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Progress in medicinal chemistry. Volume 53 /
Progress in Medicinal Chemistry provides a review of eclectic developments in medicinal chemistry. This volume continues in the serial's tradition of providing an insight into the skills required of the modern medicinal chemist; in particular, the use of an appropriate selection of the wide ran...
| Clasificación: | Libro Electrónico |
|---|---|
| Otros Autores: | , |
| Formato: | Electrónico eBook |
| Idioma: | Inglés |
| Publicado: |
Amsterdam :
Elsevier,
2014.
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| Temas: | |
| Acceso en línea: | Texto completo Texto completo |
Tabla de Contenidos:
- Front Cover; Progress in Medicinal Chemistry; Copyright; Preface; Contents; Contributors; Chapter One: Structure-Based Drug Design for G Protein-Coupled Receptors; 1. Introduction; 2. Structural Architecture of GPCRs; 3. GPCR Protein-Ligand X-Ray Structures; 4. Mechanisms of Activation: Agonist Bound Structures; 5. Biased Agonism; 6. Traditional Approaches to GPCR Drug Discovery and the Need for Change; 7. Potential of SBDD and FBDD for GPCR Drug Discovery; 7.1. Beta Adrenergic Receptors; 7.2. Histamine Receptor; 7.3. Adenosine Receptors; 7.4. CXCR4 Receptor; 7.5. CRF1 Receptor.
- 8. Conclusions and OutlookAcknowledgments; References; Chapter Two: P2X7 Antagonists as Potential Therapeutic Agents for the Treatment of CNS Disorders; 1. Introduction; 2. P2X7 in the CNS; 2.1. Neuropsychiatric Disorders; 2.2. Neurodegenerative Disorders; 2.3. Pain; 3. P2X7 Modulators in Clinical Trials; 4. P2X7 Receptor Antagonists; 4.1. Monocyclic Hetero and Carbocyclic Antagonists; 4.2. Heteroaromatic-Fused Core Antagonists; 4.3. P2X7 Antagonists in Animal Models of the CNS; 5. Conclusion; References; Chapter Three: �-Secretase Modulators: Current Status and Future Directions.
- 1. Introduction1.1. Alzheimers Disease; 1.2. �-Secretase Biology; 2. GSMs: Chemical Classes; 2.1. Acid Derivatives; 2.1.1. Myriad and Chiesi; 2.1.2. Janssen; 2.1.3. EnVivo; 2.1.4. GSK; 2.1.5. Merck; 2.1.6. Biogen Idec; 2.1.7. Pfizer/Astellas; 2.1.8. Summary; 2.2. Imidazoles and Related Analogues; 2.2.1. TorreyPines; 2.2.2. GSK; 2.2.3. Roche; 2.2.4. Janssen; 2.2.5. BMS; 2.2.6. Pfizer; 2.2.7. Merck; 2.2.8. AstraZeneca; 2.2.9. Boehringer Ingelheim; 2.2.10. Shionogi; 2.2.11. Dainippon Sumitomo; 2.2.12. Summary; 2.3. Natural Products; 3. Chemical Biology; 4. Outlook; 5. Clinical Studies.
- 6. ConclusionsReferences; Chapter Four: Recent Progress in the Discovery and Development of N-Type Calcium Channel Modulators for the Treatment of Pain; 1. Introduction; 2. Voltage-Gated Calcium Channels; 2.1. Cav Channel Architecture; 2.2. Cav Channel Physiology; 2.3. Cav Channel States; 2.4. Implications for Therapeutic Intervention; 3. N-Type Calcium Channels; 3.1. N-Type Biology; 3.2. N-Type Physiology; 3.3. Role in the Pathophysiology of Pain; 4. N-Type Clinical Landscape and Emerging Pipeline; 4.1. Peptide-Derived Therapeutics; 4.1.1. N-Type Blockade by Venom Toxins.
- 4.1.2. Peptide-Derived Therapeutics4.1.3. Peptide Mimetics; 4.2. Small Molecule N-Type Blockers; 4.2.1. Non-Selective Calcium Channel Blockers as a Starting Point; 4.2.2. Piperazine-Based Structures; 4.2.3. Piperidine-Containing Structures; 4.2.4. Indoles and Oxindoles; 4.2.5. Other Approaches; 4.3. N-Type Calcium Channel Modulators in the Clinic; 4.3.1. Z160; 4.3.2. CNV2197944; 5. Concluding Remarks; References; Subject Index; Cumulative Index of Authors for Volumes 1-53; Cumulative Index of Subjects for Volumes 1-53.