Development of small-molecule inhibitors targeting adipose triglyceride lipase

N Mayer, M Schweiger, M Romauch… - Nature chemical …, 2013 - nature.com
N Mayer, M Schweiger, M Romauch, GF Grabner, TO Eichmann, E Fuchs, J Ivkovic, C Heier
Nature chemical biology, 2013nature.com
Adipose triglyceride lipase (ATGL) is rate limiting in the mobilization of fatty acids from
cellular triglyceride stores. 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. Here we report 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.
Abstract
Adipose triglyceride lipase (ATGL) is rate limiting in the mobilization of fatty acids from cellular triglyceride stores. 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. Here we report 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.
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