Cancer-Leading Proteases: Structures, Functions, and Inhibition presents a detailed discussion on the role of proteases as drug targets and how they have been utilized to develop anticancer drugs. Proteases possess outstanding diversity in their functions. Because of their unique properties, proteases are a major focus of attention for the pharmaceutical industry as potential drug targets or as diagnostic and prognostic biomarkers. This book covers the structure and functions of proteases and the chemical and biological rationale of drug design relating to how these proteases can be exploited to find useful chemotherapeutics to fight cancers. In addition, the book encompasses the experimental and theoretical aspects of anticancer drug design based on proteases. It is a useful resource for pharmaceutical scientists, medicinal chemists, biochemists, microbiologists, and cancer researchers working on proteases.

In this book, the author focuses on exploring new organocatalytic transformations under operationally simple and environmentally friendly reaction conditions. Two new types of catalytic reactions promoted by N-heterocyclic carbenes (NHCs) are described. The oxa- and azacycle-forming reactions of sulfonylalkynols and sulfonylalkynamides are broadly considered to be a new type of activation mode in NHC chemistry, wherein the bond formation with internal O- and N-nucleophiles occurs at the -position of the propargyl sulfones with 1,2-sulfonyl migration. The resulting oxa- and azacycles are core structures in many biologically significant compounds and medicinally important agents. In addition, the book develops the chiral NHC-catalyzed kinetic resolution of -hydroxy carboxylic acid derivatives based on chiral recognition of the substrate-cocatalyst complex. In this carboxylate cocatalyst-assisted chiral acylation, the reaction rate acceleration and selectivity enhancement are interpreted in terms of the reversible complexation of the substrate and carboxylate cocatalyst, which is verified by control experiments and measured using analytical methods. The findings described here reveal a promising new aspect of not only NHC catalysis but also identifying novel catalysis systems.

Medical Empathy, Pharmacological Systems, and Treatment Strategies in Integrative Cardiovascular Chinese Medicine, volume two in the Integrative Cardiovascular Chinese Medicine series, presents sections on holism and humanity in medicine, considering the patient, medical empathy in prescribing, modifying and weaning, an overview of pharmacologic systems, an overview of pharmacology sciences and the cardiovascular drug classes and types as revealed from perspectives of Chinese and Western medicine, including descriptions of pharmaceutical drugs from China and the United States, with current pictures and inpatient directions. Finally, principles and treatments according to disease stages for each cardiovascular disease within the scope of integrative medicine is outlined. This important reference will aid cardiovascular researchers in the study of integrative Chinese and Western medicine and provide a clear, structured base to guide clinical practice and encourage collaboration between Chinese and Western medicine practitioners

This book offers an in indictment of the nation's drug enforcement approach focusing on the short-sighted policies that often deny patients suffering from chronic pain the medications they need. Pain Control and Drug Policy: A Time for Change focuses on America's national crisis in pain management caused by the widening divergence between the enormous contributions of opioids ("narcotics") to pain management in the clinical setting and the mistaken belief that they are dangerous, highly addictive drugs. After dissecting the strategy and tactics of the War on Drugs from medical, historical, legal, socioeconomic, and geopolitical perspectives, Guy Faguet MD indicts the 40-year-long War on Drugs for having failed to stem the supply of illicit drugs in America despite expenditures of half a trillion dollars, despite violating the basic human right to pain relief of tens of millions of American chronic pain sufferers, and despite fomenting organized crime, government corruption, racial injustice, and social disruption in both the United States and the producer countries. He concludes with a clarion call for the abandonment of the War on Drugs, disbanding the Drug Enforcement Administration, and encouraging Congress to repeal the Controlled Substances Act. As a clinical and research oncologist responsible for the chronic pain management of thousands of cancer patients over the course of his 30-year career, Dr. Faguet knows that the most effective and safest way to manage most cases of chronic pain is with opioids. All modern pain-management textbooks advocate "titration to effect" in cases where opioids help: that is, gradually increasing the dosage until either the pain is acceptably controlled or the side effects begin to outweigh the pain-relief benefits. Yet the vast majority of doctors don't practice what the medical textbooks teach and instead prescribe opioids very reluctantly and conservatively. As a result, only half of all chronic pain sufferers-and fewer than half of all cancer patients-get adequate pain relief from their doctors. Why do physicians radically undertreat pain that is susceptible to opioid analgesics? They fear that if they prescribe Schedule II opioids in accordance with the professional standards of pain management set by such medical bodies as the American Pain Society, they will be investigated by the DEA, stigmatized, prosecuted as criminals, stripped of their licenses, and sent to jail. Visit Guy B. Faguet, MD's website here: www.faguet.net.

A great deal of interest has been generated recently in the isolation, characterization, and biological activity of phytochemicals. Phytochemicals have the potential to enhance pharmaceuticals and drug discovery. As such, there is an urgent need for current research in the global scope of phytochemicals including the chemical and physical characteristics, analytical procedures, biological activity, safety, and industrial applications. The Handbook of Research on Advanced Phytochemicals and Plant-Based Drug Discovery examines the applications of bioactive molecules from a health perspective, examining the pharmacological aspects of medicinal plants, the phytochemical and biological activities of different natural products, and ethnobotany and medicinal properties. Moreover, it presents a novel dietary approach for human disease management. Covering topics such as computer-aided drug design, government regulation, and medicinal plant taxonomy, this major reference work is beneficial to pharmacists, medical practitioners, phytologists, hospital administrators, government officials, faculty and students of higher education, librarians, researchers, and academicians.

Blockbuster drugs-each of which generates more than a billion dollars a year in revenue-have revolutionized the industry since the early 1980s, when sales of Tagamet alone transformed a minor Philadelphia-based firm into the world's ninth-largest pharmaceutical company. In Blockbuster Drugs, Jie Jack Li tells the fascinating stories behind the discovery and development of these highly lucrative medicines, while also exploring the tumult the industry now faces as the "patent cliff" nears. Having spent most of his career in drug research and development, Li brings an insider's eye to the narrative as he recounts the tales of discovery behind such drugs as Tagamet, Zantac, Claritin, Prilosec, Nexium, Serouquel, Plavix, and Ambien. As he discusses each breakthrough, Li also shows that scientific research is filled with human drama-serendipitous discoveries, sudden insights, tense confrontations. For instance, the author tells of James Black, who persisted in the research that led to Tagamet-and that would ultimately win him a Nobel Prize-despite pressure from top executives to pursue "more profitable" work. The book shows how research behind Prilosec combined creativity, international cooperation, and luck-the turning point being a chance encounter of American and Swedish scientists at a conference in Uppsala. There are also tales of fabulous rewards-George Rieveschl, the chemist who invented Benadryl, made a fortune on royalties-and of unjust desserts. Finally, Li shows that for the world's largest prescription drug manufacturers, recent years have been harrowing, as many popular drugs have come off patent in the U.S. market, meaning hundreds of billions of dollars in lost revenue. Anyone who enjoys tales of scientific discovery, or is curious about the history behind the prescriptions they take, or wants a revealing inside look at the pharmaceutical industry will find this book well worth reading.

Nervous System Drug Delivery: Principles and Practice helps users understand the nervous system physiology affecting drug delivery, the principles that underlie various drug delivery methods, and the appropriate application of drug delivery methods for drug- and disease-specific treatments. Researchers developing nervous system putative therapeutic agents will use this book to optimize drug delivery during preclinical assessment and to prepare for regulatory advancement of new agents. Clinicians will gain direct insights into pathophysiologic alterations that impact drug delivery and students and trainees will find this a critical resource for understanding and applying nervous system drug delivery techniques.

Translational Medicine in CNS Drug Development, Volume 29, is the first book of its kind to offer a comprehensive overview of the latest developments in translational medicine and biomarker techniques. With extensive coverage on all aspects of biomarkers and personalized medicine, and numerous chapters devoted to the best strategies for developing drugs that target specific disorders, this book presents an essential reference for researchers in neuroscience and pharmacology who need the most up-to-date techniques for the successful development of drugs to treat central nervous system disorders. Despite increases in the number of individuals suffering from CNS-related disorders, the development and approval of drugs for their treatment have been hampered by inefficiencies in advancing compounds from preclinical discovery to the clinic. However, in the past decades, game-changing strides have been made in our understanding of the pathophysiology of CNS disorders and the relationship of drug exposure in plasma and CNS to pharmacodynamic measures in both animals and humans.

The Core Model: A Collaborative Paradigm for the Pharmaceutical Industry and Global Health Care develops the innovative core model, an organizational research and design paradigm and economic theory that proposes a collaborative approach to resolving global health issues and improving the productivity of drug development. The model proposes that scientific collaboration does not occur in an unstructured manner, but actually takes place within a highly structured order where knowledge is transferred, integrated and finally translated into commercial products. An understanding of this model will help solve the global pharmaceutical industrys productivity problems and address important global health care and economic issues. This book is useful to researchers, advanced students, regulators, and management in pharmaceutical industries, as well as healthcare professionals, those working in health economics, and those interested in scientific innovation processes.

NETosis: Immunity, Pathogenesis and Therapeutics takes a focused approach to the clinical aspects of NETosis and drug development, bringing critical findings. Chapters introduce NETosis, consider mechanisms and antimicrobial strategies regulating NETosis, examine NETosis in neonates, explore the role of NETosis in autoimmunity, delve into NETosis and other diseases, and present therapeutic approaches for dysregulated NETosis. Since Brinkamm, et al, discovered an unrecognized neutrophil anti-microbial mechanism responsible for the extracellular killing of invading pathogens in 2004, the novel process in which nuclear chromatin de-condenses and DNA is ejected into the extra cellular environment, trapping and inactivating tissue pathogens has rapidly evolved.

This is an introductory statistics book designed to provide scientists with practical information needed to apply the most common statistical tests to laboratory research data. The book is designed to be practical and applicable, so only minimal information is devoted to theory or equations. Emphasis is placed on the underlying principles for effective data analysis and survey the statistical tests. It is of special value for scientists who have access to Minitab software. Examples are provides for all the statistical tests and explanation of the interpretation of these results presented with Minitab (similar to results for any common software package). The book is specifically designed to contribute to the AAPS series on advances in the pharmaceutical sciences. It benefits professional scientists or graduate students who have not had a formal statistics class, who had bad experiences in such classes, or who just fear/don't understand statistics. Chapter 1 focuses on terminology and essential elements of statistical testing. Statistics is often complicated by synonyms and this chapter established the terms used in the book and how rudiments interact to create statistical tests. Chapter 2 discussed descriptive statistics that are used to organize and summarize sample results. Chapter 3 discussed basic assumptions of probability, characteristics of a normal distribution, alternative approaches for non-normal distributions and introduces the topic of making inferences about a larger population based on a small sample from that population. Chapter 4 discussed hypothesis testing where computer output is interpreted and decisions are made regarding statistical significance. This chapter also deasl with the determination of appropriate sample sizes. The next three chapters focus on tests that make decisions about a population base on a small subset of information. Chapter 5 looks at statistical tests that evaluate where a significant difference exists. In Chapter 6 the tests try to determine the extent and importance of relationships. In contrast to fifth chapter, Chapter 7 presents tests that evaluate the equivalence, not the difference between levels being tested. The last chapter deals with potential outlier or aberrant values and how to statistically determine if they should be removed from the sample data. Each statistical test presented includes an example problem with the resultant software output and how to interpret the results. Minimal time is spent on the mathematical calculations or theory. For those interested in the associated equations, supplemental figures are presented for each test with respective formulas. In addition, Appendix D presents the equations and proof for every output result for the various examples. Examples and results from the appropriate statistical results are displayed using Minitab 18O. In addition to the results, the required steps to analyze data using Minitab are presented with the examples for those having access to this software. Numerous other software packages are available, including based data analysis with Excel.