of information, this title also provides a thorough overview of the current developments in post-translational modification studies, structural proteomics, biochemical proteomics, microfabrication, applied proteomics, and bioinformatics relevant to proteomics. Presents a comprehensive and coherent review of the major issues faced in terms of technology development, bioinformatics, strategic approaches, and applications Chapters offer a rigorous overview with summary of limitations, emerging approaches, questions, and realistic future industry and basic science applications Discusses higher level integrative aspects, including technical challenges and applications for drug discovery Accessible to the novice while providing experienced investigators essential information Proteomics for Biological Discovery is an essential resource for students, postdoctoral fellows, and researchers across all fields of biomedical research, including biochemistry, protein chemistry, molecular genetics, cell/developmental biology, and bioinformatics. |
cleavable linkers in chemical biology: Molecular Biology in Medicinal Chemistry Theodor Dingermann, Dieter Steinhilber, Gerd Folkers, 2006-03-06 This readily comprehensible book explains the identification of molecular targets via cellular assays, reporter genes or transgenic models, as well as surveying recent advances in the synthesis, separation and analysis of drugs. A special section is devoted to molecular genetics methods. With its examination of these novel methods and generous practical advice, this is essential reading for all pharmaceutical chemists, molecular biologists and medical researchers using molecular methods to study drugs and their action. |
cleavable linkers in chemical biology: Carbohydrate Chemistry Amélia Pilar Rauter, Thisbe K Lindhorst, Yves Queneau, 2021-12-15 In many fields, most notably medicine and molecular biology, the understanding of the structure and function of carbohydrates and glycoconjugates remains vital. This new volume contains critical reviews covering the latest findings in both chemical and biological sciences, and demonstrates the interdisciplinary nature of modern carbohydrate research. This book addresses diverse applications that continue to be major challenges for carbohydrate chemists. The book starts with a review of Gérard Descotes contribution to the field as a pioneer of French modern carbohydrate chemistry. Green nanocatalytic oxidation of free sugars, photosensitive glycomacrocycles, the application of disaccharides in supramolecular chemistry, recent advances in the radiation chemistry of polysaccharides, and the cell wall pectic rhamnogalacturonan II, an enigma in plant glycobiology are just some of the diverse topics presented in Volume 45. This set of reports will certainly benefit any researcher who wishes to learn about the latest developments in the carbohydrate field. |
cleavable linkers in chemical biology: Mass Spectrometry-Based Chemical Proteomics W. Andy Tao, Ying Zhang, 2019-07-10 PROVIDES STRATEGIES AND CONCEPTS FOR UNDERSTANDING CHEMICAL PROTEOMICS, AND ANALYZING PROTEIN FUNCTIONS, MODIFICATIONS, AND INTERACTIONS—EMPHASIZING MASS SPECTROMETRY THROUGHOUT Covering mass spectrometry for chemical proteomics, this book helps readers understand analytical strategies behind protein functions, their modifications and interactions, and applications in drug discovery. It provides a basic overview and presents concepts in chemical proteomics through three angles: Strategies, Technical Advances, and Applications. Chapters cover those many technical advances and applications in drug discovery, from target identification to validation and potential treatments. The first section of Mass Spectrometry-Based Chemical Proteomics starts by reviewing basic methods and recent advances in mass spectrometry for proteomics, including shotgun proteomics, quantitative proteomics, and data analyses. The next section covers a variety of techniques and strategies coupling chemical probes to MS-based proteomics to provide functional insights into the proteome. In the last section, it focuses on using chemical strategies to study protein post-translational modifications and high-order structures. Summarizes chemical proteomics, up-to-date concepts, analysis, and target validation Covers fundamentals and strategies, including the profiling of enzyme activities and protein-drug interactions Explains technical advances in the field and describes on shotgun proteomics, quantitative proteomics, and corresponding methods of software and database usage for proteomics Includes a wide variety of applications in drug discovery, from kinase inhibitors and intracellular drug targets to the chemoproteomics analysis of natural products Addresses an important tool in small molecule drug discovery, appealing to both academia and the pharmaceutical industry Mass Spectrometry-Based Chemical Proteomics is an excellent source of information for readers in both academia and industry in a variety of fields, including pharmaceutical sciences, drug discovery, molecular biology, bioinformatics, and analytical sciences. |
cleavable linkers in chemical biology: Chemical Linkers in Antibody–Drug Conjugates (ADCs) Floris van Delft, John M Lambert, 2021-12-15 The covalent conjugation of potent cytotoxic agents to monoclonal antibodies, known as antibody-drug conjugates (ADCs) is a powerful approach in the field of targeted treatment of cancer. Clearly, both monoclonal antibody and cytotoxic payload are crucial elements in determining the clinical value of an ADC and have receive ample attention. However, the structural element connecting the two –the chemical linker– also plays an essential role in mode-of-action, efficacy, pharmacokinetics and safety profile of an ADC, but is often underappreciated in considerations of ADC design. Chemical Linkers in Antibody–Drug Conjugates aims to shine a detailed light on the various key attributes of chemical linkers in ADCs, for drug-to-antibody ratio, for stability, for release mechanism of payload, for pharmacokinetics, for stability determination, and for efficacy and safety. Ideal for postgraduate students and active researchers in drug discovery and development, this book provides a comprehensive description of linkers used in ADCs (clinical and late preclinical), insight into key quality attributes of linkers for ADCs, and aids the reader in understanding the role of linker chemistry and designing new ADCs. |
cleavable linkers in chemical biology: Antibody-Drug Conjugates L. Nathan Tumey, 2020 This volume looks at key methodologies that are commonly used across antibody drug conjugates (ADCs) programs. The chapters in this book cover topics such as conjugations to endogenous cysteine residues; click chemistry conjugations; antibody conjugations via glycosyl remodeling; analysis of ADCs by native mass spectrometry; characterization of ADCs by capillary electrophoresis; LC/MS methods for studying lysosomal ADC catabolism; and determination of ADC concentration by ligand-binding assays. 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 practical, Antibody-Drug Conjugates: Methods and Protocols is a valuable resource that aims to lower the activation barrier when undertaking a new discipline, and provides a toolbox for the next generation of ADC scientists. |
cleavable linkers in chemical biology: Therapeutic Oligonucleotides Jens Kurreck, 2008 This book provides a compelling overall update on current status of RNA interference |
cleavable linkers in chemical biology: Innovations for Next-Generation Antibody-Drug Conjugates Marc Damelin, 2018-05-29 Antibody-drug conjugates (ADCs) stand at the verge of a transformation. Scores of clinical programs have yielded only a few regulatory approvals, but a wave of technological innovation now empowers us to overcome past technical challenges. This volume focuses on the next generation of ADCs and the innovations that will enable them. The book inspires the future by integrating the field’s history with novel strategies and cutting-edge technologies. While the book primarily addresses ADCs for solid tumors, the last chapter explores the emerging interest in using ADCs to treat other diseases. The therapeutic rationale of ADCs is strong: to direct small molecules to the desired site of action (and away from normal tissues) by conjugation to antibodies or other targeting moieties. However, the combination of small and large molecules imposes deep complexity to lead optimization, pharmacokinetics, toxicology, analytics and manufacturing. The field has made significant advances in all of these areas by improving target selection, ADC design, manufacturing methods and clinical strategies. These innovations will inspire and educate scientists who are designing next-generation ADCs with the potential to transform the lives of patients. |
cleavable linkers in chemical biology: Introduction to Bioorganic Chemistry and Chemical Biology David Van Vranken, Gregory A. Weiss, 2018-10-08 Introduction to Bioorganic Chemistry and Chemical Biology is the first textbook to blend modern tools of organic chemistry with concepts of biology, physiology, and medicine. With a focus on human cell biology and a problems-driven approach, the text explains the combinatorial architecture of biooligomers (genes, DNA, RNA, proteins, glycans, lipids, and terpenes) as the molecular engine for life. Accentuated by rich illustrations and mechanistic arrow pushing, organic chemistry is used to illuminate the central dogma of molecular biology. Introduction to Bioorganic Chemistry and Chemical Biology is appropriate for advanced undergraduate and graduate students in chemistry and molecular biology, as well as those going into medicine and pharmaceutical science. Please note that Garland Science flashcards are no longer available for this text. However, the solutions can be obtained through our Support Material Hub link below, but should only be requested by instructors who have adopted the book on their course. |
cleavable linkers in chemical biology: Chemoselective and Bioorthogonal Ligation Reactions W. Russ Algar, Philip Dawson, Igor L. Medintz, 2017-03-17 This timely, one-stop reference is the first on an emerging and interdisciplinary topic. Covering both established and recently developed ligation chemistries, the book is divided into two didactic parts: a section that focuses on the details of bioorthogonal and chemoselective ligation reactions at the level of fundamental organic chemistry, and a section that focuses on applications, particularly in the areas of chemical biology, biomaterials, and bioanalysis, highlighting the capabilities and benefits of the ligation reactions. With chapters authored by outstanding scientists who range from trailblazers in the field to young and emerging leaders, this book on a highly interdisciplinary topic will be of great interest for biochemists, biologists, materials scientists, pharmaceutical chemists, organic chemists, and many others. |
cleavable linkers in chemical biology: Antibody-Drug Conjugates and Immunotoxins Gail Lewis Phillips, 2012-12-13 This volume gathers the leading research on antibody-drug conjugates and immunotoxins. Following a rigorous overview, the volume delves into focused sections on all aspects of ADCs and ITs from clinical development through to targeted therapeutic applications and the latest technologies. |
cleavable linkers in chemical biology: Oligonucleotide-Based Drugs and Therapeutics Nicolay Ferrari, Rosanne Seguin, 2018-07-31 A comprehensive review of contemporary antisense oligonucleotides drugs and therapeutic principles, methods, applications, and research Oligonucleotide-based drugs, in particular antisense oligonucleotides, are part of a growing number of pharmaceutical and biotech programs progressing to treat a wide range of indications including cancer, cardiovascular, neurodegenerative, neuromuscular, and respiratory diseases, as well as other severe and rare diseases. Reviewing fundamentals and offering guidelines for drug discovery and development, this book is a practical guide covering all key aspects of this increasingly popular area of pharmacology and biotech and pharma research, from the basic science behind antisense oligonucleotides chemistry, toxicology, manufacturing, to safety assessments, the design of therapeutic protocols, to clinical experience. Antisense oligonucleotides are single strands of DNA or RNA that are complementary to a chosen sequence. While the idea of antisense oligonucleotides to target single genes dates back to the 1970's, most advances have taken place in recent years. The increasing number of antisense oligonucleotide programs in clinical development is a testament to the progress and understanding of pharmacologic, pharmacokinetic, and toxicologic properties as well as improvement in the delivery of oligonucleotides. This valuable book reviews the fundamentals of oligonucleotides, with a focus on antisense oligonucleotide drugs, and reports on the latest research underway worldwide. • Helps readers understand antisense molecules and their targets, biochemistry, and toxicity mechanisms, roles in disease, and applications for safety and therapeutics • Examines the principles, practices, and tools for scientists in both pre-clinical and clinical settings and how to apply them to antisense oligonucleotides • Provides guidelines for scientists in drug design and discovery to help improve efficiency, assessment, and the success of drug candidates • Includes interdisciplinary perspectives, from academia, industry, regulatory and from the fields of pharmacology, toxicology, biology, and medicinal chemistry Oligonucleotide-Based Drugs and Therapeutics belongs on the reference shelves of chemists, pharmaceutical scientists, chemical biologists, toxicologists and other scientists working in the pharmaceutical and biotechnology industries. It will also be a valuable resource for regulatory specialists and safety assessment professionals and an important reference for academic researchers and post-graduates interested in therapeutics, antisense therapy, and oligonucleotides. |
cleavable linkers in chemical biology: Chemical Ligation Luca D. D'Andrea, Alessandra Romanelli, 2017-04-03 Presenting a wide array of information on chemical ligation – one of the more powerful tools for protein and peptide synthesis – this book helps readers understand key methodologies and applications that protein therapeutic synthesis, drug discovery, and molecular imaging. • Moves from fundamental to applied aspects, so that novice readers can follow the entire book and apply these reactions in the lab • Presents a wide array of information on chemical ligation reactions, otherwise scattered across the literature, into one source • Features comprehensive and multidisciplinary coverage that goes from basics to advanced topics • Helps researchers choose the right chemical ligation technique for their needs |
cleavable linkers in chemical biology: Caged Compounds Gerard Marriott, 1998-06-22 The critically acclaimed laboratory standard for more than forty years, Methods in Enzymology is one of the most highly respected publications in the field of biochemistry. Since 1955, each volume has been eagerly awaited, frequently consulted, and praised by researchers and reviewers alike. More than 285 volumes have been published (all of them still in print) and much of the material is relevant even today--truly an essential publication for researchers in all fields of life sciences. |
cleavable linkers in chemical biology: Contemporary Chemical Approaches for Green and Sustainable Drugs Marianna Torok, 2022-08-26 Contemporary Chemical Approaches for Green and Sustainable Drugs provides readers with the knowledge they need to integrate sustainable approaches into their work. Sections cover different aspects of green and sustainable drug development from design to disposal, including computer-aided drug design, green resourcing of drugs and drug candidates, an overview of the health concerns of pharmaceutical pollution, and a survey of potential chemical methods for its reduction. Drawing together the knowledge of a global team of experts, this book provides an inclusive overview of the chemical tools and approaches available for minimizing the negative environmental impact of current and newly developed drugs. This will be a useful guide for all academic and industrial researchers across green and sustainable chemistry, medicinal chemistry, environmental chemistry and pharmaceutical science. - Provides an integrative overview of the environmental risks of drugs and drug by products to support chemists in pre-emptively addressing these issues - Highlights the advantages of computer-aided drug design, green and sustainable sourcing, and novel methods for the production of safer, more effective drugs - Presents individual chapters written by renowned experts with diverse backgrounds - Reflects research in practice through selected case studies and extensive state-of-the-art reference sections to serve as a starting point in the design of any specialized environmentally-conscious medicinal chemistry project |
cleavable linkers in chemical biology: Advanced Chemical Biology Howard C. Hang, Matthew R. Pratt, Jennifer A. Prescher, 2023-04-03 Advanced Chemical Biology The modern approach to teaching chemical biology Advanced Chemical Biology is organized around the central dogma of life, progressing from genes to proteins and higher-order cellular structures, including core application areas such as imaging, chemical genetics, activity-based protein profiling, and natural product discovery and biosynthesis. Advanced topics and applications in, e. g., microbiology, developmental biology, and neurobiology, are covered in separate sections. Every chapter is homogeneous in style and layout, consisting of a short historical introduction followed by a description of the underlying concepts and a selection of recent examples of how the concept has been turned into practice. The subdivision of the contents into core and supplemental chapters enables a flexible use in teaching, both for a one-semester and a two-semester course. Written by authors and editors coming from the leading scientific institutions that have developed the concepts and technologies for this discipline, Advanced Chemical Biology includes specific information on topics like: DNA function, synthesis and engineering, chemical approaches to genome integrity, and RNA function, synthesis, and probing Chemical approaches to transcription and RNA regulation in vivo, chemical biology of genome engineering, and peptide/protein synthesis and engineering Directed evolution for chemical biology, chemical biology of cellular metabolism, chemical biology of lipids, and protein post-translational modifications Chemical glycobiology, chemical and enzymatic modification of proteins, genetic code expansion, bio-orthogonal chemistry, and cellular imaging With its broad scope and focus on turning concepts into applications, Advanced Chemical Biology is an excellent starting point for anyone entering the field and looking for a guide to the wide range of available methods and strategies that chemical biology has to offer. With a Foreword by Nobel Laureate Carolyn Bertozzi. |
cleavable linkers in chemical biology: Integrative Structural Biology with Hybrid Methods Haruki Nakamura, Gerard Kleywegt, Stephen K. Burley, John L. Markley, 2019-01-08 This book presents a new emerging concept of Integrative Structural Biology. It covers current trends of the molecular and cellular structural biology, providing new methods to observe, validate, and keep the structural models of the large cellular machines with recent scientific results. Structures of very large macromolecular machines in cells are being determined by combining observations from complementary experimental methods. Thus, this volume presents the each methods such as X-ray crystallography, NMR spectroscopy, 3DEM, small-angle scattering (SAS), FRET, crosslinking, and enables the readers to understand the hybrid methods. This book discusses how those integrative models should be represented, validated and archived. A unique highlight of this book is discussion of the data validation and archive, which are big problems in this filed along with the progress of this field. The researchers in biology will be interested in this book as a guide book for learning the current structure biology, but also those in structure biology may use this book as a comprehensive reference to cover broad topics. |
cleavable linkers in chemical biology: Single Molecule Spectroscopy R. Rigler, M. Orrit, T. Basche, 2012-12-06 The topics range from single molecule experiments in quantum optics and solid-state physics to analogous investigations in physical chemistry and biophysics. |
cleavable linkers in chemical biology: Subcellular Proteomics Eric Bertrand, Michel Faupel, 2007-08-29 This volume summarizes the new developments that made subcellular proteomics a rapidly expanding area. It examines the different levels of subcellular organization and their specific methodologies. In addition, the book includes coverage of systems biology that deals with the integration of the data derived from these different levels to produce a synthetic description of the cell as a system. |
cleavable linkers in chemical biology: Next Generation Antibody Drug Conjugates (ADCs) and Immunotoxins Ulf Grawunder, Stefan Barth, 2017-04-07 This book describes the newest developments in antibody drug conjugates and immunotoxins, paving their way to clinical application. Lessons learned from the current state of the art are used to further improve our understanding of their mechanisms of action and off target activities. The book introduces scientists to all of the prerequisites that must be properly addressed, including identification of the right target, specific traits of target binding antibodies, proper selection of the toxic payload, internalization induced by binding, and next generation conjugation and linker technologies. These knowledge-based, revolutionary new drug principles will form the cornerstone of the future standard of care and will lead to major advances in application, as well as improved quality of life and patient survival rates. This book will be of interest to biotech companies and researchers working in the fields of immunology, pharmacology, and oncology. |
cleavable linkers in chemical biology: Essentials of Chemical Biology Andrew D. Miller, Julian A. Tanner, 2013-05-03 This excellent work fills the need for an upper-level graduate course resource that examines the latest biochemical, biophysical, and molecular biological methods for analyzing the structures and physical properties of biomolecules... This reviewer showed [the book] to several of his senior graduate students, and they unanimously gave the book rave reviews. Summing Up: Highly recommended... CHOICE Chemical biology is a rapidly developing branch of chemistry, which sets out to understand the way biology works at the molecular level. Fundamental to chemical biology is a detailed understanding of the syntheses, structures and behaviours of biological macromolecules and macromolecular lipid assemblies that together represent the primary constituents of all cells and all organisms. The subject area of chemical biology bridges many different disciplines and is fast becoming an integral part of academic and commercial research. This textbook is designed specifically as a key teaching resource for chemical biology that is intended to build on foundations lain down by introductory physical and organic chemistry courses. This book is an invaluable text for advanced undergraduates taking biological, bioorganic, organic and structural chemistry courses. It is also of interest to biochemists and molecular biologists, as well as professionals within the medical and pharmaceutical industry. Key Features: A comprehensive introduction to this dynamic area of chemistry, which will equip chemists for the task of understanding and studying the underlying principles behind the functioning of biological macro molecules, macromolecular lipid assemblies and cells. Covers many basic concepts and ideas associated with the study of the interface between chemistry and biology. Includes pedagogical features such as: key examples, glossary of equations, further reading and links to websites. Clearly written and richly illustrated in full colour. |
cleavable linkers in chemical biology: Peptide-Lipid Interactions Sidney A. Simon, Thomas J. McIntosh, 2002-11-13 This volume contains a comprehensive overview of peptide-lipid interactions by leading researchers. The first part covers theoretical concepts, experimental considerations, and thermodynamics. The second part presents new results obtained through site-directed EPR, electron microscopy, NMR, isothermal calorimetry, and fluorescence quenching. The final part covers problems of biological interest, including signal transduction, membrane transport, fusion, and adhesion. Key Features * world-renowned experts * state-of-the-art experimental methods * monolayers, bilayers, biological membranes * theoretical aspects and computer simulations * rafts * synaptic transmission * membrane fusion * signal transduction |
cleavable linkers in chemical biology: A Handbook for DNA-Encoded Chemistry Robert A. Goodnow, Jr., 2014-04-28 This book comprehensively describes the development and practice of DNA-encoded library synthesis technology. Together, the chapters detail an approach to drug discovery that offers an attractive addition to the portfolio of existing hit generation technologies such as high-throughput screening, structure-based drug discovery and fragment-based screening. The book: Provides a valuable guide for understanding and applying DNA-encoded combinatorial chemistry Helps chemists generate and screen novel chemical libraries of large size and quality Bridges interdisciplinary areas of DNA-encoded combinatorial chemistry – synthetic and analytical chemistry, molecular biology, informatics, and biochemistry Shows medicinal and pharmaceutical chemists how to efficiently broaden available chemical space for drug discovery Provides expert and up-to-date summary of reported literature for DNA-encoded and DNA-directed chemistry technology and methods |
cleavable linkers in chemical biology: Molecular Biology and Biotechnology Robert Allen Meyers, 1995-06-29 This is one volume 'library' of information on molecular biology, molecular medicine, and the theory and techniques for understanding, modifying, manipulating, expressing, and synthesizing biological molecules, conformations, and aggregates. The purpose is to assist the expanding number of scientists entering molecular biology research and biotechnology applications from diverse backgrounds, including biology and medicine, as well as physics, chemistry, mathematics, and engineering. |
cleavable linkers in chemical biology: Optical Probes in Biology Jin Zhang, Sohum Mehta, Carsten Schultz, 2016-04-19 Optical probes, particularly the fluorescent varieties, enable researchers to observe cellular events in real time and with great spatial resolution. Optical Probes in Biology explores the diverse capabilities of these powerful and versatile tools and presents various approaches used to design, develop, and implement them. The book examines the use |
cleavable linkers in chemical biology: Combinatorial Strategies in Biology and Chemistry Annette Beck-Sickinger, Peter Weber, 2002-01-21 Dieses Buch führt die Molekularbiologie und die kombinatorische Chemie in absolut praxistauglicher Weise zusammen. Spezialisten aus der Chemie oder der Biologie wird der Einstieg in die Kombinatorik leicht gemacht! Eine große Vielfalt von Themen und Verfahren vermittelt schnell und effektiv einen Überblick über ein spannendes und aufstrebendes Gebiet. |
cleavable linkers in chemical biology: Advanced and Modern Approaches for Drug Delivery Amit Kumar Nayak, Md Saquib Hasnain, Bibek Laha, Sabyasachi Maiti, 2023-07-29 Advanced and Modern Approaches for Drug Delivery explores novel approaches currently used for drug delivery, including the must up-to-date techniques and technology. The approaches discussed allow pharmaceutical scientists to design effective drug delivery systems or devices for the management and treatment of numerous diseases and conditions. Detailed information on a wide variety of subjects, including dendrimers, lipid nanostructures, solid lipid nanoparticles, stimuli-responsive smart systems, self-assembled protein-drug nanoparticles, nanoconjugate formulations, nanofibers, iontophoretic systems, microneedle systems, ultra-sound triggered systems, targeted carrier-based intracellular delivery systems, resealed erythrocyte-based systems, 3 D-printing tool, site-specific monoclonal antibodies, and bio-inspired systems are all comprehensively discussed. With contributions from those in academia and industry, this book is an excellent reference for all those needing to understand drug delivery systems. - Provides thorough insights into the most up-to-date approaches and technologies for drug delivery and therapeutics - Discusses possible future approaches - Includes perspectives from industry and academia |
cleavable linkers in chemical biology: Chemistry of Peptide Synthesis N. Leo Benoiton, 2016-04-19 Chemistry of Peptide Synthesis is a complete overview of how peptides are synthesized and what techniques are likely to generate the most desirable reactions. Incorporating elements from the author's role of Career Investigator of the Medical Research Council of Canada and his extensive teaching career, the book emphasizes learning rather th |
cleavable linkers in chemical biology: Chemistry and Biology of O-GlcNAcylation Wen Yi, |
A Simple and Effective Cleavable Linker for Chemical …
Ideally, a cleavable linker is stable under a wide variety of conditions, is efficiently and selectively cleaved, and can be synthesized in a low number of easy chemical transforma-tions. We …
Cleavable Linker: A Promising Strategy for Maintaining
f bioconjugate linkers with a built-in cleavage chemical trigger that can magnetic beads linked with different bioconjugate function groups thr ugh a cleavable disulfide linker. The beads can …
Severing Ties: Quantifying the Payload Release from …
For example, some cleavable linkers leverage the low pH in lysosomes to cause cleav-age, such as acid-labile hydrazone linkers. Other linker types rely on a reducing environment for …
Cleavable linkers in antibody–drug conjugates
There are three main types of chemically cleavable linkers: acid cleavable, reducible disulfides and those cleavable by exogenous stimuli. The first two are clinically established methods, …
A Mild Chemically Cleavable Linker System for Functional …
The incorporation of a cleavable linker between the biotin tag and the site of attachment to the target protease provides a significant advance as it allows specific elution of probe-labeled …
Cleavable linkers and their application in MS-based target …
Continuous development in chemistry has led to a wide variety of different types of cleavable linkers (chemically cleavable, photocleavable, enzymatically cleavable and MS-cleavable), of …
Cleavable Linkers In Chemical Biology (book)
Concepts and Case Studies in Chemical Biology Herbert Waldmann,Petra Janning,2014-10-06 Retaining the proven didactic concept of the successful Chemical Biology Learning through …
Design of cleavable linkers and applications in chemical …
Another promising tool to solve this problem is cleavable linker. To develop a simple and efficient cleavable linker for activity based probes, a cleavable building block derived from tartaric acid …
A Novel Family of Acid-Cleavable Linker Based on Cyclic …
Cleavable linkers have become the subject of intense study in the field of chemical biology, particularly because of their applications in the construction of antibody-drug conjugates …
Cleavable linkers in antibody drug conjugates
β-Glucuronidase-cleavable linkers β-Glucuronidases are hydrolytic lysosomal enzymes in the glycosidase class that catalyse the breakdown of β-glucuronic acid residues in polysaccharides
Useful Tools for Biomolecule Isolation, Detection, and …
For instance, photolytic-based cleavable linkers typically undergo efficient release, but upon cleavage, they release reactive carbonyl compounds (aldehydes, ketones) that can react with …
Engineering Enzyme-Cleavable Oligonucleotides by …
Both these cleavable dipeptide linkers can be efficiently incorpo-rated into oligonucleotides via automated DNA synthesis to produce constructs with well-defined molecular structures and …
Evaluation and Optimization of Chemically-Cleavable Linkers …
Herein, we report our efforts to conduct a parallel assessment of two widely-used chemically-cleavable linkers equipped with dialkoxydiphenylsilane (DADPS linker) and azobenzene (AZO …
Enzyme-Cleavable Linkers for Protein Chemical Synthesis …
A wide range of SPCL linkers have been developed but their cleavage requires chemical conditions sometimes incompatible with sensitive protein targets. Here, we describe the …
Cleavable Linkers In Chemical Biology (book)
Cleavable Linkers In Chemical Biology: Linkers in Biomacromolecules ,2021-01-20 Linkers in Biomacromolecules Volume 647 in the Methods in Enzymology series continues the legacy of …
A solid-phase compatible silane-based - ChemRxiv
Here we report the silane-based Cleavable Linkers for Isotopically-labeled Proteomics (sCLIP) method. sCLIP streamlines sample preparation with unparalleled early-stage isobaric labeling …
A thermally-cleavable linker for solid-phase synthesis
Abstract—Oxabicyclo[2.2.1]norbornenes constitute a convenient and readily cleaved linker for solid-phase organic synthesis. A sim-ple and inexpensive furfuryl-substituted resin has been …
Reeling in the Catch: Advancing Cleavable Linkers for …
Chemistry and Biology, Yang and coworkers (2010) present a detailed study of a diazobenzene system that is shown to be highly effective for cleavage in sophis-ticated proteomics …
An N terminomics toolbox combining 2 …
Here, we introduce an N terminomics toolbox that combines selective N-termi-nal biotinylation using 2-pyridinecarboxaldehyde (2PCA) reagents with chemically cleavable linkers to enable …
Optimizing Solid-Phase Protein Synthesis: A Systematic …
cleavable linkers to optimize SPCL. By combining the low loading-controlled pore glass (CPG- developed an optimized s enabled the successful assembly of five peptide fragments through …
A Simple and Effective Cleavable Linker for Chemical Proteomic…
Ideally, a cleavable linker is stable under a wide variety of conditions, is efficiently and selectively cleaved, and can be synthesized in a low number of easy chemical transforma …
Cleavable Linker: A Promising Strategy for Maintaining
f bioconjugate linkers with a built-in cleavage chemical trigger that can magnetic beads linked with different bioconjugate function groups thr ugh a cleavable disulfide linker. …
Severing Ties: Quantifying the Payload Release from Antibody …
For example, some cleavable linkers leverage the low pH in lysosomes to cause cleav-age, such as acid-labile hydrazone linkers. Other linker types rely on a reducing …
Cleavable linkers in antibody–drug conjugates
There are three main types of chemically cleavable linkers: acid cleavable, reducible disulfides and those cleavable by exogenous stimuli. The first two are clinically …
A Mild Chemically Cleavable Linker System for Functional Pr…
The incorporation of a cleavable linker between the biotin tag and the site of attachment to the target protease provides a significant advance as it allows specific …