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Mayer, N; Schweiger, M; Romauch, M; Grabner, GF; Eichmann, TO; Fuchs, E; Ivkovic, J; Heier, C; Mrak, I; Lass, A; Höfler, G; Fledelius, C; Zechner, R; Zimmermann, R; Breinbauer, R.
Development of small-molecule inhibitors targeting adipose triglyceride lipase.
Nat Chem Biol. 2013; 9(12):785-7
Doi: 10.1038/nchembio.1359
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- Co-authors Med Uni Graz
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Eichmann Thomas
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Grabner Gernot
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Höfler Gerald
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Romauch Matthias
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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 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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