1.

Record Nr.

UNINA9910139201903321

Titolo

GPCR molecular pharmacology and drug targeting [[electronic resource] ] : shifting paradigms and new directions / / edited by Annette Gilchrist

Pubbl/distr/stampa

Hoboken, N.J., : Wiley, c2010

ISBN

1-118-03517-8

1-282-68599-6

9786612685996

0-470-62732-8

0-470-62731-X

Descrizione fisica

1 online resource (544 p.)

Altri autori (Persone)

GilchristAnnette

Disciplina

612/.015756

Soggetti

G proteins

Drug targeting

Lingua di pubblicazione

Inglese

Formato

Materiale a stampa

Livello bibliografico

Monografia

Note generali

Includes index.

Nota di contenuto

GPCR MOLECULAR PHARMACOLOGY AND DRUG TARGETING: SHIFTING PARADIGMS AND NEW DIRECTIONS; CONTENTS; PREFACE; CONTRIBUTORS; CHAPTER 1: The Evolution of Receptors: From On-Off Switches to Microprocessors; CHAPTER 2: The Evolving Pharmacology of GPCRs; CHAPTER 3: The Emergence of Allosteric Modulators for G Protein - Coupled Receptors; CHAPTER 4: Receptor-Mediated G Protein Activation: How, How Many, and Where?; CHAPTER 5: Molecular Pharmacology of Frizzleds-with Implications for Possible Therapy

CHAPTER 6: Secretin Receptor Dimerization: A Possible Functionally Important Paradigm for Family B G Protein-Coupled ReceptorsCHAPTER 7: Past and Future Strategies for GPCR Deorphanization; CHAPTER 8: High-Throughput GPCR Screening Technologies and the Emerging Importance of the Cell Phenotype; CHAPTER 9: Are "Traditional" Biochemical Techniques Out of Fashion in the New Era of GPCR Pharmacology?; CHAPTER 10: Fluorescence and Resonance Energy Transfer Shine New Light on GPCR Function; CHAPTER 11: Integration of Label-Free Detection Methods in GPCR Drug Discovery

CHAPTER 12: Screening for Allosteric Modulators of G Protein-Coupled



ReceptorsCHAPTER 13: Ultra-High-Throughput Screening Assays for GPCRs; CHAPTER 14: New Techniques to Express and Crystallize G Protein-Coupled Receptors; CHAPTER 15: Structure and Modeling of GPCRs: Implications for Drug Discovery; CHAPTER 16: X-Ray Structure Developments for GPCR Drug Targets; CHAPTER 17: Pharmacological Chaperones: Potential for the Treatment of Hereditary Diseases Caused by Mutations in G Protein-Coupled Receptors; INDEX

Sommario/riassunto

G protein-coupled receptors (GPCRs) are a large protein family of transmembrane receptors vital in dictating cellular responses. GPCRs are involved in many diseases, but are also the target of around half of all modern medicinal drugs.  Shifting Paradigms in G Protein Coupled Receptors takes a look at the way GPCRs are examined today, how they react, how their mutations lead to disease, and the many ways in which they can be screened for compounds that modulate them. Chemists, pharmacologists, and biologists will find essential information in this comprehensive reference.