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Leading researchers, from the Novartis group that pioneered Gleevec/GlivecTM and around the world, comprehensively survey the state of the art in the drug discovery processes (bio- and chemoinformatics, structural biology, profiling, generation of resistance, etc.) aimed at generating PTK inhibitors for the treatment of various diseases, including cancer. Highlights include a discussion of the rationale and the progress made towards generating "selective" low molecular-weight kinase inhibitors; an analysis of the normal function, role in disease, and application of platelet-derived growth factor antagonists; and a summary of the factors involved in successful structure-based drug design. Additional chapters address the advantages and disadvantages of in vivo preclinical models for testing protein kinase inhibitors with antitumor activity and the utility of different methods in the drug discovery and development process for determining "on-target" vs "off-target" effects of kinase inhibitors.
This book presents state-of-the-art information on the molecules of cell signalling pathways that represent actual or future targets for cancer therapy. By giving an update of the most promising approaches in this rapidly evolving field, the book contributes to the translation of the recent advances in the knowledge of intracellular signalling into the generation of innovative biomolecules as specific tools to target the most promising tumour-specific candidates. The book begins logically with the molecules first encountered along the signalling pathways, the membrane receptors for growth factors (Part I). Next, Part II presents several examples of intracellular molecular targets that are situated one step beyond in the pathways, while Part III addresses the difficult task of tuning the delicate balance between cell death and survival. In Part IV, the reader is taken into the practical problems raised by the therapy of specific cancers (glioma, childhood leukaemia), and into an original strategy from the field of nuclear medicine with the potential to generate innovative molecular-targeted cancer therapies.
In this volume the entire focus is devoted to the macromolecule target specificity of DNA interactive developmental therapeutic agents of current interest. A brief introduction to DNA interactive anticancer agents is included for readers who may benefit from an overview surrounding the developments that have contributed to our general understanding of this field. The following nine chapters have been carefully chosen so that they describe topics which are at the forefront of development in DNA-targeted cancer chemotherapy. Issues that have been addressed include the mechanisms of selective DNA topoisomerase I and II poisoning by antitumor agents (Chapters 1 and 2), sequence-specific recognit...
Oligonucleotides diffuse poorly through biological barriers, including cell membranes. They are also rapidly degraded in vivo by nucleuses. Aiming to improve the administration of compounds, the book studies the development of nucleotide chemistry.
With its focus on drugs so recently introduced that they have yet to be found in any other textbooks or general references, the information and insight found here makes this a genuinely unique handbook and reference. Following the successful approach of the previous volumes in the series, inventors and primary developers of successful drugs from both industry and academia tell the story of the drug's discovery and describe the sometimes twisted route from the first drug candidate molecule to the final marketed drug. The 11 case studies selected describe recent drugs ranging across many therapeutic fields and provide a representative cross-section of present-day drug developments. Backed by plenty of data and chemical information, the insight and experience of today's top drug creators makes this one of the most useful training manuals that a junior medicinal chemist may hope to find. The International Union of Pure and Applied Chemistry has endorsed and sponsored this project because of its high educational merit.
The aims of this volume are to highlight the tremendous pharmacological potential of protein kinase and protein phosphatase inhibitors, to provide a thorough overview of the most remarkable achievements in the field and to illustrate how beneficial these studies can be for the advancement of both basic knowledge on biological regulation and deregulation and for the clinical treatment of a wide spectrum of diseases. This goal is attained by contributions of leader investigators in the field, who address the issue from different angles.
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.
This new volume of Methods in Enzymology continues the legacy of this premier serial with quality chapters authored by leaders in the field. This volume covers protein kinase inhibitors in research and medicine, and includes chapters on such topics as fragment-based screening, broad kinome profiling of kinase inhibitors, and designing drug-resistant kinase alleles. - Continues the legacy of this premier serial with quality chapters authored by leaders in the field - Covers research methods in biomineralization science - Contains sections focusing on protein kinase inhibitors in research and medicine
Highly Commended, BMA Medical Book Awards 2014 Chronic myeloid leukemia is a clonal disease that results from an acquired genetic change in a single pluripotential hemopoietic stem cell. Efforts to confront this disease have been assisted by advances in cellular and molecular biology and the speed at which these findings have transformed the therapeutic algorithm. Nevertheless, there is some uncertainty with regards to how best to assess efficacy of treatment, especially with regards to the most appropriate surrogate markers for overall survival. From the standpoint of biology and clinical management, this handbook provides an authoritative state-of-the-art review of current and developing progress.
The AACR Annual Meeting highlights the best cancer science and medicine from institutions all over the world. Attendees are invited to stretch their boundaries, form collaborations, attend sessions outside their own areas of expertise, and learn how to apply exciting new concepts, tools, and techniques to their own research. Part A contains abstracts 1-3062 accepted for the 2017 meeting.