Modulation of carnitine palmitoyltransferase-1 for the treatment of obesity.

The rising incidence of obesity, as a disorder of energy metabolism, has provoked a search for pharmacological agents that either increase energy expenditure or reduce food intake. The fatty acid oxidation pathway, and its rate-limiting enzyme carnitine palmitoyltransferase (CPT)-1 are potential targets for the treatment of obesity. The modulation of CPT-1 may simultaneously affect energy metabolism and food intake to aid in the management of obesity. Both the inhibition and enhancement of CPT-1 activity are currently under investigation as strategies for the treatment of obesity. In this review, key data on both sides of the 'CPT-1 activity balance' as they relate to obesity therapy are discussed.