title: Peripheral targets in obesity treatment: a comprehensive update.
abstract: Obesity is a major epidemic of our time and is associated with diseases such as metabolic syndrome, type 2 diabetes mellitus and atherosclerotic cardiovascular disease. Although weight loss drugs, when accompanied by diet and exercise, could be a very helpful medical tool in treating obese or overweight patients, their usefulness has been questioned due to the complexity of this type of medication, which regards a plethora of issues such as efficacy and safety of the drug and also risks and benefits among different patients. In general, obesity drugs that target peripheral pathophysiological mechanisms can be divided into two main categories. The first category includes anti-obesity agents able to reduce or limit energy absorption, such as pancreatic lipase and microsomal triglyceride transfer protein inhibitors. The second category consists of a heterogeneous group of compounds aiming to decrease fat mass by increasing energy expenditure or by redistributing adipose tissue. Angiogenesis inhibitors, beta-3 receptor agonists, sirtuin-I activators, diazoxide and other molecules belong to this group. The glucagon-like peptide-1 receptor agonists consist the third category of peripheral anti-obesity agents discussed therein. This review aims to provide a general overview of the molecules and substances that are already or could potentially be used as peripheral anti-obesity drugs, the molecular mechanisms by which they act, as well as their current stage of development, production and/or availability.
authors.affiliation: Department of Experimental Physiology, University of Athens Medical School, Athens, Greece; Department of Internal Medicine III and Institute of Physiology, University of Dresden, Dresden, Germany.
authors.forename: A
authors.initials: A
authors.lastname: Chatzigeorgiou
authors.forename: E
authors.initials: E
authors.lastname: Kandaraki
authors.forename: A G
authors.initials: AG
authors.lastname: Papavassiliou
authors.forename: M
authors.initials: M
authors.lastname: Koutsilieris
mesh_terms: D000217:Acyltransferases / Q000037:antagonists & inhibitors; D000273:Adipose Tissue / Q000187:drug effects; D020533:Angiogenesis Inhibitors; D019440:Anti-Obesity Agents / Q000627:therapeutic use*; D002352:Carrier Proteins / Q000037:antagonists & inhibitors; D051048:Diacylglycerol O-Acyltransferase / Q000037:antagonists & inhibitors; D004734:Energy Metabolism / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000627:therapeutic use; D000067757:Glucagon-Like Peptide-1 Receptor; D006801:Humans; D008049:Lipase / Q000037:antagonists & inhibitors; D009765:Obesity / Q000188:drug therapy*; D018027:Receptors, Glucagon / Q000819:agonists; D051297:Sodium-Glucose Transporter 2; D000077203:Sodium-Glucose Transporter 2 Inhibitors; D037042:Thyroid Hormone Receptors beta / Q000819:agonists
chemical_list: D020533:Angiogenesis Inhibitors; D019440:Anti-Obesity Agents; D002352:Carrier Proteins; D004791:Enzyme Inhibitors; C000593833:GLP1R protein, human; D000067757:Glucagon-Like Peptide-1 Receptor; D018027:Receptors, Glucagon; C089180:SLC5A2 protein, human; D051297:Sodium-Glucose Transporter 2; D000077203:Sodium-Glucose Transporter 2 Inhibitors; D037042:Thyroid Hormone Receptors beta; C106092:microsomal triglyceride transfer protein; D000217:Acyltransferases; D051048:Diacylglycerol O-Acyltransferase; C021802:2-acylglycerol O-acyltransferase; D008049:Lipase; C518354:PNLIP protein, human
keywords: Adipose tissue; anti-obesity drugs; energy absorption; energy expenditure