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This book summarizes the latest findings about the role of cancer stem cells (CSCs) in cancer biology and how this knowledge could be used for novel anticancer therapies. It provides an overview of CSCs in selected malignancies with particular emphasis on hematopoietic neoplasias. It then reviews the role of CSCs in metastasis formation and initiat
An essential outline of the main facets of polypharmacology in drug discovery research Extending drug discovery opportunities beyond the "one drug, one target" philosophy, a polypharmacological approach to the treatment of complex diseases is emerging as a hot topic in both industry and academic research. Polypharmacology in Drug Discovery presents an overview of the various facets of polypharmacology and how it can be applied as an innovative concept for developing medicines for treating bacterial infections, epilepsy, cancer, psychiatric disorders, and more. Filled with a collection of instructive case studies that reinforce the material and illuminate the subject, this practical guide: Co...
This book reviews recent physicochemical and biophysical techniques applied in drug discovery research, and it outlines the latest advances in computational drug design. Divided into 10 chapters, the book discusses about the role of structural biology in drug discovery, and offers useful application cases of several biophysical and computational methods, including time-resolved fluorometry (TRF) with Förster resonance energy transfer (FRET), X-Ray crystallography, nuclear magnetic resonance spectroscopy, mass spectroscopy, generative machine learning for inverse molecular design, quantum mechanics/molecular mechanics (QM/MM,ONIOM) and quantum molecular dynamics (QMT) methods. Particular attention is given to computational search techniques applied to peptide vaccines using novel mathematical descriptors and structure and ligand-based virtual screening techniques in drug discovery research. Given its scope, the book is a valuable resource for students, researchers and professionals from pharmaceutical industry interested in drug design and discovery.
This series provides a comprehensive resource for postgraduate students and for scientists in academia or industry wanting to learn topics outside their own areas of expertise.
This book reviews the challenges and opportunities posed by flow chemistry in drug discovery, and offers a handy reference tool for medicinal chemists interested in the synthesis of biologically active compounds. Prepared by expert contributors, the respective chapters cover not only fundamental methodologies and reactions, such as the application of catalysis, especially biocatalysis and organocatalysis; and non-conventional activation techniques, from photochemistry to electrochemistry; but also the development of new process windows, processes and reactions in drug synthesis. Particular attention is given to automatization and library synthesis, which are of great importance in the pharma...
This book overviews purinergic receptors that are playing key roles in human and pathophysiological processes. The book elaborates on how selective P1 and P2 modulators have been developed as therapeutics for a variety of diseases. It also provides an overview of current perspectives in the design of purinergic receptor modulators and future challenges such as the availability of selective ligands for all receptor subtypes. Divided into 12 chapters, this comprehensive volume also offers a multidisciplinary perspective on the historical evolution, starting with a chapter devoted to the roots and early discoveries of adenosine and its receptors, followed by a twenty-year retrospective on the s...
This book deals with the recent advances in DNA-Encoded Library (DEL) technology that has emerged as an alternative to high throughput screening (HTS) over the last decade and has been heralded as a "disruptive" technology for drug discovery. The book aims to provide a comprehensive overview of all of the major components of the DEL process from conception to bench execution and clinical investigations. The contributions from experts in the field combine different perspectives from academia and industry. The book will be of interest to researchers in the drug discovery field as well as to graduate students and scholars who are interested in this rapidly improving technology.
Toll-like receptors (TLRs) represent a powerful system for recognition and elimination of pathogen-associated molecular patterns (PAMPs) from bacteria, viruses, and other pathogens and damage-associated molecular patterns (DAMPs) released from dying cells. TLRs are mainly expressed on immune cells, but can also be present on other cell populations. Typical PAMPs include bacterial cell wall components, viral pathogens, or pathogenic nucleic acids, including viral RNA and DNA. Activation of TLRs leads to the production of proinflammatory cytokines and type I interferons which are important for induction of the host immune response against bacterial and viral infections. However, dysregulation and overstimulation can be detrimental leading to hyper-inflammation, sepsis, and loss of tissue integrity. Furthermore, TLRs are involved in the pathogenesis of acute viral infections, including COVID-19. Consequently, TLRs are promising targets for pharmacological intervention and treatment.
Published by the University of Nebraska Press, Lincoln, and Yad Vashem, Jerusalem “We were both small nations whose existence could never be taken for granted,” Vaclav Havel said of the Czechs and the Jews of Israel in 1990, and indeed, the complex and intimate link between the fortunes of these two peoples is unique in European history. This book, by one of the world’s leading authorities on the history of Czech and Slovak Jewry during the Nazi period, is the first to thoroughly document this singular relationship and to trace its impact, both practical and profound, on the fate of the Jews of Bohemia and Moravia during the Holocaust. Livia Rothkirchen provides a detailed and comprehe...
Retaining the successful approach found in the previous volume in this series, the inventors and primary developers of drugs that successfully made it to market tell the story of the drug's discovery and development and relate the often twisted route from the first candidate molecule to the final marketed drug. 11 selected case studies describe recently introduced drugs that have not been previously covered in textbooks or general references. These range across six different therapeutic fields and provide a representative cross-section of the current drug development efforts. Backed by copious data and chemical information, the insight and experience of the contributors makes this one of the most useful training manuals that a junior medicinal chemist can hope to find and has won the support and endorsement of IUPAC.