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Drug Discovery Stories: From Bench to Bedside presents a collection of cases on the development of highly successful pharmaceuticals. It delves into the realm of drug discovery, exploring the structural biology and biological functions of the sought-after targets. The book covers the identification of promising compounds, their transformation from hits to leads through meticulous optimization, and the elucidation of how key compounds interact with the target (in essence, providing invaluable insights for drug design). Additionally, it covers essential information such as the pivotal biological and PK data of lead compounds, any noteworthy clinical results, and a comprehensive overview of other candidate compounds. The field of drug discovery and development has experienced rapid evolution, with numerous new drugs receiving approval each year. While several books have been published on this subject, there is a pressing need for a new book series that accurately reflects the current advancements in drug discovery. This book aims to not only cater to the drug discovery community but also engage other communities involved in chemical biology, synthetic chemistry, and pharmacology. - Analyzes the drug discovery stories of different blockbuster drugs - Includes the newly approved drugs - Covers key aspects related to the drug development of the drugs

Practical guide to navigate problems involved with promiscuous ligands and multi-target drug discovery, supported by case studies and real examples Polypharmacology covers the two-sided nature of polypharmacology: its relevance for adverse drug effects, as well as its benefit for certain therapeutic drug classes in effectively treating complex diseases like psychosis and cancer. The book provides practical guidelines and advice to help readers design drugs that have multiple targets while minimizing unwanted off-target effects, discusses important disease areas like viral infection, diabetes, and obesity that have advanced significantly in the last decade, and guides researchers in neighboring areas to polypharmacology. The book is divided into four parts. Part A covers the link between off-targets and adverse drug reactions, how to screen for off-target activity, and how to recognize and optimize compounds with a potential for off-target activity. Part B discusses disease areas which benefit from polypharmacological approaches. Part C highlights important approaches, such as compound design, data mining with web-based tools, and multi-target peptides. Part D provides case study coverage on topics like CDK4/6 inhibitors for cancer treatment, the potential of multi-target ligands for COVID, and protein degraders and PROTACs. Sample topics discussed in Polypharmacology include: Molecular properties and structural motifs in pharmacological promiscuity, covering lipophilicity, molecular weight, and other parametersKinase liabilities in early drug discovery, covering core kinases driving the cell division cycle and consequences of interference, and cell cycle checkpoints controlling cell divisionTreatment of major depressive disorder, covering tricyclic antidepressants, monoamine oxidase inhibitors, and selective serotonin and norepinephrine reuptake inhibitorsTrends in the field, such as novel antipsychotics, standardization of screening tools, and the SmartCube System®, as well as lessons from history Delivering the latest research developments in the field, Polypharmacology is an essential reference on the subject for medicinal chemists, pharmacologists, biochemists, computational chemists, and biologists, as well as pharmaceutical professionals involved in drug discovery programs.

This third edition of Medicinal Chemistry of Anticancer Drugs, provides an updated resource for students and researchers from the point of view of medicinal chemistry and drug design, focusing on the mechanism of action of antitumor drugs from the molecular level, and on the relationship between chemical structure and chemical and biochemical reactivity of antitumor agents. Antitumor chemotherapy is a very active field of research, and a huge amount of information on the topic is generated every year. This new edition includes updated sections on the hot topic of cancer immunotherapy, cancer polypharmacology, multitargeted cancer therapy, medicinal chemistry of cancer diagnosis, theranostic anticancer agents, and pre-mRNA processing in cancer. Although many books are available that deal with clinical aspects of cancer chemotherapy, this book provides a unique and valuable perspective from the point of view of medicinal chemistry and drug design. It will be useful to undergraduate and postgraduate students of medicinal chemistry, pharmacology, biological chemistry, pharmacy and other health sciences. Researchers and practitioners will find a comprehensive treatment of the topic and a large number of references to reviews and the primary literature. - Provides a resource that is organized consistently based on targets and mechanisms of action from a molecular point-of-view - Focuses on the relationship between chemical structure and chemical and biochemical reactivity of antitumor agents, providing a rationalization on the action of these type of drugs and the design of new active structures - Features a large number of color figures which give information in a clear-and-concise way - Includes extensive references to review articles and primary literature - Includes updated sections on the hot topic of cancer immunotherapy, cancer polypharmacology, multitargeted cancer therapy, medicinal chemistry of cancer diagnosis, theragnostic anticancer agents, and pre-mRNA processing in cancer

There is a growing interest in unmet needs for the development of a new discipline in drug discovery and in university education on polypharmacology. However, there has not been a book with the comprehensive compilation of basic knowledge and advanced methodology that is needed. This book aims to meet the needs making Polypharmacology a new sub-discipline of Pharmacology, not only being a hot area of pharmacological research and education but also a new paradigm for drug discovery. It contains the contents covering the entire scope of Polypharmacology including systemic in-depth exposition of basic knowledge, novel concepts, innovative technologies, and translational and clinical applications by showcasing state-of-the-art strategies and step-by-step instructions of cutting-edge methods. The contents of this book targets broad readerships including scientists in pharmacology research and drug development, and university teachers and graduates in medical school or school of pharmacy.

The gold-standard of pharmacology texts – completely updated to reflect the latest research and developments A Doody's Core Title for 2020! Goodman & Gilman's: The Pharmacological Basis of Therapeutics, Thirteenth Edition represents the pinnacle of authority and accuracy in describing the actions and uses of therapeutic agents in relation to physiology and pathophysiology. Goodman & Gilman's careful balance of basic science and clinical application has guided thousands of practitioners and students to a clear understanding of the drugs essential to preventing, diagnosing, and treating disease. The Thirteenth Edition includes more than 500 color illustrations, with many new figures emphasizing mechanisms of drug action. More than 30 new contributors have added to this edition, while the focus on basic principles is undiminished. This edition is enhanced by timely new content: •NEW chapters including Treatment of Pulmonary Arterial Hypertension, Immunity and Inflammation, Immunoglobulins and Vaccines, and Treatment of Viral Hepatitis •Expanded coverage of cardiovascular disease, with separate chapters on myocardial ischemia, hypertension, and heart failure •Increased emphasis on cellular signaling pathways involved in drug action •Summary tables at the end of each chapter that organize drugs discussed in that chapter into relevant categories and detail therapeutic usage, clinical pharmacology, and tips •Chapter Content Outlines at the beginning of each chapter •Abbreviation boxes in every chapter to easily identify the abbreviations appearing in that chapter More than a textbook, Goodman & Gilman's is a working template for the effective and rational prescribing of drugs in daily practice.