Seifert, Roland / Wieland, Thomas (eds.) G Protein-coupled Receptors as Drug Targets Analysis of Activation and Constitutive Activity Methods and Principles in Medicinal Chemistry (Volume 24) Edited by Mannhold, Raimund / Kubinyi, Hugo / Folkers, Gerd
Short description This highly recommended reference for researchers in academia and industry introduces current models and concepts, while providing an overview of the methods of investigating constitutive GPCR activity. Well illustrated with experimental data and schemes.
From the contents GENERAL CONCEPTS Historical Background and Introduction. The Nature of Constitutive Activity and Inverse Agonism. Molecular Mechanisms of GPCR Activation. Molecular and Cellular Determinants of GPCR Splice Variant Constitutive Activity. Naturally Occurring Constitutively Active Receptors: Physiologic and Pharmacologic Implications. The Impact of G-Proteins on Constitutive GPCR Activity. (Patho)physiological and Therapeutic Relevance of Constitutive GPCR Activity. Methodological Approaches.
CONSTITUTIVE ACITVITY OF SELECTED GPCR SYSTEMS Constitutive Activity of -Adrenoceptors: Analysis in Membrane Systems. Constitutive Activity of -Adrenoceptors: Analysis by Physiological Methods. Constitutive Activity at the 1-Adrenoceptors: Past and Future Implications. Constitutive Activity of Muscarinic Acetylcholine Receptors: Implications for Receptor Activation and Physiological Relevance. Constitutively Active Histamine Receptors. Constitutively Active Serotonin Receptors. Virally Encoded Constitutively Active Chemokine Receptors.
