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Iminosugars form undoubtedly the most attractive of carbohydrate mimics reported so far. In these structures, the substitution of the endocyclic oxygen of sugars by a basic nitrogen atom leads to remarkable biological properties and raises many challenges in organic synthesis. Since the discovery of their biological activity as glycosidase inhibitors in the 1970’s, these polyvalent molecules have progressively made their way from the laboratory to the clinic. The impressive series of discoveries in the field over the past ten years indicates clearly that it is “a boom time” for iminosugar chemistry and biology. The scope of their profile as inhibitors has been extended to a number of enzymes such as phosphorylases, glycosyltransferases or metalloproteinases, and iminosugars now constitute lead compounds for the development of new therapeutic agents for a wide range of diseases including diabetes, viral infections, lysosomal storage disorders and tumor metastasis. Latest developments, from iminosugar synthesis to their use in clinical studies, are presented in this book, which contains contributions from over fifteen of the major chemists, biochemists and drug developers in this rapidly expanding field. An extensive table correlating the structures of more than 600 iminosugars of therapeutic interest with their biological activities is also included in the book and should prove particularly useful to aid with the design and the discovery of novel bioactive substances. Iminosugars: From Synthesis to Therapeutic Application provides a unique resource for academic and industrial researchers working in the field of iminosugars and glycomimetics of biological and/or therapeutic interest: organic chemists, medicinal chemists, carbohydrate chemists and medical scientists.
Carbohydrate Chemistry demonstrates the interdisciplinary nature of modern carbohydrate research, and benefits any researcher who wishes to learn about the latest developments in the carbohydrate field.
Protein Homeostasis Diseases: Mechanisms and Novel Therapies offers an interdisciplinary examination of the fundamental aspects, biochemistry and molecular biology of protein homeostasis disease, including the use of natural and pharmacological small molecules to treat common and rare protein homeostasis disorders. Contributions from international experts discuss the biochemical and genetic components of protein homeostasis disorders, the mechanisms by which genetic variants may cause loss-of-function and gain-of-toxic-function, and how natural ligands can restore protein function and homeostasis in genetic diseases. Applied chapters provide guidance on employing high throughput sequencing and screening methodologies to develop pharmacological chaperones and repurpose approved drugs to treat protein homeostasis disorders. - Provides an interdisciplinary examination of protein homeostasis disorders, with an emphasis on treatment strategies employing small natural and pharmacological ligands - Offers applied approaches in employing high throughput sequencing and screening to develop pharmacological chaperones to treat protein homeostasis disease - Gathers expertise from a range of international chapter authors who work across various biological methods and disease specific disciplines of relevance
This series presents critical reviews of the present position and future trends in modern chemical research. The short and concise reports on chemistry, each written by the world’s renowned experts, are still valid and useful after 5 or 10 years.
This book contains the best known approaches for preparing the main types of glycosides in a short and comprehensive study. It also includes synthetic pathways of challenging glycosides known as antiviral or antineoplasic drugs, or synthetic substrates used for enzymatic detection including those used as substrates for detection of gene markers in plant biotechnology. Special attention is made on the structural characterization, providing the basic tools for the structural assignment through NMR, X-Ray and mass spectra techniques. Some of the chapters cover strategies for preparation of antiviral and antineoplasic drugs included in a drug design course.
This contributed volume contains 25 chapters from leading international scientists working on dengue and Zika viruses, who came together in Praia do Tofo in Mozambique to discuss the latest developments in the fields of epidemiology, pathogenesis, structural virology, immunology, antiviral drug discovery and development, vaccine efficacy, and mosquito control programs. The meeting venue offered an opportunity to discuss current research on these flaviviruses in an idyllic setting, and also to develop first-hand appreciation of the issues in infectious diseases facing developing countries and of the research gaps in Africa. For readers, who should include basic and clinical researchers in the field and public health professionals, the chapters are organized to provide a comprehensive overview of the various topics in current dengue and Zika virus research. A unique feature of the proceedings of this meeting is the inclusion of the discussions that took place following presentations. These have been transcribed and appended to the end of the relevant chapters, and they form the “salt in the soup” of this book.
This volume provides a collection of contemporary perspectives on using activity-based protein profiling (ABPP) for biological discoveries in protein science, microbiology, and immunology. A common theme throughout is the special utility of ABPP to interrogate protein function and small-molecule interactions on a global scale in native biological systems. Each chapter showcases distinct advantages of ABPP applied to diverse protein classes and biological systems. As such, the book offers readers valuable insights into the basic principles of ABPP technology and how to apply this approach to biological questions ranging from the study of post-translational modifications to targeting bacterial effectors in host-pathogen interactions.
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.
A thorough introduction is provided to the variety and complexity of the roles that glycoconjugates play in the cells of the nervous system. Basic information as well as the latest developments in neural glycobiology are discussed. Topics covered range from the structure and metabolism of the saccharide chains and current approaches used in their study, to changes glycoconjugates undergo during development and aging of the nervous system and the roles they have in neurological disease. The breadth and depth of topics covered make it an essential reference for those new to the field as well more seasoned investigators.
A review of childhood neurodegenerative and other progressive but non-degenerative disorders to guide their diagnosis and management.