Download or read book RAS Drug Discovery written by Adrian Gill and published by Elsevier. This book was released on 2024-10-01 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: KRAS Drug Discovery: Past, Present and Future is a comprehensive overview of the state-of-the-art medicinal chemistry approaches towards targeting the formerly undruggable oncogene, KRAS. It includes Seminal medicinal chemistry case histories of KRASG12C inhibitors such as Sotorosib, the first approved KRASG12C inhibitor for NSCLC, alongside the latest advances towards identification of in vivo tools and development candidates targeting KRAS G12D, KRAS G13C and other mutations. The book also provides the reader with a comprehensive overview of the in vitro assay systems, in vivo pharmacology xenograft models and chemical biology tools available to characterize small molecule inhibitors of KRAS.

Download or read book RAS Past Present and Future written by and published by Academic Press. This book was released on 2022-01-29 with total page 358 pages. Available in PDF, EPUB and Kindle. Book excerpt: Advances in Cancer Research, volume 153 provides a timely review of the biology, biochemistry, and current approaches to therapeutically target the RAS oncoprotein, the most frequently mutated oncogene family in human cancers. 2021 saw the approval of the first direct RAS inhibitor (sotorasib) for use in treating non-small cell lung cancers harboring KRAS(G12C) mutations. The successful approval and use of this drug highlights that the once “undruggable RAS is indeed pharmacologically tractable. This volume provides an overview of efforts to develop additional approaches to therapeutically target oncogenic RAS. In addition, the reader will find excellent reviews on the history and research efforts to understand the biochemistry and oncogenic activity of RAS in human cancers. Overview of the history and development of efforts to pharmacologically inhibit RAS. Discussion of the biochemistry and biology of different RAS mutant proteins and how this might be effectively leveraged in the development of anti-RAS therapies. Up-to-date reviews of the cutting-edge approaches to develop new anti-RAS pharmacologics.

Download or read book Conquering RAS written by Asfar Azmi and published by Academic Press. This book was released on 2016-08-11 with total page 296 pages. Available in PDF, EPUB and Kindle. Book excerpt: Conquering RAS: From Biology to Cancer Therapy provides introductory knowledge on how modern RAS biology is taking shape in light of newer technological development. Each chapter is written in a manner that emphasizes simplicity and readability for both new investigators and established researchers. While RAS biology has been intensively studied for more than three decades, we are yet to see any effective therapeutics that could interfere in the signaling cascade regulated by this master oncogene. The book covers topics ranging from basic RAS biology, to translational biology and drug discovery applications. These topics will be appealing to basic researchers working in labs who seek deeper understanding of the modern concepts in RAS research. On the other side, the oncologist at the patient’s bedside will find the book useful as they routinely face the daunting task of treating patients that predominantly have a disease driven by oncogenic KRAS. Brings together wide ranging topics in RAS basic and translational biology for the scientific and clinical communities Showcases recent advancements in RAS research under one comprehensive volume Includes video clips, color illustrations, and important website links to facilitate a clear understanding of RAS in cancer research

Download or read book Human Drug Targets written by Edward D. Zanders and published by John Wiley & Sons. This book was released on 2015-12-14 with total page 456 pages. Available in PDF, EPUB and Kindle. Book excerpt: The identification of drug targets in a given disease has been central to pharmaceutical research from the latter half of the 20th century right up to the modern genomics era. Human Drug Targets provides an essential guide to one of the most important aspects of drug discovery – the identification of suitable protein and RNA targets prior to the creation of drug development candidates. The first part of the book consists of introductory chapters that provide the background to drug target discovery and highlight the way in which these targets have been organised into online databases. It also includes a user’s guide to the list of entries that forms the bulk of the book. Since this is not designed to be a compendium of drugs, the emphasis will be on the known (or speculated) biological role of the targets and not on the issues associated with pharmaceutical development. The objective is to provide just enough information to be informative and prompt further searches, while keeping the amount of text for each of the many entries to a minimum. Human Drug Targets will prove invaluable to those drug discovery professionals, in both industry and academia, who need to make some sense of the bewildering array of online information sources on current and potential human drug targets. As well as creating order out of a complex target landscape, the book will act as an ideas generator for potentially novel targets that might form the basis of future discovery projects.

Download or read book RAS Family GTPases written by Channing Der and published by Springer Science & Business Media. This book was released on 2007-04-29 with total page 403 pages. Available in PDF, EPUB and Kindle. Book excerpt: Since 1982, Ras proteins have been the subject of intense research investigation by the biomedical research community. The wide interest in Ras has been stimulated for three key reasons. This book features chapters contributed by leading investigators in the field that highlight the current state-of-the art in Ras biochemistry, structure and biology. This book is an excellent reference for students in the biomedical sciences and for investigators in the field.

Download or read book Tumor Organoids written by Shay Soker and published by Humana Press. This book was released on 2017-10-20 with total page 225 pages. Available in PDF, EPUB and Kindle. Book excerpt: Cancer cell biology research in general, and anti-cancer drug development specifically, still relies on standard cell culture techniques that place the cells in an unnatural environment. As a consequence, growing tumor cells in plastic dishes places a selective pressure that substantially alters their original molecular and phenotypic properties.The emerging field of regenerative medicine has developed bioengineered tissue platforms that can better mimic the structure and cellular heterogeneity of in vivo tissue, and are suitable for tumor bioengineering research. Microengineering technologies have resulted in advanced methods for creating and culturing 3-D human tissue. By encapsulating the respective cell type or combining several cell types to form tissues, these model organs can be viable for longer periods of time and are cultured to develop functional properties similar to native tissues. This approach recapitulates the dynamic role of cell–cell, cell–ECM, and mechanical interactions inside the tumor. Further incorporation of cells representative of the tumor stroma, such as endothelial cells (EC) and tumor fibroblasts, can mimic the in vivo tumor microenvironment. Collectively, bioengineered tumors create an important resource for the in vitro study of tumor growth in 3D including tumor biomechanics and the effects of anti-cancer drugs on 3D tumor tissue. These technologies have the potential to overcome current limitations to genetic and histological tumor classification and development of personalized therapies.

Download or read book The Quest for the Cure written by Brent R. Stockwell and published by Columbia University Press. This book was released on 2011-06-01 with total page 289 pages. Available in PDF, EPUB and Kindle. Book excerpt: After more than fifty years of blockbuster drug development, skeptics are beginning to fear we are reaching the end of drug discovery to combat major diseases. In this engaging book, Brent R. Stockwell, a leading researcher in the exciting new science of chemical biology, describes this dilemma and the powerful techniques that may bring drug research into the twenty-first century. Filled with absorbing stories of breakthroughs, this book begins with the scientific achievements of the twentieth century that led to today's drug innovations. We learn how the invention of mustard gas in World War I led to early anti-cancer agents and how the efforts to decode the human genome might lead to new approaches in drug design. Stockwell then turns to the seemingly incurable diseases we face today, such as Alzheimer's, many cancers, and others with no truly effective medicines, and details the cellular and molecular barriers thwarting scientists equipped with only the tools of traditional pharmaceutical research. Scientists such as Stockwell are now developing methods to combat these complexities technologies for constructing and testing millions of drug candidates, sophisticated computational modeling, and entirely new classes of drug molecules all with an eye toward solving the most profound mysteries of living systems and finding cures for intractable diseases. If successful, these methods will unlock a vast terrain of untapped drug targets that could lead to a bounty of breakthrough medicines. Offering a rare, behind-the-scenes look at this cutting-edge research, The Quest for the Cure tells a thrilling story of science, persistence, and the quest to develop a new generation of cures.

Download or read book Kinase Drug Discovery written by Richard A. Ward and published by Royal Society of Chemistry. This book was released on 2012 with total page 333 pages. Available in PDF, EPUB and Kindle. Book excerpt: Kinase drug discovery remains an area of significant interest across academia and in the pharmaceutical industry. There are now around 13 FDA approved small molecule drugs which target kinases and many more compounds in various stages of clinical development. Although there have been a number of reviews/publications on kinase research, this book fills a gap in the literature by considering the current and future opportunities and challenges in targeting this important family of enzymes. The book is forward-looking and identifies a number of hot topics and key areas for kinase drug discovery over the coming years. It includes contributions from highly respected authors with a combined experience in the industry of well over 200 years, which has resulted in a book of great interest to the kinase field and across drug discovery more generally. Readers will gain a real insight into the huge challenges and opportunities which this target class has presented drug discovery scientists. The many chapters cover a wide breadth of topics, are well written and include high quality colour and black and white images. Topics covered include an outline of how medicinal chemistry has been able to specifically exploit this unique target class, along with reflections on the mechanisms of kinases inhibitors. Also covered is resistance to kinase inhibitors caused by amino acid mutations, case studies of kinase programs and reviews areas beyond protein kinases and beyond the human kinome. Also described are modern approaches to finding kinase leads and the book finishes with a reflection of how kinase drug discovery may progress over the coming years.

Download or read book Structural Biology in Drug Discovery written by Jean-Paul Renaud and published by John Wiley & Sons. This book was released on 2020-01-09 with total page 1367 pages. Available in PDF, EPUB and Kindle. Book excerpt: With the most comprehensive and up-to-date overview of structure-based drug discovery covering both experimental and computational approaches, Structural Biology in Drug Discovery: Methods, Techniques, and Practices describes principles, methods, applications, and emerging paradigms of structural biology as a tool for more efficient drug development. Coverage includes successful examples, academic and industry insights, novel concepts, and advances in a rapidly evolving field. The combined chapters, by authors writing from the frontlines of structural biology and drug discovery, give readers a valuable reference and resource that: Presents the benefits, limitations, and potentiality of major techniques in the field such as X-ray crystallography, NMR, neutron crystallography, cryo-EM, mass spectrometry and other biophysical techniques, and computational structural biology Includes detailed chapters on druggability, allostery, complementary use of thermodynamic and kinetic information, and powerful approaches such as structural chemogenomics and fragment-based drug design Emphasizes the need for the in-depth biophysical characterization of protein targets as well as of therapeutic proteins, and for a thorough quality assessment of experimental structures Illustrates advances in the field of established therapeutic targets like kinases, serine proteinases, GPCRs, and epigenetic proteins, and of more challenging ones like protein-protein interactions and intrinsically disordered proteins

Download or read book Complete Accounts of Integrated Drug Discovery and Development written by Ahmed F. Abdel-Magid and published by ACS Symposium. This book was released on 2019 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: The chapters in this book are written to accentuate the interdependency and synergy between drug discovery and process development disciplines to advance a new chemical entity into clinical trials and eventually to the market. Due to the success of our previous books (Comprehensive Accounts of Pharmaceutical Research and Development: From Discovery to Late-Stage Process Development, Volumes 1 and 2), the editors sought to further arm experienced modern synthetic organic chemists, and budding researchers perhaps still in universities with real world examples from the pharmaceutical industry. In addition, the chapters contain citations of a large number of valuable selected references to the primary literature. The book highlights the tireless efforts of Discovery and Process Chemists, and their roles in the advancement of drug discovery and development. The editors were motivated to create this book by our appreciation of the value of chemical research by both Discovery and Process Chemists in producing new pharmaceutical entities. Their combined efforts make it possible to introduce novel and effective drugs into the market to treat hundreds of millions of patients and alleviate their suffering, improve their quality of life and possibly save their lives from diseases and disorders. The chapters presented in this book are written by a selected group of outstanding, highly accomplished Medicinal and Process Chemists with noted experiences and diverse backgrounds representing some of the top pharmaceutical companies. The chapters highlight examples of emerging concepts, new developments and challenges arising in the discovery of new drug candidates and the development of new practical synthetic chemistry processes to produce these drug candidates on large scale. The story leading up to the discovery of each drug or drug candidate is presented by the Discovery Chemist(s), and then the Process Chemist(s) describe the development of the same drug to give the reader a complete story of drug discovery and development. The reader will experience a rare and unique opportunity to obtain the complete perspectives of Discovery and Process Chemistry in a single book. While most of these topics have appeared in the primary literature where space is critical and brevity valued, the book permits the editors and contributors to tell the complete tales as stories, from start to finish or to the current state of the drug development.

Download or read book Fragment based Drug Discovery written by Daniel A. Erlanson and published by John Wiley & Sons. This book was released on 2015-12-02 with total page 524 pages. Available in PDF, EPUB and Kindle. Book excerpt: From its origins as a niche technique more than 15 years ago, fragment-based approaches have become a major tool for drug and ligand discovery, often yielding results where other methods have failed. Written by the pioneers in the field, this book provides a comprehensive overview of current methods and applications of fragment-based discovery, as well as an outlook on where the field is headed. The first part discusses basic considerations of when to use fragment-based methods, how to select targets, and how to build libraries in the chemical fragment space. The second part describes established, novel and emerging methods for fragment screening, including empirical as well as computational approaches. Special cases of fragment-based screening, e. g. for complex target systems and for covalent inhibitors are also discussed. The third part presents several case studies from recent and on-going drug discovery projects for a variety of target classes, from kinases and phosphatases to targeting protein-protein interaction and epigenetic targets.

Download or read book Protein NMR Spectroscopy written by John Cavanagh and published by Elsevier. This book was released on 2010-07-21 with total page 915 pages. Available in PDF, EPUB and Kindle. Book excerpt: Protein NMR Spectroscopy, Second Edition combines a comprehensive theoretical treatment of NMR spectroscopy with an extensive exposition of the experimental techniques applicable to proteins and other biological macromolecules in solution. Beginning with simple theoretical models and experimental techniques, the book develops the complete repertoire of theoretical principles and experimental techniques necessary for understanding and implementing the most sophisticated NMR experiments. Important new techniques and applications of NMR spectroscopy have emerged since the first edition of this extremely successful book was published in 1996. This updated version includes new sections describing measurement and use of residual dipolar coupling constants for structure determination, TROSY and deuterium labeling for application to large macromolecules, and experimental techniques for characterizing conformational dynamics. In addition, the treatments of instrumentation and signal acquisition, field gradients, multidimensional spectroscopy, and structure calculation are updated and enhanced. The book is written as a graduate-level textbook and will be of interest to biochemists, chemists, biophysicists, and structural biologists who utilize NMR spectroscopy or wish to understand the latest developments in this field. Provides an understanding of the theoretical principles important for biological NMR spectroscopy Demonstrates how to implement, optimize and troubleshoot modern multi-dimensional NMR experiments Allows for the capability of designing effective experimental protocols for investigations of protein structures and dynamics Includes a comprehensive set of example NMR spectra of ubiquitin provides a reference for validation of experimental methods

Download or read book Genomics in Drug Discovery and Development written by Dimitri Semizarov and published by John Wiley & Sons. This book was released on 2008-11-03 with total page 496 pages. Available in PDF, EPUB and Kindle. Book excerpt: Early characterization of toxicity and efficacy would significantly impact the overall productivity of pharmaceutical R&D and reduce drug candidate attrition and failure. By describing the available platforms and weighing their relative advantages and disadvantages, including microarray data analysis, Genomics in Drug Discovery and Development introduces readers to the biomarker, pharmacogenomic, and toxicogenomics toolbox. The authors provide a valuable resource for pharmaceutical discovery scientists, preclinical drug safety department personnel, regulatory personnel, discovery toxicologists, and safety scientists, drug development professionals, and pharmaceutical scientists.

Download or read book Fragment based Drug Discovery written by Daniel A. Erlanson and published by John Wiley & Sons. This book was released on 2016-02-23 with total page 524 pages. Available in PDF, EPUB and Kindle. Book excerpt: From its origins as a niche technique more than 15 years ago, fragment-based approaches have become a major tool for drug and ligand discovery, often yielding results where other methods have failed. Written by the pioneers in the field, this book provides a comprehensive overview of current methods and applications of fragment-based discovery, as well as an outlook on where the field is headed. The first part discusses basic considerations of when to use fragment-based methods, how to select targets, and how to build libraries in the chemical fragment space. The second part describes established, novel and emerging methods for fragment screening, including empirical as well as computational approaches. Special cases of fragment-based screening, e. g. for complex target systems and for covalent inhibitors are also discussed. The third part presents several case studies from recent and on-going drug discovery projects for a variety of target classes, from kinases and phosphatases to targeting protein-protein interaction and epigenetic targets.

Download or read book Animal Models in Cancer Drug Discovery written by Asfar Azmi and published by Academic Press. This book was released on 2019-04-16 with total page 470 pages. Available in PDF, EPUB and Kindle. Book excerpt: Animal Models in Cancer Drug Discovery brings forward the most cutting-edge developments in tumor model systems for translational cancer research. The reader can find under this one volume virtually all types of existing and emerging tumor models in use by the research community. This book provides a deeper insight on how these newer models could de-risk modern drug discovery. Areas covered include up to date information on latest organoid derived models and newer genetic models. Additionally, the book discusses humanized animal tumor models for cancer immunotherapy and how they leverage personalized therapies. The chapter on larger animal, canine models and their use in and their use in pre-investigational new drug (pre-IND) development makes the volume unique. Unlike before, the incorporation of several simplified protocols, breeding methodologies, handling and assessment procedures to study drug intervention makes this book a must read. Animal Models in Cancer Drug Discovery is a valuable resource for basic and translational cancer researchers, drug discovery researchers, contract research organizations, and knowledge seekers at all levels in the biomedical field. Encompasses discussions on innovative animal models, xenograft, genetic models, primary models, organoid systems, humanized and other models in modern biology paradigms that are enhancing research in the field of drug discover Covers the use of these models in personalized medicine, immunotherapy, toxicology, pre-IND assessments and related drug development arenas Presents protocols, procedures, and a comprehensive glossary to help new readers understand technical terms and specialized nomenclature

Download or read book Innovations and Implementations of Computer Aided Drug Discovery Strategies in Rational Drug Design written by Sanjeev Kumar Singh and published by Springer Nature. This book was released on 2021-02-02 with total page 334 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book presents various computer-aided drug discovery methods for the design and development of ligand and structure-based drug molecules. A wide variety of computational approaches are now being used in various stages of drug discovery and development, as well as in clinical studies. Yet, despite the rapid advances in computer software and hardware, combined with the exponential growth in the available biological information, there are many challenges that still need to be addressed, as this book shows. In turn, it shares valuable insights into receptor-ligand interactions in connection with various biological functions and human diseases. The book discusses a wide range of phylogenetic methods and highlights the applications of Molecular Dynamics Simulation in the drug discovery process. It also explores the application of quantum mechanics in order to provide better accuracy when calculating protein-ligand binding interactions and predicting binding affinities. In closing, the book provides illustrative descriptions of major challenges associated with computer-aided drug discovery for the development of therapeutic drugs. Given its scope, it offers a valuable asset for life sciences researchers, medicinal chemists and bioinformaticians looking for the latest information on computer-aided methodologies for drug development, together with their applications in drug discovery.

Download or read book Drug Discovery in Pancreatic Cancer written by Haiyong Han and published by Springer Science & Business Media. This book was released on 2010-03-11 with total page 307 pages. Available in PDF, EPUB and Kindle. Book excerpt: Pancreatic cancer is the fourth leading cause of cancer death in the United States. Every year, about 33,700 people in the United States will be diagnosed with pancreatic cancer and over 32,000 patients will die from the disease. The median survival of patients with advanced pancreatic cancer is about 6-months. This dismal picture of pancreatic cancer is mainly due to the lack of early diagnosis and effective treatment for patients with advanced disease. To increase the survival rate of pancreatic cancer patients, better tumor markers for diagnosis and new molecular targets for drug development are desperately needed. A lot of effort has been made in searching for pancreatic cancer-causing genes or genes associated with progression of malignant behavior in pancreatic cancer. As a result, alterations in the expression of several cancer-related genes have been identified in pancreatic tumors. The identification and characterization of these cancer-related genes have significantly increased our understanding of pancreatic cancer development, but unfortunately the treatment of pancreatic cancer has not advanced as much in the past 20 years. Over the past decade, tremendous advances have been made in the field of cancer drug discovery, particularly, in the area of molecular and genetic models and technologies. Many of those advanced models and technologies have been applied to the drug discovery processes for pancreatic cancer. In this book, a team of experts will describe the latest development in the application of these models and technologies in pancreatic cancer. The authors include basic researchers as well as clinicians who work in the front-line of the war against pancreatic cancer and have the first-hand experience on these cutting-edge tools and techniques. The book can be divided into two general areas: 1) model systems and 2) genomics and proteomics tools. In recent years there have been a lot of advances in the model systems for pancreatic cancer, including the further characterization of normal and cancerous pancreatic cell lines, the establishment of transgenic mouse models that recapitulate the initiation and progression of human pancreatic cancer, the development of a new xenograft model system for the evaluation of novel agents, and the establishment of a zebrafish pancreatic cancer model. The first four chapters of the book will be devoted to these models. The advances in genomics and proteomics research have made a major impact in cancer drug discovery. A number of these –omics-based tools and techniques have been applied in the pancreatic cancer drug discovery. Chapters 5-9 of the book will discuss techniques for genome-wide examination of gene expression, copy number, methylation, function and regulation. Chapters 10-11 will discuss in situ techniques for studying chromosomal and gene copy number abnormalities as well protein expression changes in cancer samples. Chapters 12-14 will focus on techniques for global examination of protein expression levels in biospecimens obtained from pancreatic cancer patients. Cancer drug discovery has become more and more target-centric.