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Oncogenic transcription factors are an increasingly important target for anticancer therapies. Inhibiting these transcription factors could allow tumour cells to be "reprogrammed", leading to apoptosis or differentiation from the malignant phenotype. As the use of kinase inhibitors is gradually declining, transcription factor inhibition is the next hot topic for oncology research and merits much attention. This book highlights recent progress in the development of small-molecule inhibitors of oncogenic transcription factors. It also presents the evidence that this important protein class can be modulated in a number of ways to develop novel classes of therapeutic agents. The broad range of aspects covered by the book is noteworthy and renders it enormously valuable. This title serves as a unique reference book for postgraduates, academic researchers and practitioners working in the fields of biochemistry, biotechnology, cell and molecular biology and bio-inorganic chemistry.
While drug therapies developed in the last 50 years have markedly improved the management of some types of cancers, treatment outcomes, and drug side-effects for the most common types remain unacceptable. However, recent technological advances are leading to improved therapies based on targeting distinct biological pathways in cancer cells. "Chemistry and Pharmacology of Anticancer Drugs" is a comprehensive survey of all families of anticancer agents currently in use or in advanced stages of clinical trials, including biologicals.
The book is unique in providing molecular structures for all anticancer drugs, discussing them in terms of history, chemistry, mechanism of action, structure-function relationships, and pharmacology. It also provides some relevant information on side effects, dosing, and formulation. The author, a renowned scientist in cancer research and drug development, also provides up-to-date information on the drug discovery process, including new research tools, tumor-targeting strategies, and fundamental concepts in the emerging areas of personalized medicine (e.g., oncogenomics) and chemoprevention.
"Chemistry and Pharmacology of Anticancer Drugs"is an indispensable resource for cancer researchers, medicinal chemists, and other biomedical scientists involved in the development of new anticancer treatments. Its breadth of coverage also makes it suitable for undergraduate and postgraduate courses in medicine, pharmacy, nursing, and related disciplines.
1.Provide new insights into drug discovery for schizophrenia 2.There has been little progress in this field since the 1950s 3.MedChemComm, Toxicology Research, Issues in Toxicology Series 4.Geneticists, pharmacologists, molecular biologists and medicinal chemists in academia and industry. 5.Will fill the gaps in knowledge of neurobiology of schizophrenia and providing novel perspectives in drug development.
Traditional Chinese medicine has a strong scientific basis, but the science of these important preparations is often rarely discussed. Western approaches often simplify traditional Chinese medicine to drug discovery in Chinese plants, however, the majority of traditional Chinese medications use complex mixtures of plant extracts, rather than single purified drugs. The combination of different extracts is based on yin, yang and chi theories, which are often poorly understood in the West. Yin and yang are known to be the balance of agonists and antagonists, whereas chi derives from signalling processes in the body and regulates bodily functions. Traditional Chinese medical practitioners understand that yin, yang and chi constantly interact in the body to maintain health. Western medical practitioners understand how to use agonists and antagonists and how to modify signalling processes, but generally do not accept the use of complex plant extracts to perform these functions. Aimed at medical scientists, and including detailed explanations of the theories behind the science, this text may help researchers to understand Chinese medical practitioners and to communicate more effectively with them. It will also lead to greater acceptance of traditional medications in the West. Presenting a clear rationale for the use of traditional Chinese medications in Western medical facilities, it enables scientists to find new directions in experimental design and encourage examination of these useful, but often poorly understood, preparations in clinical trials.
This book brings together drug design practitioners, all leaders in their field, who are actively advancing the field of quantitative methods to guide drug discovery, from structure-based design to empirical statistical models - from rule-based approaches to toxicology to the fields of bioinformatics and systems biology. The aim of the book is to show how various facets of the drug discovery process can be addressed in a quantitative fashion (ie: numerical analysis to enable robust predictions to be made). Each chapter includes a brief review of the topic showing the historical development of quantitative approaches, a survey/summary of the current state-of-the-art, a selection of well chosen examples with some worked through and an appreciation of what problems remain to be overcome as well as an indication of how the field may develop. After an overview of quantitative approaches to drug design the book describes the development of concepts of "drug-like properties", of quantitative structure-activity relationships and molecular modelling, and in particular, structure-based design approaches to guide lead optimisation. How to manage and describe chemical structures, underpins all quantitative approaches to drug design and these are described in the following chapters. The next chapter covers the value of a quantitative approach, and also the challenge which is to describe the confidence in any prediction, and methods to assess predictive model quality. The later chapters describe the application of quantitative approaches to describing and optimising potency, selectivity, drug metabolism and pharmacokinetic properties and toxicology, and the design of chemical libraries to feed the screening approaches to lead generation that underpin modern drug discovery. Finally the book describes the impact of bioinformatics, current status of predicting ligand affinity direct from the protein structure, and the application of quantitative approaches to predicting environmental risk. The book provides a summary of the current state-of-the-art in quantitative approaches to drug design, and future opportunities, but it also provides inspiration to drug design practitioners to apply careful design, to make best use of the quantitative methods that are available, while continuing to improve them. Drug discovery still relies heavily on random screening and empirical screening cascades to identify leads and drugs and the process has many failures to deliver only a small handful of drugs. With the rapidly escalating costs of drug discovery and development together with spiralling delivery, quantitative approaches hold the promise of shifting the balance of success, to enable drug discovery to maintain its economic viability.
Modelling and simulation technologies have improved dramatically over the past decade and their applications in toxicity prediction and risk assessment are of great importance. Such approaches will become increasingly necessary as industrial chemicals advance and as new pharmaceuticals enter the market. In this comprehensive discussion of predictive toxicology and its applications, leading experts express their views on the technologies currently available and the potential for future developments. The book covers a wide range of topics including the in silico, in vitro and in vivo approaches being used in the safety assessment of chemical substances. It reflects the growing and urgent need to strengthen our ability to predict the risks posed by industrial and pharmaceutical chemicals in humans. Extensive information on the use of current animal models used for various toxicities and target-mediated toxicities is included. Also discussed are the recently introduced regulatory initiatives.
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 (Kadcyla (TM)), brentuximab vedotin (Adcetris (TM)), inotuzumab ozogamicin (Besponsa (TM)), gemtuzumab ozogamicin (Mylotarg (TM)) and moxetumomab pasudotox-tdfk (Lumoxiti (R))] 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.
The discovery and development of effective medicines for the treatment of psychiatric disorders such as schizophrenia and depression has been heralded as one of the great medical achievements of the past century. Indeed, the profound impact of these medicines on our understanding of the pathophysiology underlying these diseases, the treatment of psychiatric patients and even our social perception of mental illnesses cannot be underestimated. However, there is still an urgent medical need for even more effective, safe and well-tolerated treatments. For example, currently available treatments for schizophrenia address mainly the positive symptoms and largely neglect the negative symptoms and cognitive disfunction which greatly impact overall morbidity. Similarly, whilst the current first line antidepressants show significantly improved side effect profiles compared to the first generation therapies, there still up to 40% of patients who are treatment resistant, and even in the patient population which responds well, the onset of action is slow at typically 2-3 weeks. The aim of this book is to provide the first point of call for those involved or just interested in this rapidly expanding and increasingly fragmented field of research and drug discovery. The editors will combine their wide ranging experience and extensive network of contacts with leading scientists and opinion leaders in this field to provide an authoritative reference text covering the evolution, major advances, challenges and future directions in drug discovery and medicinal chemistry for major psychiatric disorders.
From crystal structure prediction to totally empirical screening, the quest for new crystal forms has become one of the most challenging issues in the solid state science and particularly in the pharmaceutical world. In this context, multi-component crystalline materials like co-crystals have received renewed interest as they offer the prospect of optimized physical properties. As illustrated in this first book_ entirely dedicated to this emerging class of pharmaceutical compounds_ the outcome of such endeavours into crystal engineering have demonstrated clear impacts on production, marketing and intellectual property protection of active pharmaceutical ingredients (APIs). Indeed, co-crystallization influences relevant physico-chemical parameters (such as solubility, dissolution rate, chemical stability, melting point, hygroscopicity, a) and often offers solids with properties superior to those of the free drug. Combining both reports of the latest research and comprehensive overviews of basic principles, with contributions from selected experts in both academia and industry, this unique book is an essential reference, ideal for pharmaceutical development scientists and graduate students in pharmaceutical science."
Comprehensive Biomarker Discovery and Validation for Clinical Application provides the reader with an extensive introduction into all aspects of proteomics biomarker discovery, validation and development. It discusses the current status of science and technology, its limitations, bottlenecks as well as future development trends to improve the success rate of translating biomarker discovery into useful clinical tests. The most important feature of the book is to provide an overview of current technologies and the challenges encountered during biomarker discovery and validation, such as patient selection, sample handling, data processing, statistical analysis and registration and approval of validated biomarkers through European and US regulatory authorities. The authors introduce the reader to each of these topics in significant detail and provide examples or guidelines for best practice. There are prominent chapters included on biomarkers in translational and personalised medicine; an introduction to regulatory affairs and bring biomarkers to the market; biomarker discovery and the use of mass spectrometry based profiling platforms; MALDI imaging techniques in tissue-based biomarkers discovery and a clinical application study on the use of diagnostic assays for early diagnosis of heart failure using various proteomic methods. The book concludes with a final chapter on future trends in biomarker discovery and validation. The book targets a readership of industrial and academic researchers that are involved in biomarker discovery and validation or that manage biobanks, develop sample preparation methods, analytical profiling systems and bioinformatics tools. Common pitfalls and success stories in biomarker discovery are highlighted and guidelines for best practice are provided for the different parts of the procedure. The book will be an essential information resource for scientists working in the field.
Nuclear receptors (NR) are ligand-induced activated transcription factors that are involved in numerous biological processes. Since the 1990's when the first structures were determined by means of X ray diffraction, the number of NR structures has increased considerably. Moreover several "omics" projects (genomics, pharmcogenomics and proteomics) have opened up great opportunities for the discovery of new targets, the characterization of abnormal protein patterns, the selection of "tailored" drugs and the evaluation of drug efficacy even with a lack of structural data. Furthermore, structure-based drug design, computational methods for in silico screening and nanobiotechnology- based tools are simplifying this time-consuming and money-intensive research of lead compounds and, possibly, new drugs. Biological interactions such as those that occur between a protein and ligand are concerted events where flexible molecules interact. Thus understanding flexibility of large molecules or biological complexes is of primary importance to help define the right model to approximate the reality for drug discovery, virtual screening, food safety analysis, etc. NRs are known as flexible targets, with many structural similarities, in particular for their Ligand Binding Domain: these similarities could be assumed to share behavioural qualities that belong to this class of compounds. Thus to supply a possible, complete and exhaustive answer to questions about the behaviour of NRs, their interactions with new potential drugs, endocrine disruptors such as animal and human food toxins, food additives or industry residuals, it is mandatory to approach the problem from a different point of view: a molecular modelling approach, steered synthesis, and in vitro and in vivo tests, etc. The aim of this book is to provide a state of the art review on investigations into Nuclear Receptors.
Multi-target drug discovery (MTDD) is an emerging area of increasing interest to the drug discovery community. Drugs that modulate several targets have the potential for an improved balance of efficacy and safety compared to single targets agents. Although there are a number of marketed drugs that are thought to derive their therapeutic benefit by virtue of interacting with multiple targets, the majority of these were discovered accidentally. Written by world renowned experts, this is the first book to gather together knowledge and experiences of the rational discovery of multi-target drugs. It describes the current state of the art, the achievements and the challenges of the field and importantly the lessons learned by researchers to date and their application to future MTDD.
This book documents the latest research into the theory and application of force-fields, semi-empirical molecular orbital, density functional and ab initio calculations, Quantum Mechanical (QM) based modelling, Atoms in Molecules (AIM) approach, and biomolecular dynamics. It also covers theory and application of 2D cheminformatics, QSAR/QSPR, ADME properties of drugs, drug docking/scoring protocols and approaches, topological methodology, and modelling accurate inhibition constants of enzymes. Finally, the book gives the theory and applications of multiscale modelling of proteins and biomolecular systems. The information need for a book in this area is due to the continuing rapid advance of firstly theoretical approaches, secondly software/hardware and lastly the successful application of the technology and this book fills a gap in the literature. The co-editors have extensive experience of teaching and researching in the field and the book includes contributions from cutting-edge academic and industrial researchers in their respective fields. It is essential reading for medicinal chemists, computational chemists and those in the pharmaceutical industry.
Due to injuries sustained in sports and in combat, interest in TBI has never been greater. Biomarkers for Traumatic Brain Injury will fulfil a gap in our understanding of what is occurring in the brain following injury that can subsequently be detected in biological fluids and imaging. This knowledge will be useful for all researchers and clinicians interested in the biochemical and structural sequelae underpinning clinical manifestations of TBI and help guide appropriate patient management. Current and prospective biomarkers for the assessment of traumatic brain injury (TBI), particularly mild TBI, are examined using a multidisciplinary approach involving biochemistry, molecular biology, and clinical chemistry. The book incorporates presentations from outstanding researchers and clinicians in the area and describes advanced proteomic and degradomic technologies in the development of novel biomarker assays. For practical purposes, the focus of this volume is on detection of blood-based biomarkers to improve diagnostic certainty of mild TBI in conjunction with radiological and clinical findings. It represents contributions from internationally-recognized researchers at the forefront of traumatic brain injury many of whom are recipients of grants and contracts from the United States Department of Defense for research specifically on developing diagnostic tests for TBI. The book will be essential reading for scientists, pharmacologists, chemists, medical and graduate students.
Kinase drug discovery remains an area of significant interest across academia and in the pharmaceutical industry. There are now around 13 FDA approved small molecule drugs which target kinases and many more compounds in various stages of clinical development. Although there have been a number of reviews/publications on kinase research, this book fills a gap in the literature by considering the current and future opportunities and challenges in targeting this important family of enzymes. The book is forward-looking and identifies a number of hot topics and key areas for kinase drug discovery over the coming years. It includes contributions from highly respected authors with a combined experience in the industry of well over 200 years, which has resulted in a book of great interest to the kinase field and across drug discovery more generally. Readers will gain a real insight into the huge challenges and opportunities which this target class has presented drug discovery scientists. The many chapters cover a wide breadth of topics, are well written and include high quality colour and black and white images. Topics covered include an outline of how medicinal chemistry has been able to specifically exploit this unique target class, along with reflections on the mechanisms of kinases inhibitors. Also covered is resistance to kinase inhibitors caused by amino acid mutations, case studies of kinase programs and reviews areas beyond protein kinases and beyond the human kinome. Also described are modern approaches to finding kinase leads and the book finishes with a reflection of how kinase drug discovery may progress over the coming years.
There are about 8 million deaths each year from neglected tropical diseases (NTDs) in the underdeveloped world, whilst drug discovery focus and practice is only recently taking on greater urgency and embracing the latest technologies. This unique book is a state of the art review of drug discovery in respect of NTDs and highlights best practice to guide the ongoing drug discovery effort and also to raise debate and awareness in areas that remain highly neglected. All the major diseases such as malaria, trypanosomatids and TB are covered, with a review of each disease and established compounds, new mechanistic classes and new horizons. Each chapter highlights the key science that has led to breakthroughs, with detailed assessment of the key medicinal chemistry involved, and critical appraisal of new emerging approaches. Later chapters highlight under publicized disease areas where the medical needs are neglected and research is very limited, to raise awareness. The editors, acknowledged experts in the field, have a wealth of experience in successful drug discovery practice and tropical diseases.
Pharmaceutical process research and development is an exacting, multidisciplinary effort but a somewhat neglected discipline in the chemical curriculum. This book presents an overview of the many facets of process development and how recent advances in synthetic organic chemistry, process technology and chemical engineering have impacted on the manufacture of pharmaceuticals. In 15 concise chapters the book covers such diverse subjects as route selection and economics, the interface with medicinal chemistry, the impact of green chemistry, safety, the crucial role of physical organic measurements in gaining a deeper understanding of chemical behaviour, the role of the analyst, new tools and innovations in reactor design, purification and separation, solid state chemistry and its role in formulation. The book ends with an assessment of future trends and challenges. The book provides a valuable overview of: both early and late stage chemical development, how safe and scaleable synthetic routes are designed, selected and developed, the importance of the chemical engineering, analytical and manufacturing interfaces, the key enabling technologies, including catalysis and biocatalysis, the importance of the green chemical perspective and solid form issues. The book, written and edited by experts in the field, is a contemporary, holistic treatise, with a logical sequence for process development and mini-case histories within the chapters to bring alive different aspects of the process. It is completely pharmaceutical themed, encompassing all essential aspects, from route and reagent selection to manufacture of the active compound. The book is aimed at both graduates and postgraduates interested in a career in the pharmaceutical industry. It informs them about the breadth of the work carried out in chemical research and development departments, and gives them a feel for the challenges involved in the job. The book is also of value to academics who often understand the drug discovery arena, but have far less appreciation of the drug development area, and are thus unable to advise their students about the relative merits of careers in chemical development versus discovery.
Intracellular cell signaling is a well understood process. However, extracellular signals such as hormones, adipokines, cytokines and neurotransmitters are just as important but have been largely ignored in other works. They are causative agents for diseases including hypertension, diabetes, heart disease, and arthritis so offer new, and often more approachable, targets for drug design. Aimed at medical professionals and pharmaceutical specialists, this book integrates extracellular and intracellular signalling processes and offers a fresh perspective on new drug targets. Written by colleagues at the same institution, but with contributions from leading international authorities, it is the result of close cooperation between the authors of different chapters. Readers are introduced to a new approach to disease causation by adipokines and toxic lipids. Heart disease, migraines, stroke, Alzheimer's disease, diabetes, cancer, and arthritis are approached from the perspective of prevention and treatment by alteration of extracellular signalling. Evidence is presented that the avoidance of toxic lifestyles can reduce the incidence of such illnesses and new therapeutic targets involving adipokines, ceramide and endocannabinoids are discussed.
In recent years, medical developments have resulted in an increase in human life expectancy. Some developed countries now have a larger population of individuals aged over 64 than those under 14. One consequence of the ageing population is a higher incidence of certain neurodegenerative disorders. In order to prevent these, we need to learn more about them. This book provides up-to-date information on the use of transgenic mouse models in the study of neurodegenerative disorders such as Alzheimer's and Huntington's disease. By reproducing some of the pathological aspects of the diseases, these studies could reveal the mechanism for their onset or development. Some of the transgenic mice can also be used as targets for testing new compounds with the potential to prevent or combat these disorders. The editors have extensive knowledge and experience in this field and the book is aimed at undergraduates, postgraduates and academics. The chapters cover disorders including: Alzheimer's disease, Parkinson's disease, Huntington's and other CAG diseases, amyotrophic lateral sclerosis (ALS), recessive ataxias, disease caused by prions, and ischemia.
Ion channel drug discovery is a rapidly evolving field fuelled by recent, but significant, advances in our understanding of ion channel function combined with enabling technologies such as automated electrophysiology. The resurgent interest in this target class by both pharmaceutical and academic scientists was clearly highlighted by the over-subscribed RSC/BPS 'Ion Channels as Therapeutic Targets' symposium in February 2009. This book builds on the platform created by that meeting, covering themes including advances in screening technology, ion channel structure and modelling and up-to-date case histories of the discovery of modulators of a range of channels, both voltage-gated and non-voltage-gated channels. The editors have built an extensive network of contacts in the field through their first-hand scientific experience, collaborations and conference participation and the organisation of the meeting at Novartis, Horsham, increased the network enabling the editors to draw on the experience of eminent researchers in the field. Interest and investment in ion channel modulation in both industrial and academic settings continues to grow as new therapeutic opportunities are identified and realised for ion channel modulation. This book provides a reference text by covering a combination of recent advances in the field, from technological and medicinal chemistry perspectives, as well as providing an introduction to the new 'ion channel drug discoverer'. The book has contributions from highly respected academic researchers, industrial researchers at the cutting edge of drug discovery and experts in enabling technology. This combination provides a complete picture of the field of interest to a wide range of readers.
Anti-Inflammatory Drug Discovery provides a comprehensive review of recent medicinal chemistry approaches to a variety of important therapeutic targets and provides a key reference for those interested in the prosecution of modern drug discovery programs directed at anti-inflammatory mechanisms of action. The editors, with extensive experience in this field, have selected key thought-leaders who will bring their experience to the medicinal chemistry literature for each target, ranging from components of the arachadonic acid cascade, to kinases, GPCRs, sphingolipids and others, to summarize its background biology and detail new insights, major advances and issues related to bringing new anti-inflammatory therapies to market. Consisting of five main sections key targets covered will include the AA Cascade: mPGES1, cPLA2, Leukotriene A4 Hydrolase, CRTH2; Kinases: P38/PDE4, MAPKAP Kinase 2 (MK2), Syk Kinase Inhibitors, Jak Kinases, IKK , Bruton's Tyrosine Kinase; GPCRs: CCR1, CCR2 Antagonists, CB2 Agonists; Sphingolipids: S1P1 Receptor Agonists, Sphingosine Lyase and Sphingosine Kinase 1 and a final miscellaneous section that looks at Non-Steroidal Dissociated Glucocorticoid Receptor Agonists. The book will be essential reading for pharmacologists, medicinal chemists and pharmaceutical scientists working in industry and academia.
The need for customized stem cell therapies for specific conditions will be a major issue in the coming decades. This unique book by experts in the field reviews the subject as it stands today. Its coverage includes: basic and applied stem cell research and history; sources of adult stem cells; a comparison of difficulties in derivation, and the applications of embryonic and adult stem cells. Specific topics dealt with include advantages and problems associated with stem cell / matrix interactions and stem cell differentiation, difficulties using stem cells for clinical application, stem cell based tissue engineering - myth or reality, stem cells and immunity, natural biological matrices versus synthetic (biocompatibility and integration), stem cell delivery, labeling, imaging and tracking, bioreactors: 2D and 3D cell culturing for in-vitro studies and for stem cell implantation, ethical and safety issues and Good Manufacturing Practice (GMP).
Until now, the area of drug metabolism and pharmacokinetics has been lacking in texts written for the Medicinal Chemist. This outstanding book, aimed at postgraduate medicinal chemists and those working in industry, fills this gap in the literature. Written by medicinal chemists and ADMET scientists with a combined experience of around 300 years, this aid to discovering drugs addresses the absorption, distribution, metabolism, excretion and toxicity (ADMET) issues associated with drugs. The book starts by describing drug targets and their structural motifs before moving on to explain ADMET for the medicinal chemist. It is the functional groups which most profoundly influence the drug molecules of which they form a part. They characterise the pharmacology, are essential to the activity, and alter the ADMET characteristics of each drug. Their effects follow a pattern, thus allowing medicinal chemists to predict and overcome potential challenges. For this reason, the Editors have taken the unique approach of dividing the remainder of the book into chapters which each focus on a different functional group. They describe drugs containing the functional group under consideration, explain why the group is there, and outline its physicochemical properties before going on to detail the ADMET issues. Where possible, prodrugs and bioisosteres, which may give alternative ADMET outcomes, are described. The chapters cross refer where similar matters are covered but individual chapters can be used in a stand alone manner. The book ends with a discussion of future targets and chemistry needs.
This book is one of a three-volume set that provides theoretical, practical and troubleshooting guidelines on all aspects of the pre-clinical Drug Discovery process. There is particular focus on the design, development and role of screening assays in Drug Discovery, including new developments and future trends, the main assay types utilized in screening campaigns, and the methods utilized in enabling the progression of "Hits" to "Leads" and "Candidates" The books will fill current gaps in the literature such as primary, stem cell and other novel assay methods. Other relatively new research areas included are siRNA, high content screening, protein-protein interactions, pathway assays, non micro-titre plate based assays, label free assays, IT tools, approaches to identify biopharmaceuticals, emerging models and future trends in Drug Discovery.
This book offers an integrated review of the most recent trends in natural products drug discovery and key lead candidates that are outstanding for their chemistry and biology as a starting point in novel drug development. The authors focus on different trends that are and will continue to be impacting multiples stages of modern drug discovery from NPs that have not been included in other works. This is complemented with a series of case studies from leading experts from industry and academia on key molecules and derivatives that have been chosen for their novelty in chemistry, biology and clinical applications. The book intends to reflect the current confluence of different disciplines in chemical biology and synthetic chemistry supported by a more profound knowledge of systems biology that ensures the concurrency and synergisms of expertise from different research fields that impact in the discovery of novel molecules. In the first section the chapters reflect recent approaches to exploit the biosynthetic potential of microbial resources (including genome mining, metagenomic and epigenetic approaches), as well as biosynthetic chemistry tools to respond to product supply and novel screening alternatives that have lead to the discovery of novel chemistry. The second part reviews, in the form of case studies, some examples of bioactive molecules in the important therapeutic areas of antiinfectives, oncology and antiparasitics.
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