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Cancer drug development is currently undergoing a profound shift. Drugs targeting fundamental cellular processes such DNA-replication and microtubule function, often referred to as “chemotherapy” and still the backbone of most cancer treatment regimens, are increasingly being complemented by or replaced with kinase inhibitors. This new class of drugs targets enzymes which provide growth and survival signals to cancer cells by transferring phosphate groups from Adenosine-5'-triphosphate (ATP) to other proteins, lipids, nucleotides, and carbohydrates.

 

This book summarizes the current state of kinase inhibitor therapy for cancer. Successful drug development relies on the expertise and dedication of many experts. To reflect this team approach to finding new kinase inhibitors and defining their optimal use for cancer treatment, the editors invited experts in academia and pharmaceutical industry to share their insights into various aspects of this process, ranging from the first chemical screens, to preclinical testing and disease-focused clinical drug development. The editors hope these lessons will be instructive for the novice as well as the expert.

TABLE OF CONTENTS

Preface.- Fundamentals.- Setting up a Kinase Discovery and Development Project.-Drug Efficacy Testing in Mice.- Kinase Targets and Disease.- Gastrointestinal Stromal Tumors (GISTS).-EGFR-Mutant Lung Cancer.- Targeting Oncogenic BRAF in Human Cancer.- Beyond BRAF in Melanoma.- JAK-mutant Myeloproliferative Neoplasms.- Will Kinase Inhibitors Make It as Glioblastoma Drugs?.- Perspectives.- Predictive Genomic Biomarkers.- Epigenetic Biomarkers.- Adjuvant Trials of Targeted Agents: The Newest Battleground in the War on Cancer.- Subject Index