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List of contributors | |
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Preface | |
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Sense, Nonsense and Antisense: Different Approaches to Drug Discovery | |
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Introduction | |
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Rational drug discovery | |
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'Irrational' drug discovery | |
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The antisense approach | |
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Conclusions | |
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References | |
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Natural Products for Drug Discovery: an Overview | |
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Introduction | |
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Secondary metabolites | |
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A future for natural products in drug discovery? | |
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Technical problems in using natural products in random screening | |
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References | |
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Advanced Screening Technology and Informatics for Natural Products Drug Discovery | |
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Introduction | |
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Screening technology | |
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Advanced informatics for natural products drug discovery | |
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New drug templates from natural products | |
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References | |
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Discovery of Specific Tyrosine Kinase Inhibitors from Microbial and Botanical Sources | |
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Drug discovery and extracts from natural sources | |
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Inhibitors of tyrosine kinases from natural sources | |
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Implementation of high throughput cell-based RTK assays | |
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Primary screening results using plant and microbial extracts | |
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Optimization of specific RTK inhibitory activities in fungal extracts using fermentation conditions | |
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Conclusions | |
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Acknowledgments | |
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References | |
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Plant Cell Culture: a Vehicle for Drug Discovery | |
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Introduction | |
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Plant cell culture technology | |
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Commercial production systems | |
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Phytochemicals from plant cell culture | |
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Screening plant cell cultures: early programmes | |
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The Phytera approach to lead discovery: ExPAND | |
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Case study: the development of antifungal drug candidates | |
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Acknowledgments | |
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References | |
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Pharmacy of the Deep--Marine Organisms as Sources of Anticancer Agents | |
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Introduction | |
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Aeroplysinin | |
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Girolline | |
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Halichondrin-B | |
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Jasplakinolide | |
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Didemnin-B | |
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Ecteinascidin 743 | |
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Dolastatin-10 | |
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Bryostatin-1 | |
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Halomon | |
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Future directions | |
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References | |
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Drug Discovery by Using Molecular Biology to Reprogramme Microorganisms | |
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Introduction | |
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Streptomycete genetics and molecular biology | |
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The chemistry of polyketide biosynthesis | |
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Molecular genetics of aromatic polyketide biosynthesis | |
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Using single genes from antibiotic clusters as a molecular toolbox | |
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Future perspectives for the 'combi-gen' approach | |
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References | |
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Small Molecule Drug Screening Based on Surface Plasmon Resonance | |
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Introduction | |
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Principles of BIA | |
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What can BIA measure? | |
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A tool in drug discovery | |
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Conclusions | |
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References | |
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An Overview of Combinatorial Chemistry and Its Applications to the Identification of Matrix Metalloproteinase Inhibitors (MMPIs) | |
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Combinatorial chemistry | |
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Matrix metalloproteinases (MMPs) | |
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Combinatorial synthesis of MMPIs | |
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Conclusions | |
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Acknowledgments | |
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References | |
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New Methods for Structure-based De Novo Drug Design | |
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The role of de novo design in drug discovery | |
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General methods and considerations in de novo design | |
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Synthetic accessibility within PRO_SELECT | |
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Conclusions | |
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Acknowledgments | |
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References | |
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Current and Future Capabilities in Automated Drug Screening and Development | |
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Introduction | |
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General considerations | |
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Capabilities in high throughput screening | |
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Preparation, filtration and extraction | |
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Molecular biology | |
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Combinatorial chemistry | |
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Full automation | |
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Costs and returns | |
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References | |
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Antisense Oligonucleotide Therapeutics | |
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Introduction | |
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First generation oligonucleotides | |
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Clinical experience with antisense oligonucleotides | |
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Conclusions | |
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References | |
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Index | |