2. Academic Validation
  3. Development of small-molecule inhibitors targeting adipose triglyceride lipase

Development of small-molecule inhibitors targeting adipose triglyceride lipase

  • Nat Chem Biol. 2013 Dec;9(12):785-7. doi: 10.1038/nchembio.1359.
Nicole Mayer  # 1,  Martina Schweiger  # 2,  Matthias Romauch 2,  Gernot F Grabner 2,  Thomas O Eichmann 2,  Elisabeth Fuchs 1,  Jakov Ivkovic 1,  Christoph Heier 2,  Irina Mrak 2,  Achim Lass 2,  Gerald Höfler 3,  Christian Fledelius 4,  Rudolf Zechner 2,  Robert Zimmermann 2,  Rolf Breinbauer 1
Affiliations

Affiliations

  • 1 Institute of Organic Chemistry, Graz University of Technology, 8010 Graz, Austria.
  • 2 Institute of Molecular Biosciences, University of Graz, 8010 Graz, Austria.
  • 3 Institute of Pathology, Medical University of Graz, 8010 Graz, Austria.
  • 4 Novo Nordisk A/S, Novo Nordisk Park, DK-2760 Måløv, Denmark.
  • # Contributed equally.
PMID: 24096302 DOI: 10.1038/nchembio.1359
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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