Therapeutic Targets
Modulation, Inhibition, and Activation
1. Edition June 2012
494 Pages, Hardcover
Professional Book
Short Description
Providing insight into where the next generations of drugs are likely to emerge, this book describes the pharmacology of therapeutically undefined targets and potential applications. In some cases, there are no defined drugs to modulate some of the targets, and in other cases inhibition or activation will render different therapeutic uses. Chapters cover specific biochemical targets like kinases, phosphatases, phosphodiesterases, and potassium channels. Because different diseases can require their own targeting strategies, the book has chapters on the strategies for targeting Alzheimer's, diabetes, pain, and inflammation.
Providing insight into where the next generations of drugs are likely to emerge, this book describes the pharmacology of therapeutically undefined targets and potential applications. In some cases, there are no defined drugs to modulate some of the targets, and in other cases inhibition or activation will render different therapeutic uses. Chapters cover specific biochemical targets like kinases, phosphatases, phosphodiesterases, and potassium channels. Because different diseases can require their own targeting strategies, the book has chapters on the strategies for targeting Alzheimer's, diabetes, pain, and inflammation.
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
Mabel Loza is Professor of Pharmacology at the University of Santiago de Compostela (USC). She created the USEF Drug Screening Platform, with more than ten years of experience in public and private mixed early drug discovery programs.
