This book provides a comprehensive overview of the development of metabolic syndrome, the underlying mechanisms and therapeutic strategies for drug development. The authors examine the context of underlying molecular pathways and integrated physiology, then expanding the discussion to diseases associated with metabolic syndrome. The development of drug therapies for these diseases and complications is extensively covered. The book offers a comprehensive and in-depth view of energy metabolism, metabolic tissues and pathways, molecular mechanism-based drug discovery and clinical implications. CONTENTS Introduction (Minghan Wang). Part I. The physiology of metabolic tissues under normal and disease states. Chapter 1: Gut as an endocrine organ: the role of nutrient-sensing in energy metabolism (Minghan Wang). Chapter 2: Central glucose sensing and control of food intake and energy homeostasis (Lourdes Mounien and Bernard Thorens). Chapter 3: Abnormalities in insulin secretion in type 2 diabetes mellitus (Taly Meas and Pierre-Jean Guillausseau). Chapter 4: Adipokine production by adipose tissue: A novel target for treating metabolic syndrome and its sequelae (Vanessa DeClercq, Danielle Stringer, Ryan Hunt, Carla G. Taylor, and Peter Zahradka). Chapter 5: Hepatic metabolic dysfunctions in type 2 diabetes: Insulin resistance and impaired glucose production and lipid synthesis (Ruojing Yang). Chapter 6: Energy metabolism in skeletal muscle and its link to insulin resistance (Minghan Wang). Part II. Metabolic diseases and current therapies. Chapter 7: Mechanisms and complications of metabolic syndrome (Minghan Wang). Chapter 8: Emerging therapeutic approaches for dyslipidemia associated with high LDL and low HDL (Margrit Schwarz and Jae B. Kim). Chapter 9: Mechanism of action of niacin: implications for atherosclerosis and drug discovery (Devan Marar, Shobha H. Ganji, Vaijinath S. Kamanna, and Moti L. Kashyap). Chapter 10: Current anti-diabetic therapies and mechanisms (Minghan Wang). Part III. Drug targets for anti-diabetic therapies. Chapter 11: GLP-1 biology, signaling mechanisms, physiology, and clinical studies (Remy Burcelin, Cendrine Cabou1, Christophe Magnan, and Pierre Gourdy). Chapter 12: Dipeptidyl peptidase IV inhibitors for treatment of diabetes (McIntosh, CHS, Kim, S-J., Pederson, RA, Heiser, U, and Demuth, H-U). Chapter 13: Sodium glucose co-transporter 2 inhibitors (Margaret Ryan and Serge A. Jabbour). Chapter 14: Fibroblast growth factor 21 as a novel metabolic regulator (Radmila Micanovic, James D. Dunbar, and Alexei Kharitonenkov). Chapter 15: Sirtuins as potential drug targets for metabolic diseases (Qiang Tong). Chapter 16: 11?-hydroxysteroid dehydrogenase type 1 as a therapeutic target for type 2 diabetes (Clarence Hale and David J. St. Jean, Jr.). Chapter 17: Monoclonal antibodies for the treatment of type 2 diabetes: A case study with glucagon receptor blockade (Hai Yan, Wei Gu, and Murielle Veniant-Ellison). Part IV. Lessons learned and future outlook. Chapter 18: Drug development for metabolic diseases: past, present and future (Minghan Wang).