Cargando…
Progress in medicinal chemistry. Volume 46 /
Appropriate selection of biochemical targets is one of the most important drivers of cost effectiveness in the discovery of new medicines. Despite the many advances in genetics, genomics and systems biology, 'validation' of a target is not achieved until therapeutic efficacy is demonstrate...
| Clasificación: | Libro Electrónico |
|---|---|
| Otros Autores: | , |
| Formato: | Electrónico eBook |
| Idioma: | Inglés |
| Publicado: |
Amsterdam ; Oxford :
Elsevier,
2008.
|
| Colección: | Progress in medicinal chemistry ;
46 |
| Temas: | |
| Acceso en línea: | Texto completo Texto completo |
Tabla de Contenidos:
- Cover; Preface; Contents; List of Contributors; 1 The Discovery of Raltegravir, an Integrase Inhibitor for the Treatment of HIV Infection; Introduction; Finding the lead; Optimisation; The Importance of Protein Binding; N-Methylpyrimidines; Resistance Profiling; Discovery of Raltegravir; Other Integrase Inhibitors; Conclusion; References; 2 Inhibitors of 11beta-Hydroxysteroid Dehydrogenase Type 1; Introduction; The SDR superfamily and 11beta-HSD1 enzymology; Protein crystal structures of 11beta-HSD1; Potential therapeutic indications; Biological assays; Inhibitors of 11beta-HSD1
- In vivo Studies of Selected 11beta-HSD1 inhibitorsClinical studies on 11beta-HSD1 inhibitors; Conclusion; References; 3 alpha7 Nicotinic Acetylcholine Receptor Agonists and Positive Allosteric Modulators; Introduction; alpha7 nAChR agonists; alpha7 nAChR Positive Allosteric Modulators; Conclusions; References; 4 Small Molecule Bradykinin B1 Receptor Antagonists as Potential Therapeutic Agents for Pain; Introduction; Tools for evaluating B1 antagonists; Medicinal chemistry and preclinical studies; Conclusions; References
- 5 Histone Deacetylase Inhibitors: A Novel Class of Anti-Cancer Agents on its Way to the MarketIntroduction; Biological background; HDAC crystal and co-crystal structures; HDAC inhibitors; Isoform selectivity of HDAC inhibitors; Developmental status of HDAC inhibitors; Future perspective; References; 6 5-HT2C Ligands: Recent Progress; Introduction; Possible therapeutic utilities of selective ligands for the 5-HT2C receptor subtype; Side-effect Concerns; Medicinal Chemistry towards 5-HT2C Ligands; Conclusion; References; Subject Index; Cumulative Index of Authors for Volumes 1- 46