Therapeutic Targets: Modulation, Inhibition, and Activation

Preface vii

Contributors ix

1. cAMP-Specific Phosphodiesterases: Modulation, Inhibition, and Activation 1
R. T. Cameron and George S. Baillie

2. Protease-Activated Receptor 2 37
Qihai Gu and Lu-Yuan Lee

3. Voltage-Gated Sodium Channels as Therapeutic Targets 63
Joshua S. Wingerd, Irina Vetter, and Richard J. Lewis

4. Multitarget Drugs for Stabilization of Calcium Cycling and Neuroprotection in Neurodegenerative Diseases and Stroke 123
Antonio M. G. de Diego, Silvia Lorrio, Jesús M. Hernández-Guijo, Luis Gandía, and Antonio G. García

5. Oligomerization of G-Protein-Coupled Receptors 201
Juan F. López-Giménez and Javier González-Maeso

6. Sigma 1 Receptor Chaperone: Pharmacology and Therapeutic Perspectives 225
Daniel Zamanillo, Enrique Portillo-Salido, José Miguel Vela, and Luz Romero

7. Lipids as New Targets 279
Eduardo Domúnguez

8. Knowledge Base for Nuclear Receptor Drug Discovery 309
Albert A. Antolín and Jordi Mestres

9. Gene Promoters and Transcription Control Regions as Therapeutic Targets 327
Antonio Zorzano, David Sebastian, Jana Sánchez-Wandelmer, Laia Miret, and Fernando Albericio

10. Roles of Glucagon-Like Peptide and Glucose-Dependent Insolinotropic Polypeptide Hormones in Brain Function and Neurodegeneration 351
Christian Hölscher

11. Exocytotic Machinery as a Target for the Development of New Drugs for Schizophrenia 375
María Jose Guerrero, Itsaso Hormaeche, María Uribarri, Julie Masse, and José María Palacios

12. Targeting Epigenetic Abnormalities in the Brain 409
Erin Y. Sterner, Lisa E. Kalynchuk, and Hector J. Caruncho

13. Rodent Models as Tools for Discovering Novel Therapeutic Targets in the Brain: The Case of Epilepsy 427
Justin J. Botterill, Axel J. Guskjolen, Lisa E. Kalynchuk, and Hector J. Caruncho

14. New Approaches Applied to Drug Screening 455
José Brea and María Isabel Loza

Index 477