G protein-coupled receptors as drug targets : analysis of activation and constitutive activity /
edited by Roland Seifert and Thomas Wieland.
- Weinheim : Wiley-VCH, c2005.
- xxvii, 275 p. ill. 26 cm.
- Methods and principles in medicinal chemistry ; v. 24 .
Includes bibliographical references and index.
Preface. - A personal foreword. - List of contributors. - Abbreviations and terminology. - I. General concepts. - 1. Historical background and introduction. - 2. The nature of constitutive activity and inverse agonism. - 3. Molecular mechanisms of GPCR activation. - 4. Molecular and cellular determinants of GPCR splice variant constitutive activity. - 5. Naturally occurring constitutively active receptors: physiologic and pharmacologic implications. - 6. The impact of G-Proteins on constitutive GPCR activity. - 7. (Patho)physiological and therapeutic relevance of constitutive GPCR activity and inverse agonism at GProtein-coupled receptors. - 8. Methodological approaches. - II. Constitutive activity of selected GPCR systems. - 9. Constitutive activity of -adrenoceptors: analysis in membrane systems. - 10. Constitutive activity of -adrenoceptors: analysis by physiological methods. - 11. Constitutive activity at the 1-Adrenoceptors: past and future implications. - 12. Constitutive activity of muscarinic acetylcholine receptors: implications for receptor activation and physiological relevance. - 13.Constitutively active histamine receptors.- 14. Constitutively active serotonin receptors. - 15. Virally encoded constitutively active chemokine receptors. - Index.