Adipose triglyceride lipase (ATGL) is rate limiting in the mobilization of fatty acids from cellular triglyceride stores. Adipose triglyceride lipase is a recently described adipose-enriched protein with triglyceride-specific lipase activity This central role in lipolysis marks ATGL as an interesting pharmacological target as deregulated fatty acid metabolism is closely linked to dyslipidemic and metabolic disorders. This paper reports on the development and characterization of a small-molecule inhibitor of ATGL. Atglistatin is selective for ATGL and reduces fatty acid mobilization in vitro and in vivo.
Nicole Mayer et al Development of small-molecule inhibitors targeting adipose triglyceride lipase. Nature Chemical Biology Published online 06 October 2013