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Pharmacology & Therapeutics of Constitutively Active Receptors : Advances in Pharmacology, Volume 70.
Volume 70 of Advances in Pharmacology presents the pharmacology and therapeutics of constitutively active receptors. With a variety of chapters and the best authors in the field, the volume is an essential resource for pharmacologists, immunologists, and biochemists alike. Advances in Pharmacology p...
| Clasificación: | Libro Electrónico |
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| Otros Autores: | |
| Formato: | Electrónico eBook |
| Idioma: | Inglés |
| Publicado: |
Burlington :
Elsevier Science,
2014.
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| Temas: | |
| Acceso en línea: | Texto completo |
Tabla de Contenidos:
- Front Cover; Pharmacology & Therapeutics of Constitutively Active Receptors; Copyright; Contents; Preface; Contributors; Chapter One: Constitutively Active Rhodopsin and Retinal Disease; 1. Introduction; 2. Rhodopsin Activity; 2.1. Physiology of rhodopsin activity; 2.2. Molecular switches that lock rhodopsin in an inactive state; 3. Constitutive Activity in Rhodopsin that Causes Disease; 3.1. Leber congenital amaurosis and vitamin A deficiency; 3.1.1. Opsin: Active apoprotein; 3.2. Congenital night blindness; 3.2.1. G90D: Active dark state; 3.2.2. T94I, A292E, and A295V: Active dark state.
- 3.3. Retinitis pigmentosa3.3.1. S186W and D190N: Thermal activation; 3.3.2. G90V: Active dark state and thermal activation; 3.3.3. K296E: Active apoprotein and stable arrestin interactions; 4. How Constitutive Activity Can Cause Different Phenotypes; 4.1. Different levels of activity as an underlying cause of different phenotypes; 4.2. Do all constitutively active mutants adopt the same active-state conformation?; 5. Conclusion; Conflict of Interest; Acknowledgments; References; Chapter Two: Constitutive Activity in Gonadotropin Receptors; 1. Introduction.
- 2. Naturally Occurring CAMs of the Gonadotropin Receptors2.1. CAMs of the human LHCGR; 2.2. CAMs of the human FSHR; 3. Experimental Models of Gonadotropin Receptor CAMs; 3.1. LHCGR CAMs and LH/hCG overexpressing mice; 3.2. FSHR CAMs and FSHR overexpressing mice; 4. Molecular Basis of Constitutive Activity in Gonadotropin Receptors; 4.1. Mechanism of ligand-induced activation in gonadotropin receptors; 4.2. Mechanisms leading to constitutive activity of gonadotropin receptors; 5. Design of New Molecules for Controlling the Activity of Constitutively Active Gonadotropin Receptors; 6. Conclusion.
- Conflict of InterestAcknowledgments; References; Chapter Three: Constitutive Activities in the Thyrotropin Receptor: Regulation and Significance; 1. Introduction; 2. Constitutive Activity in the Thyrotropin Receptor; 2.1. Properties related to Gs-mediated basal signaling activity; 2.1.1. Structural determinants involved in regulation of basal signaling activity; 2.1.2. Physiological aspects of basal signaling; 2.2. Modulation of constitutive signaling activity; 2.2.1. Constitutive signaling activity induced by mutations; 2.2.2. Silencing of constitutive activity.
- 2.2.2.1. Constitutive inactivation by mutations2.2.2.2. Small-molecule ligands with inverse agonistic properties; 2.2.2.3. Antibodies with inverse agonistic properties; 3. Conclusion; Conflict of Interest; Acknowledgments; References; Chapter Four: Constitutive Activity in Cannabinoid Receptors; 1. Introduction; 2. Challenges in Proving Constitutive Receptor Activity; 2.1. Demonstrating constitutive receptor activity requires the use of agonist, inverse agonist, and neutral antagonist; 2.2. Constitutive active receptor versus constitutive agonist tone.