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Publisher Summary This chapter presents an overview of obesity therapeutics. When measured by body mass index (BMI), a BMI of 30 is the threshold for obesity. Obesity is mischaracterized as a cosmetic or life style issue, when in reality it is a devastating disease with tremendous health and financial consequences. In the United States alone, it has been estimated that more than 300,000 deaths occur per year from obesity. This distressing effect on life expectancy is to a large extent related directly to the life threatening co-morbidities of obesity such as noninsulin-dependent diabetes, hypertension, coronary artery disease, and some forms of cancer. The less lethal comorbidities associated with obesity include gallstones, osteoarthritis, degenerative arthritis, and apnea. The chapter discusses the regulation of obesity through multiple integrated pathways and highlights historical approaches to obesity therapeutics. It also highlights current approaches to obesity therapeutics and discusses neuropeptide Y receptors, melanin-concentrating hormone receptor, and the role of protein tyrosine phosphatase 1B (PTP1B). The use of PTP1B inhibitors for the treatment of obesity and diabetes is an active area for anti-obesity research. The untapped potential of antiobesity drugs is also explored in the chapter. |