Molecular Cancer Therapeutics: Strategies for Drug Discovery and Development
Molecular Cancer Therapeutics covers state-of-the-art strategies to identify and develop cancer drug target molecules and lead inhibitors for clinical testing. It provides a thorough treatment of drug target discovery, validation, and development. The introductory chapters provide an overview of pathways to discovery and development of molecular cancer therapeutics. Subsequent chapters progress from initial stages of drug target discovery to drug discovery, development, and testing in preclinical and clinical models. Topics include drug lead screening, drug-to-lead development, proof-of-concept studies, medicinal chemistry issues, intellectual property concerns, and clinical development.
This invaluable reference promotes understanding of steps involved in developing drug leads for industrial partnering and development. It provides an overview of the strategies for discovery and validation of drug target molecules, and discusses cell- and molecule-based drug screening strategies, as well as mouse models for cancer. Coverage also includes how to refine drug leads for suitability in clinical testing, the special issues of clinical testing of molecular-targeted drugs, and intellectual property concerns.
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Cancer Genetics and Drug Target Selection
Protein Transduction Strategies for Target
Assay Development Issues
Transgenic Mouse Models of Cancer
Pharmacodynamic Assays in Cancer Drug
Pharmacokinetic and Toxicology Issues in Cancer
Clinical Development Issues
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activity analysis angiogenesis antiangiogenic anticancer agents anticancer drugs antitumor apoptosis assay bcr-abl Biol biological biomarkers BRCA1 breast cancer cancer cells Cancer Res carcinoma cell cycle cell lines cellular Clin clinical trials compounds cytotoxic disease dose drug discovery effects efficacy EGFR enzyme epidermal growth factor evaluation expression profiling gefitinib gemcitabine gene expression genetic genome Gleevec growth factor receptor human cancer human tumor identify inhibition Iressa leukemia levels malignant metabolism metastases methylation mg/kg mice microarray molecular molecules mouse mutations Natl NF-kB normal cells oncogene Oncol paclitaxel pathways patients peptide pharmacokinetic Phase phenotype plasma potential preclinical predict prenylation Proc prostate protein kinase protein transduction response RNA interference RNAi samples screening selective shRNAs signaling siRNAs specific strategy studies Teicher therapy tissue tissue microarray topotecan toxicity transcription transgenic treatment tumor cells tumor growth delay tumor models tumor-suppressor tyrosine kinase inhibitor VEGF vivo xenograft xenograft models
Página 249 - Demetri GD, von Mehren M, Blanke CD et al. Efficacy and safety of imatinib mesylate in advanced gastrointestinal stromal tumors.