G Protein-Coupled Receptors - Part A

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G Protein-Coupled Receptors, Part A, Volume 193 in the Progress in Molecular Biology and Translational Science series, highlights new advances in the field. G protein-coupled receptors (GPCRs) represent the largest class of cell surface proteins with an intricate involvement of nearly every physiological process in our body. Approximately, one third of the clinically prescribed medicines target GPCRs and the quest to improve the exiting GPCR-targeting therapeutics continues. These two volumes are focused on activation, signaling and regulation of GPCRs with specific examples of receptor systems and cellular processes. Front Cover G Protein-Coupled Receptors - Part A Copyright Contents Contributors Preface Chapter One: Computational and experimental approaches to probe GPCR activation and signaling 1. Introduction 1.1. Molecular switches in GPCR receptors 2. Experimental methods to study GPCR activation and signal transduction 3. Computational methods to study GPCR activation 3.1. All-atom molecular dynamics in explicit solvent 3.2. Coarse-grained MD simulations 3.3. Other coarse-grained approaches 3.4. Data analysis 4. Computational methods to study GPCR signal transduction 4.1. All-atom molecular dynamics 4.2. Coarse-grained and other methods 4.3. Biased signaling of GPCR ligands 5. Viral Hijacking of GPCR Signaling References Chapter Two: Adrenergic receptors in breast cancer 1. Breast cancer 2. Stress 3. Adrenergic receptors 4. β2-Adrenergic receptors in the normal breast and breast cancer 5. Beta-blockers 6. α2-Adrenergic receptors in breast cancer 7. Conclusions References Chapter Three: Tools for adapting to a complex habitat: G-protein coupled receptors in Trichoderma 1. Introduction 2. Activation of GPCRs 3. Downstream targets of GPCR receptors 3.1. G protein signaling 3.2. Mitogen activated protein kinases (MAPkinases) 3.3. cAMP pathway 4. Regulation mechanisms of GPCRs 4.1. GPCR internalization 4.2. Posttranslational modifications (PTMs) of GPCRs 4.2.1. Phosphorylation 4.2.2. Ubiquitination 4.2.3. Glycosylation 4.2.4. Lipidation 4.2.5. PTM prediction in Trichoderma GPCRs 5. GPCRs in Trichoderma 5.1. Asexual and sexual development 5.2. Nutrient sensing 5.3. Regulating secondary metabolism 5.4. Light response 5.5. Interspecies and interkingdom interactions upon plant association References Chapter Four: Targeting G protein coupled receptors for alleviating neuropathic pain 1. Introduction 2. General etiology of neuropathic pain 3. Opioid receptors in neuropathic pain 4. Modulation of mesolimbic circuitry by opioids 5. Cannabinoid receptors 6. Chemokines receptors 7. Adenosine receptors 8. Conclusion and future prospective Acknowledgments Conflict of interest References Chapter Five: Crosstalk between neurons and glia through G-protein coupled receptors: Insights from Caenorhabditis elegans 1. Introduction 2. Neuron-glial interactions through neurotransmitter GPCRs 2.1. Metabotropic glutamate receptors (mGluRs) 2.2. γ-Aminobutyric acid (GABA) receptors 2.3. Dopamine (DA) receptors 2.4. Serotonin receptors 2.5. Muscarinic acetylcholine receptors (mAChRs) 3. Conclusion Acknowledgments References Chapter Six: Cardiovascular GPCR regulation by regulator of G protein signaling proteins 1. Introduction 2. Cardiac GPCRs and RGS proteins 3. Vascular cardiac GPCRs and RGS proteins 4. Platelet/other cardiovascular GPCRs and RGS proteins 5. Conclusions and future perspectives References Chapter Seven: The interaction, mechanism and function of GPR158-RGS7 cross-talk References Chapter Eight: Taste GPCRs and their ligands 1. Introduction 2. Currently known ligands 3. Functional cell-based assays for discovery of taste GPCR ligands 4. Facilitating ligands discovery through computational methods 4.1. Ligand-based methods 4.2. Data collections 4.3. Machine learning 4.4. Structure-based methods 4.5. Combined ligand and structure-based methods 5. Future directions 5.1. Experimental assays expansion and scale up 5.2. The CryoEM era 5.3. Polymorphism in taste GPCRs 6. Concluding remarks Acknowledgments References Chapter Nine: Palmitoylation and G-protein coupled receptors 1. Introduction 2. S-palmitoylation 2.1. Palmitoylation occurs in various species and subcellular organelles 2.2. The enzymes behind S-palmitoylation 2.3. Palmitoyltransferases (PATs) 2.4. GPCRs and the role of protein palmitoylation 2.4.1. Protein trafficking and conformation and stability 2.5. GPCRs and S-palmitoylation 2.5.1. 5-HT1A 2.5.2. Melanocortin 1 receptor 2.5.3. 2-adrenergic receptors C–C chemokine receptor type 5 3. Conclusion References Index Back Cover