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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 | |