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Optimization in Drug Discovery
Recent analyses of drug attrition rates reveal that a significant number of drug candidates fail in the later stage of clinical development owing to absorption, distribution, metabolism, elimination (ADME), and toxicity issues. Lead optimization in drug discovery, a process attempting to uncover and correct these defects of drug candidates, is highly beneficial in lowering the cost and time to develop therapeutic drugs by reducing drug candidate failures in development. At present, parallel synthesis combining with high-throughput screening has made it easier to generate highly potent compounds (i. e. , hits). However, to be a potential drug, a hit must have drug-like characteristics in addi...
Frontiers in Drug Design and Discovery
"Frontiers in Drug Design and Discovery" is an Ebook series devoted to publishing the latest and the most important advances in drug design and discovery. Eminent scientists write contributions on all areas of rational drug design and drug discovery inclu
Optimization in Drug Discovery
Thoroughly revised and updated, Optimization in Drug Discovery: In Vitro Methods, Second Edition presents a wide spectrum of in vitro assays including formulation, plasma binding, absorption and permeability, cytochrome P450 (CYP) and UDP-glucuronosyltransferases (UGT) metabolism, CYP inhibition and induction, drug transporters, drug-drug interactions via assessment of reactive metabolites, genotoxicity, and chemical and photo-mutagenicity assays. Written for the Methods in Pharmacology and Toxicology series, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible protocols, and tips on troubleshooting and avoiding known pitfalls. Expert authors have developed and utilized these in vitro assays to achieve drug-like characteristics in addition to efficacy properties and good safety profiles of drug candidates. Comprehensive and up-to-date, Optimization in Drug Discovery: In Vitro Methods, Second Edition aims to guide researchers down the difficult path to successful drug discovery and development.
Cytochrome P450
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2015: Which new directions for Alzheimer's disease?
According to the World Health Organization, more than 40 million people in the world are affected with dementia. To date, 60-70% of the cases of dementia are attributed to the Alzheimer's disease (AD). This neurodegenerative disorder gradually takes place over a period of at least 20 years before the onset of symptoms, which are impaired memory, apathy and depression. The characteristics of AD consist in neurofibrillary tangles (intraneuronal aggregates of hyperphosphorylated tau proteins) and senile plaques (dense extraneuronal deposits composed of amyloid ß (Aß)). The other features linked to these two core pathological hallmarks of AD are inflammation, oxidative stress, progressive syna...
Biomarker Methods in Drug Discovery and Development
In this book, expert researchers provide a tool box for those who have a general interest in biomarker research and for those currently specializing in certain technologies but desiring an understanding of other available methodologies. Its chapters include validated, mature methods as well as new, incredibly promising protocols. This book is the perfect biomarker technical guideline and reference to stimulate more exciting biomarker research and technology development.
Discovery DMPK Quick Guide
This book is intended for a broad readership, in particular, those working or interested in drug discovery coming from various disciplines such as medicinal chemistry, pharmacology, drug metabolism and pharmacokinetics, bioanalysis, clinical sciences, biochemistry, pharmaceutics, and toxicology. It provides, for the first time, a completely integrated look at multiple aspects of ADME sciences (absorption, distribution, metabolism, and excretion) in a summary format that is clear, concise, and self-explanatory. DMPK in Drug Discovery - Guide to Data Interpretation and integration leverages the prior knowledge from the first book that covers the basics of each concept (Drug Metabolism and Pharmacokinetics Quick Guide). This reference book is meant to be used day to day and provides many useful tables (used for data interpretation), figures, and case studies that can facilitate drug discovery. The case studies are intended to be short and relevant to the topic discussed and present another dimension to the discussions.
Directory of Graduate Research
Faculties, publications and doctoral theses in departments or divisions of chemistry, chemical engineering, biochemistry and pharmaceutical and/or medicinal chemistry at universities in the United States and Canada.
