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This timely guide to kinase inhibitor drug development is the first to cover the entire drug pipeline, from target identification to compound development and clinical application. Edited by the pioneers in the field, on the drug development side this ready reference discusses classical medicinal chemistry approaches as well as current chemical genomics strategies. On the clinical side, both current and future therapeutic application areas for kinase inhibitor drugs are addressed, with a strong focus on oncology drugs. Backed by recent clinical experience with first-generation drugs in the battle against various forms of cancer, this is crucial reading for medicinal, pharmaceutical and biochemists, molecular biologists, and oncologists, as well as those working in the pharmaceutical industry.
One of the major shortcomings of the current drug discovery and development process is the inability to bridge the gap between early stage discoveries and pre-clinical research in order to advance innovations beyond the discovery phase. This book examines a drug discovery and development model, where the respective expertise of academia and industry are brought together to take promising discoveries through to proof of concept, providing a means to de-risk the drug discovery and development process.
The proceedings set LNCS 11727, 11728, 11729, 11730, and 11731 constitute the proceedings of the 28th International Conference on Artificial Neural Networks, ICANN 2019, held in Munich, Germany, in September 2019. The total of 277 full papers and 43 short papers presented in these proceedings was carefully reviewed and selected from 494 submissions. They were organized in 5 volumes focusing on theoretical neural computation; deep learning; image processing; text and time series; and workshop and special sessions.
Chemogenomics brings together the most powerful concepts in modern chemistry and biology, linking combinatorial chemistry with genomics and proteomics. This first reference devoted to the topic covers all stages of the early drug discovery process, from target selection to compound library and lead design. With the combined expertise of 20 research groups from academia and leading pharmaceutical companies, this is a must-have for every drug developer and medicinal chemist applying the powerful methods of chemogenomics to speed up the drug discovery process.
The AACR Annual Meeting is a must-attend event for cancer researchers and the broader cancer community. This year's theme, "Delivering Cures Through Cancer Science," reinforces the inextricable link between research and advances in patient care. The theme will be evident throughout the meeting as the latest, most exciting discoveries are presented in every area of cancer research. There will be a number of presentations that include exciting new data from cutting-edge clinical trials as well as companion presentations that spotlight the science behind the trials and implications for delivering improved care to patients. This book contains abstracts 1-2696 presented on April 17-18, 2016, at the AACR Annual Meeting.
The AACR Annual Meeting is a must-attend event for cancer researchers and the broader cancer community. This year's theme, "Delivering Cures Through Cancer Science," reinforces the inextricable link between research and advances in patient care. The theme will be evident throughout the meeting as the latest, most exciting discoveries are presented in every area of cancer research. There will be a number of presentations that include exciting new data from cutting-edge clinical trials as well as companion presentations that spotlight the science behind the trials and implications for delivering improved care to patients. This book contains abstracts 2697-5293 presented on April 19-20, 2016, at the AACR Annual Meeting.
Tailored to the needs of medicinal and natural products chemists, the second edition of this unique handbook brings the contents up to speed, almost doubling the amount of chemical information with an additional volume. As in the predecessor, a short introductory section covers the theoretical background and evaluates currently available instrumentation and equipment. The main part of the book then goes on to systematically survey the complete range of published microwave-assisted synthesis methods from their beginnings in the 1990s to mid-2011, drawing on data from more than 5,000 reports and publications. Throughout, the focus is on those reactions, reagents and reaction conditions that work, and that are the most relevant for medicinal and natural products chemistry. A much expanded section is devoted to combinatorial, highthroughput and flow chemistry methods.
Innovative and forward-looking, this volume focuses on recent achievements in this rapidly progressing field and looks at future potential for development. The first part provides a basic understanding of the factors governing protein-ligand interactions, followed by a comparison of key experimental methods (calorimetry, surface plasmon resonance, NMR) used in generating interaction data. The second half of the book is devoted to insilico methods of modeling and predicting molecular recognition and binding, ranging from first principles-based to approximate ones. Here, as elsewhere in the book, emphasis is placed on novel approaches and recent improvements to established methods. The final part looks at unresolved challenges, and the strategies to address them. With the content relevant for all drug classes and therapeutic fields, this is an inspiring and often-consulted guide to the complexity of protein-ligand interaction modeling and analysis for both novices and experts.
In this new edition of a bestseller, all the contents have been brought upto-date by addressing current standards and best practices in the assessment and prediction of ADMET properties. Although the previous chapter layout has been retained, substantial revisions have been made, with new topics such as pro-drugs, active metabolites and transporters covered in detail in a manner useful to the Drug Discovery scientist. The authors discuss the parameters and processes important for the absorption, distribution and retention of drug compounds in the body, plus the potential problems created by their transformation into toxic byproducts. While aimed at all those dealing professionally with the development and application of pharmaceutical substances, the readily comprehensible style makes this book equally suitable for students of pharmacy and related subjects. Uniquely comprehensive, the book relates physicochemistry and chemical structure to pharmacokinetic properties and ultimately drug efficacy and safety.
Written with the practicing medicinal chemist in mind, this is the first modern handbook to systematically address the topic of bioisosterism. As such, it provides a ready reference on the principles and methods of bioisosteric replacement as a key tool in preclinical drug development. The first part provides an overview of bioisosterism, classical bioisosteres and typical molecular interactions that need to be considered, while the second part describes a number of molecular databases as sources of bioisosteric identification and rationalization. The third part covers the four key methodologies for bioisostere identification and replacement: physicochemical properties, topology, shape, and overlays of protein-ligand crystal structures. In the final part, several real-world examples of bioisosterism in drug discovery projects are discussed. With its detailed descriptions of databases, methods and real-life case studies, this is tailor-made for busy industrial researchers with little time for reading, while remaining easily accessible to novice drug developers due to its systematic structure and introductory section.