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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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
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author 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
author_facet 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
author_sort Mayer, Nicole
collection PubMed
description 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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spelling pubmed-38297762014-06-01 Development of small molecule inhibitors targeting adipose triglyceride lipase 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 Nat Chem Biol Article 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. 2013-10-06 2013-12 /pmc/articles/PMC3829776/ /pubmed/24096302 http://dx.doi.org/10.1038/nchembio.1359 Text en Users may view, print, copy, download and text and data- mine the content in such documents, for the purposes of academic research, subject always to the full Conditions of use: http://www.nature.com/authors/editorial_policies/license.html#terms
spellingShingle Article
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
Development of small molecule inhibitors targeting adipose triglyceride lipase
title Development of small molecule inhibitors targeting adipose triglyceride lipase
title_full Development of small molecule inhibitors targeting adipose triglyceride lipase
title_fullStr Development of small molecule inhibitors targeting adipose triglyceride lipase
title_full_unstemmed Development of small molecule inhibitors targeting adipose triglyceride lipase
title_short Development of small molecule inhibitors targeting adipose triglyceride lipase
title_sort development of small molecule inhibitors targeting adipose triglyceride lipase
topic Article
url 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
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