Obesity is growing at an alarming rate with huge consequences on health and economy. The
worldwide prevalence of obesity has nearly doubled in less than 35 years. Obesity causes many
physiological dysfunctions that affect nearly every organ producing multiple morbidities. Despite these
facts, there is still no clear, well-defined solution. Notwithstanding the devastating prevalence and
consequences of obesity, today only five medicines, orlistat, lorcaserin, phentermine-topiramate,
bupropion-naltrexone and liraglutide, are approved by the FDA for long-term treatment of obesity. In
this review, the current approaches to treat obesity such as the development of diacylglycerol Oacyltransferase-
1 inhibitors, growth hormone secretagogue receptor-1a antagonists/inverse agonists,
melanocortin-3 receptors agonists and melanin concentrating hormone receptor-1 antagonists, will be
discussed. The main focus will be on the molecules that were able to reach clinical trials. The last
section is dedicated to the “browning” phenomenon of white adipose tissues and the potential of
Aldh1a1 inhibitors to treat obesity.
Keywords: Adipose tissues plasticity, Aldh1a1, brown adipose tissues, DGAT-1 inhibitors, GHS-R1 antagonists/inverse
agonists, MCHR1 antagonists, melanocortin-3 receptors agonists, obesity.
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