Development of small molecule inhibitors targeting adipose triglyceride lipase

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....

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Detalles Bibliográficos
Autores principales: Mayer, Nicole, Schweiger, Martina, Romauch, Matthias, Grabner, Gernot F., Eichmann, Thomas O., Fuchs, Elisabeth, Ivkovic, Jakov, Heier, Christoph, Mrak, Irina, Lass, Achim, Höfler, Gerald, Fledelius, Christian, Zechner, Rudolf, Zimmermann, Robert, Breinbauer, Rolf
Formato: Online Artículo Texto
Lenguaje:English
Publicado: 2013
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3829776/
https://www.ncbi.nlm.nih.gov/pubmed/24096302
http://dx.doi.org/10.1038/nchembio.1359
Descripción
Sumario: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.

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