New Tools to Interrogate Endocannabinoid Signalling


Book Description

Legalization of cannabis extracts around the world has led to a resurgence of interest into research surrounding endocannabinoids (eCBs) and the endocannabinoid system. This system is formed of a complex array of receptors, metabolic enzymes and transporters that finely tune the manifold biological activities of eCBs and there is an urgent need for the development of selective drugs to dissect the contribution of eCBs to the aetiology of various diseases. New Tools to Interrogate Endocannabinoid Signalling comprehensively covers the innovative research into both natural and synthetic compounds that affect this pathway and taking a target-based approach, assesses their potential for therapeutic use. With contributions from global leaders in the field, this timely volume will be a valuable resource to pharmaceutical researchers and medicinal chemists working in natural products and endocannabinoid drug discovery in academia and industry.




Endocannabinoid Signaling


Book Description

This second edition provides new and updated chapters detailing all major elements of the ECB system. Chapters guide readers through identification of drug targets, electrophysiology, computational chemistry, and machine learning. Written in the successful Methods in Molecular Biology series format, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible protocols, and notes on troubleshooting and avoiding known pitfalls. Comprehensive and cutting-edge, Endocannabinoid Signaling: Methods and Protocols, Second Edition is a valuable resource for all researchers interested in learning more about this important and developing field.




Antiviral Discovery for Highly Pathogenic Emerging Viruses


Book Description

New antiviral drugs are urgently needed. Recent outbreaks caused by viruses with great epidemiological impact such as Zika, or extraordinary virulence such as Ebola, Nipah, Lassa, Crimean-Congo haemorrhagic fever highlight the current lack of clinically proven vaccines and treatments for these potentially catastrophic agents. Antiviral Discovery for Highly Pathogenic Emerging Viruses comprehensively outlines the state of the art in antiviral drug discovery including identification of targets, screening strategies and the current pipeline of antiviral candidates including regulatory issues. The book also addresses the challenges faced in proceeding from pre-clinical studies to animal models and clinical trials with these highly pathogenic agents. Ideal for drug discovery scientists and medicinal chemists with an interest in antiviral drug discovery and development, this book provides a complete overview of the latest progress in the field, recent advances and the challenges that remain in developing these highly pathogenic agents. Illustrated throughout with case studies this book is a valuable resource in this complex and multidisciplinary field.




Chemical Linkers in Antibody–Drug Conjugates (ADCs)


Book Description

The covalent conjugation of potent cytotoxic agents to monoclonal antibodies, known as antibody-drug conjugates (ADCs) is a powerful approach in the field of targeted treatment of cancer. Clearly, both monoclonal antibody and cytotoxic payload are crucial elements in determining the clinical value of an ADC and have receive ample attention. However, the structural element connecting the two –the chemical linker– also plays an essential role in mode-of-action, efficacy, pharmacokinetics and safety profile of an ADC, but is often underappreciated in considerations of ADC design. Chemical Linkers in Antibody–Drug Conjugates aims to shine a detailed light on the various key attributes of chemical linkers in ADCs, for drug-to-antibody ratio, for stability, for release mechanism of payload, for pharmacokinetics, for stability determination, and for efficacy and safety. Ideal for postgraduate students and active researchers in drug discovery and development, this book provides a comprehensive description of linkers used in ADCs (clinical and late preclinical), insight into key quality attributes of linkers for ADCs, and aids the reader in understanding the role of linker chemistry and designing new ADCs.




Drug Repurposing


Book Description

Drug repurposing is the development of existing drugs for new uses: given that 9 in 10 drugs that enter drug development are never marketed and therefore represent wasted effort, it is an attractive as well as inherently more efficient process. Three repurposed drugs can be brought to market for the same cost as one new chemical entity; and they can also be identified more quickly, an important benefit for patients whose diseases are progressing faster than therapeutic innovation. But repurposing also requires a fresh look at configuring pharmaceutical R&D, considering clinical, regulatory and patent issues much earlier than would otherwise be the case; a holistic gedanken experiment almost needs to be undertaken at the very start of any repurposing development. In addition to new ways of thinking, the discovery of repurposing opportunities can take advantage of artificial intelligence techniques to match the perfect new use for an existing drug. And while repurposing of medicines has been in the mind of every doctor since Hypocrates, modern clinical practice will simply have to adapt to new repurposing techniques in an age where the number of known diseases is increasing much faster than the healthcare dollars available.




Protein–Protein Interaction Regulators


Book Description

New genomic information has revealed the crucial role that protein-protein interactions (PPIs) play in regulating numerous cellular functions. Aberrant forms of these interactions are common in numerous diseases and thus PPIs have emerged as a vast class of critical drug targets. Despite the importance of PPIs in biology, it has been extremely challenging to convert targets into therapeutics and targeting PPIs had long been considered a very difficult task. However, over the past decade the field has advanced with increasing growth in the number of successful PPI regulators. Protein-Protein Interaction Regulators surveys the latest advances in the structural understanding of PPIs as well as recent developments in modulator discovery.




Phenotypic Drug Discovery


Book Description

Phenotypic drug discovery has been highlighted in the past decade as an important strategy in the discovery of novel medical entities. This book aims to equip researchers with a thought-provoking guide to the application and development of contemporary phenotypic drug discovery for clinical success.




The Medicinal Chemist's Guide to Solving ADMET Challenges


Book Description

The Medicinal Chemist’s Guide to Solving ADMET Challenges summarizes a series of design strategies and tactics that have been successfully employed across pharmaceutical and academic laboratories to solve common ADMET issues. These are exemplified with a curated collection of concrete examples displayed in a highly visual “table-of-contents” style format, allowing readers to rapidly identify the most promising approaches applicable to their own challenges. Each ADMET parameter is introduced in a concise yet comprehensive manner and includes background, relevance and screening strategies. Medicinal chemistry knowledge of how best to modify molecular structure to solve ADMET issues is challenging to retrieve from the literature, public databases and even corporate data warehouses. The Medicinal Chemist’s Guide to Solving ADMET Challenges addresses this gap by presenting state-of-the-art design strategies put together by a global group of experienced medicinal chemists and ADMET experts across academia and the pharmaceutical industry.




Epigenetic Drug Discovery


Book Description

Epigenetics is one of the fastest moving fields in drug discovery, with almost every large pharmaceutical company, and a substantial number of biotechnology companies, targeting epigenetic processes to treat diseases ranging from cancer to Huntington’s disease and from inflammation to sickle cell anaemia. This book aims to provide an overview of the key topics adopted in current epigenetic drug discovery programmes with a focus on major developments and new technologies. Importantly, the book incorporates case studies and outlines the key challenges and techniques employed to overcome them. The book is an ideal resource for researchers in both industry and academia with an interest in epigenetic and genetic factors involved in drug discovery, target ID and validation. The book is also an excellent introduction for postgraduates interested in the interface between epigenetics and pharmaceuticals.




From Bud to Brain: A Psychiatrist's View of Marijuana


Book Description

The trend toward liberalizing medical and recreational marijuana use is increasing the obligation on clinicians to provide useful information to the public. This book summarizes the science all healthcare professionals need to know in order to provide objective and relevant information to a variety of patients, from recreational and medicinal users to those who use regularly, and to adolescents and worried parents. The author brings two and a half decades of studying cannabinoid research, and over forty years' experience in psychiatric and addiction medicine practice, to shed light on the interaction between marijuana and the brain. Topics range from how marijuana produces pleasurable sensations, relaxation and novelty (the 'high'), to emerging medical uses, effects of regular use, addiction, and policy. Principles of motivational interviewing are outlined to help clinicians engage patients in meaningful, non-judgmental conversations about their experiences with marijuana. An invaluable guide for physicians, nurses, psychologists, therapists, and counsellors.