Development of small molecule inhibitors targeting adipose triglyceride lipase

  title={Development of small molecule inhibitors targeting adipose triglyceride lipase},
  author={Nicole C Mayer and Martina Schweiger and Matthias Romauch and Gernot F. Grabner and Thomas O Eichmann and Elisabeth Fuchs and Jakov Ivkovic and Christoph Heier and Irina Mrak and Achim Lass and Gerald Hoefler and Christian Fledelius and Rudolf Zechner and Robert Zimmermann and Rolf Breinbauer},
  booktitle={Nature chemical biology},
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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