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Nature Research, Nature Chemical Biology, 12(9), p. 785-787, 2013

DOI: 10.1038/nchembio.1359

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Development of small molecule inhibitors targeting adipose triglyceride lipase

Journal article published in 2013 by Nicole Mayer, Martina Schweiger ORCID, Matthias Romauch, Gernot F. Grabner, Thomas O. Eichmann ORCID, Elisabeth Fuchs, Jakov Ivkovic, Christoph Heier, Irina Mrak, Achim Lass ORCID, Gerald Höfler, Christian Fledelius, Rudolf Zechner ORCID, Robert Zimmermann ORCID, Rolf Breinbauer
This paper is made freely available by the publisher.
This paper is made freely available by the publisher.

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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 interesting pharmacological target since 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.