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Obesity is an epidemic with enormous health, economic and social burdens. Current drugs for obesity treatment are far from ideal in terms of efficacy and side effects. Reviews in… Read more
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Obesity is an epidemic with enormous health, economic and social burdens. Current drugs for obesity treatment are far from ideal in terms of efficacy and side effects. Reviews in this volume of Progress in Molecular Biology and Translational Science summarize current status in studies of a number of G protein-coupled receptors that were shown to be promising targets for obesity treatments. Some of these receptors also cause monogenic obesity in humans.
Contributors
Preface
Chapter One. G Protein-Coupled Receptors as Regulators of Energy Homeostasis
Abbreviations
1 Introduction to G Protein-Coupled Receptors
2 Obesity and Current Treatments
3 Regulation of Energy Homeostasis in the Central Nervous System
4 Regulation of Energy Homeostasis by the GI Peptides
5 Regulation of Energy Homeostasis by Peptides from Endocrine Pancreas
6 Regulation of Energy Homeostasis by Orphan GPCRs
7 Regulation of Energy Homeostasis by GPCRs in Domestic Animals
8 Regulation of Energy Homeostasis by GPCRs in Lower Vertebrates
9 Genetics of Human Obesity
10 Summary
Acknowledgments
References
Chapter Two. Ghrelin Receptor in Energy Homeostasis and Obesity Pathogenesis
1 Overview of the Ghrelin Receptor
2 The Ghrelin Receptor and Energy Metabolism
3 Strategies for Treatment of Obesity and Diabetes
4 Conclusion
Acknowledgments
References
Chapter Three. Obestatin Receptor in Energy Homeostasis and Obesity Pathogenesis
1 Two Proposed Obestatin Receptors
2 Obestatin and its Receptor(s) in Energy Homeostasis
Acknowledgments
References
Chapter Four. Melanocortin-3 Receptors and Metabolic Homeostasis
1 Introduction
2 The “Leptin-Melanocortin” Pathway: A Canonical Pathway Linking Energy Stores with Neural Outputs Regulating Adaptation to Energy Requirements
3 The Central Nervous Melanocortin System
4 Cloning of the Melanocortin Receptors
5 Melanocortin-3 Receptors in Metabolic Homeostasis
6 Conclusions and Future Directions
Acknowledgments
References
Chapter Five. Melanocortin-4 Receptor in Energy Homeostasis and Obesity Pathogenesis
1 The Melanocortin-4 Receptor Gene (MC4R)
2 From Rodent MC4R Models to Human Obesity
3 Mutations in the MC4R Confer a Major Gene Effect for the Development of Obesity
4 Phenotypes Detected in MC4R Mutation Carriers
5 MC4R Mutations in Population-Based Study Groups
6 Functional Analyses
7 Nonsynonymous MC4R Polymorphisms that Confer Protection from Obesity
8 Genome-Wide Association Studies: SNPs Downstream of the MC4R Gene
9 Synthetic Association at the MC4R Locus?
10 Relevance of MC4R Mutations for Phenotypes Related to Body Weight Regulation
11 Therapeutic Implications for MC4R Mutation Carriers
12 Conclusions and Future Directions
Acknowledgments
References
Chapter Six. G Protein-Coupled Estrogen Receptor in Energy Homeostasis and Obesity Pathogenesis
Abbreviations
1 Introduction
2 Estrogen Signaling: Estrogens and ERs
3 Estrogenic Action in the Brain: Central Regulation of Energy Homeostasis
4 Estrogen Action in Adipose Tissue: Regulation of Lipogenesis/Lipolysis and Adiposity
5 Estrogens Interact with Leptin
6 Conclusions
Acknowledgments
References
Chapter Seven. Free Fatty Acid Receptor GPR120 and Pathogenesis of Obesity and Type 2 Diabetes Mellitus
1 Introduction
2 Molecular Cloning and Localization of GPR120
3 Physiology of GPR120
4 Pharmacology of the GPR120
5 GPR120 Mutations in Human Obesity
6 Conclusions
References
Chapter Eight. The Role of Cholecystokinin Receptors in the Short-Term Control of Food Intake
1 Control of Food Intake: A General Overview
2 CCK: Historical Prospective
3 Molecular Forms of CCK
4 CCK Receptors
5 Physiological Responses Evoked by CCK
6 The Role of CCK1 Receptors in the Short-Term Control of Food Intake by CCK
7 CCK: Mechanism of Action
8 Interaction Between CCK and Other Satiety Peptides
9 The Possible Role of the ENS of the Gut in the Short-Term Regulation of Food Intake by CCK
Acknowledgments
References
Chapter Nine. Adiponectin Receptors in Energy Homeostasis and Obesity Pathogenesis
1 Introduction
2 Expression
3 Physiology
4 Signaling Pathways
5 Regulation by Leptin and Insulin
6 Regulation by Steroid Hormones
7 Pathology
8 Conclusion and Future Studies
References
Chapter Ten. The Role of Bombesin and Bombesin-Related Peptides in the Short-term Control of Food Intake
1 Introduction
2 Historical Perspective
3 Distribution of Bombesin and Bombesin-Related Peptides
4 Physiological Responses Evoked by Bombesin and Bombesin-Related Peptides
5 Bombesin and Bombesin-Related Peptides Receptors
6 The Role of Bombesin and Bombesin-Related Peptides in the Short-Term Control of Food Intake
Acknowledgments
References
Index
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