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Medicinal chemistry is both science and art. The science of medicinal chemistry offers mankind one of its best hopes for improving the quality of life. The art of medicinal chemistry continues to challenge its practitioners with the need for both intuition and experience to discover new drugs. Hence sharing the experience of drug research is uniquely beneficial to the field of medicinal chemistry. Drug research requires interdisciplinary team-work at the interface between chemistry, biology and medicine. Therefore, the topic-related series Topics in Medicinal Chemistry covers all relevant aspects of drug research, e.g. pathobiochemistry of diseases, identification and validation of (emerging) drug targets, structural biology, drugability of targets, drug design approaches, chemogenomics, synthetic chemistry including combinatorial methods, bioorganic chemistry, natural compounds, high-throughput screening, pharmacological in vitro and in vivo investigations, drug-receptor interactions on the molecular level, structure-activity relationships, drug absorption, distribution, metabolism, elimination, toxicology and pharmacogenomics. In general, special volumes are edited by well known guest editors.
Carbohydrates in Drug Discovery and Development: Synthesis and Applications examines recent and notable developments in the synthesis, biology, therapeutic, and biomedical applications of carbohydrates, which is considered to be a highly promising area of research in the field of medicinal chemistry. Their role in several important biological processes, notably energy storage, transport, modulation of protein function, intercellular adhesion, malignant transformation, signal transduction, viral, and bacterial cell surface recognition formulate the carbohydrate systems to be an exceedingly considerable scaffold for the development of new chemical entities of pharmacological importance. In addition to their easy accessibility, high functionality and chiralpool characteristics are the few additional fascinating structural features of carbohydrates, which further enhance their utilities and thus they have been able to attract chemists and biologists toward harnessing these properties for the past several decades.This book covers an advanced aspect of carbohydrate-based molecular scaffolding, starting with a general introduction followed by a detailed discussion about the impact of diverse carbohydrate-containing molecules of great therapeutic values and their impact on drug discovery and development. The topics covered in this book include the significance of heparin mimetics as the possible tools for the modulation of biology and therapy, chemistry and bioactivities of C-glycosylated compounds, inositols, iminosugars, KDO, sialic acids, glycohybrids, macrocycles, plant oligosaccharides, anti-bacterial and anti-cancer vaccines, antibiotics, and more.
Die Suche nach Medikamenten mit neuen oder verbesserten Eigenschaften hat das Interesse am pharmazeutischen Potenzial von Kohlenhydraten enorm verstärkt. Dies gilt insbesondere für die Entwicklung von Antibiotika, Impfstoffen und Anti-Krebs-Mitteln. Carbohydrate-based Drug Discovery stellt mit mehr als 50 Beiträgen der weltweit führenden Experten die neuesten Entwicklungen in der Kohlenhydrat- und Biochemie vor. Dabei liegt der Schwerpunkt der Darstellung auf der pharmazeutischen Anwendung. In jüngster Zeit sind wirksame, auf Kohlenhydraten basierende Medikamente gegen HIV, Grippe, Epilepsie, Diabetes und Krebs auf den Markt gekommen bzw. werden in Studien klinisch erprobt. Doch das gesamte Potenzial dieser Substanzklasse kann man bislang wohl nur erahnen. Die pharmazeutische Industrie investiert bereits große Summen in die Forschung und Entwicklung. So kommt dieses Handbuch genau zur richtigen Zeit. Umfassend und kompetent behandelt es den gesamten Bereich der Kohlenhydratchemie. Es führt ein in die chemische Synthese, in Biosynthese und Metabolismus und informiert über die Analyse und die zellulären Funktionen von Kohlenhydraten. Einen weiteren Schwerpunkt bildet die Entwicklung von Medikamenten auf Kohlenhydrat-Basis, wie z.B. synthetischer Impfstoffe oder Thrombosemittel auf Basis synthetischer Oligosaccharide. Erschlossen wird das mit einem umfangreichen bibliographischen Anhang versehene Werk durch einen thematischen Index. Sein Herausgeber, Chi-Huey Wong, hat bereits mehrere internationale Preise für sein wissenschaftliches Werk erhalten, darunter den "Presidential Award" und den "Presidential Young Investigator Award".
Carbohydrate-Based Therapeutics Comprehensive resource summarizing opportunities and latest progress in design methodologies for carbohydrate-based therapeutics through a disease-oriented approach Carbohydrate-Based Therapeutics covers current progress and explores new frontiers in carbohydrate-based therapeutic applications, utilizing a unique approach by providing a detailed background of diseases coupled with subsequent carbohydrate-based therapies. The link between chemistry and design of novel carbohydrate-based medicines is highlighted and a broad overview of all the potential applications of carbohydrates is given. Emphasis is laid on concepts used for carbohydrate drug design, structure– activity relationship, and impact on health and diseases. The text also discusses newer topics like nanoparticles, material science, and tissue generation. Carbohydrate-Based Therapeutics includes information on: Antimicrobial carbohydrate-based therapies, covering antibacterial and antiviral vaccines, antifungal therapies, anti-influenza therapeutics, and antiadhesive carbohydrates and glycomimetics Anti-cancer carbohydrate-based therapies, covering cancer vaccines and immunotherapy, and carbohydrate tools in cancer biology Carbohydrate-based therapies in metabolic, neuronal, and immune disorders, covering carbohydrate-based therapeutics for lysosomal disorders and neurodegenerative diseases New frontiers in carbohydrate-based therapies, covering carbohydrates for tissue engineering, antiangiogenic and regenerative medicine Providing comprehensive coverage of foundational knowledge on the subject in a unique and highly accessible format while also exploring the state of the art in the field’s applications, Carbohydrate-Based Therapeutics is an essential resource for medicinal, pharmaceutical, and organic chemists, chemists in industry, biochemists, and biotechnologists.
In recent years there has been increasing evidence of the importance of carbohydrates and glycoconjugates in biomedical applications, and the use of synthetic ligands based on carbohydrates as drugs has received much attention. Focussing on drug discovery from key targets and placing an emphasis on the multi-disciplinary approaches necessary to challenge these issues, this book comprehensively covers the new and recent discoveries in the area of carbohydrate drug discovery. Carbohydrates in Drug Design and Discovery is split into five sections, beginning with a introduction and perspective on the current market. The book then goes on to discuss new synthetic methods in glycobiology, the use of glycobiology in chemical biology and glycobiology in drug discovery. Providing a worldwide perspective on this broad area, and providing examples of therapeutics already developed using these methods, this book provides a comprehensive introduction, discussion and update on this fast developing field for medicinal chemists and biochemists working in industry and academia.
The finding by Emil Fischer that glucose and fructose on treatment with phenylhydrazine gave the identical osazone led him to the elucidation of stereochemistry of carbohydrates. Since then, progress in the field of carbohydrates has been amazing with the unraveling their basic structure, biosynthesis, immunology, functions, and clinical uses, for pure carbohydrates and for protein-linked carbohydrates (glycoproteins and proteoglycans). The chapters in Carbohydrate Chemistry, Biology and Medical Applications present a logical sequence leading from the chemistry and biochemistry of carbohydrates, followed by their role in various pathological conditions, to carbohydrates as potential therapeutic and diagnostic agents. This book offers a detailed panoramic review of the chemistry and biology of carbohydrates for chemists, biologists and health professionals. Each chapter is authored by contributors expert in the particular area of research. - Explains how carbohydrates are important to life - Details the chemistry, biology and medical aspects of carbohydrates - Interdisciplinary and international team of authors
This book contains original papers and reviews on carbohydrate research in medicine, authored by participants of the 29th International Carbohydrate Symposium, where this topic had a special emphasis. The focus on biological events involving carbohydrates and glycoconjugates has delivered reliable approaches for disease treatment and diagnosis. Research on carbohydrate-based compounds for therapeutic applications is illustrated in various contributions, namely those covering the development of novel agents against Alzheimer’s disease, e.g. the neuroprotective C-glucosylated flavones and the isonucleoside-based cholinesterase inhibitors. New imino sugar glucosidase inhibitors are also disclosed, a class of compounds with potential for diabetes, Gaucher disease or cancer treatment. Also the development of a useful synthetic method towards multivalent glycoclusters of biomedical interest is here highlighted. The relevance of glycomimetics in drug discovery and the progress on carbohydrates in early diagnosis and cancer treatment are reviewed. Noteworthy is the chitosan-based delivery system for drug oral administration, a new biomaterial-based approach to improve bioavailability. Another study on the conformation of Streptococcus capsular polysaccharide backbones by molecular modelling provides useful information for bacterial immunotherapeutic approaches. All original contributions and reviews clearly demonstrate the potential of glycosciences for innovation in medicinal (glyco)chemistry and pharmaceutical research.
This book is the first of its kind entirely dedicated to carbohydrate vaccines written by renowned scientists with expertise in carbohydrate chemistry and immunochemistry. It covers the synthesis of carbohydrate antigens related to bacteria and parasites such as: Heamophilus influenza, Streptococcus pnemoniae, Shigella flexneri, Candida albicans, Mycobacterium tuberculosis, and Chlamydia. The first three chapters are of wide interest as they cover fundamental concerns in new vaccine developments. The first one presents the immune system and how carbohydrate antigens are processed before protective antibodies are produced. It also illustrates antigen presentation in the context of major histocompatibility complexes (MHCs). The second chapter describes regulatory issues when carbohydrate vaccines are involved while the third one discuss several techniques used in conjugation chemistry and the implication of certain chemical linkages that may induce unexpected anti-linker antibodies. This section will be particularly appealing for those involved in drug-conjugate design, pro-drug developments, and drug vectorization. The book concludes with one chapter that illustrates the principle through which peptide antigens can functionally mimic carbohydrate epitopes, thus, unraveling the potential for peptide surrogates as replacement for complex carbohydrate structures. This book is unique in that it covers all aspects related to carbohydrate vaccines including the success story with the first semi-synthetic bacterial polysaccharide vaccine against Heamophilus influenza type b responsible for pneumonia and meningitis, liable for more than 600,000 infant deaths worldwide in developing countries. The book also presents regulatory issues and will thus be vital for government agencies approving candidate vaccines. It widely covers synthetic methodologies for the attachment of carbohydrate antigens to peptides and immunogenic protein carriers. Vaccines against bacterial antigens, cancer, and parasites are also discussed by worldwide experts in this field in details. No other book contains such a wide panel of different expertise. It will also be useful to students and researchers involved with the immunology of forreings antigens and how the under appreciated carbohydrate antigens are processed by the immune system.
Sugar chains (glycans) are often attached to proteins and lipids and have multiple roles in the organization and function of all organisms. "Essentials of Glycobiology" describes their biogenesis and function and offers a useful gateway to the understanding of glycans.
A new focus on glycoscience, a field that explores the structures and functions of sugars, promises great advances in areas as diverse as medicine, energy generation, and materials science, this report finds. Glycans-also known as carbohydrates, saccharides, or simply as sugars-play central roles in many biological processes and have properties useful in an array of applications. However, glycans have received little attention from the research community due to a lack of tools to probe their often complex structures and properties. Transforming Glycoscience: A Roadmap for the Future presents a roadmap for transforming glycoscience from a field dominated by specialists to a widely studied and integrated discipline, which could lead to a more complete understanding of glycans and help solve key challenges in diverse fields.