Development of small-molecule inhibitors targeting adipose triglyceride lipase.
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ABSTRACT:
SUBMITTER: Mayer N
PROVIDER: S-EPMC3829776 | biostudies-literature | 2013 Dec
REPOSITORIES: biostudies-literature
Publications
Development of small-molecule inhibitors targeting adipose triglyceride lipase.
Mayer Nicole N Schweiger Martina M Romauch Matthias M Grabner Gernot F GF Eichmann Thomas O TO Fuchs Elisabeth E Ivkovic Jakov J Heier Christoph C Mrak Irina I Lass Achim A Höfler Gerald G Fledelius Christian C Zechner Rudolf R Zimmermann Robert R Breinbauer Rolf R
Nature chemical biology 20131006 12
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. ...[more]
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