Medizinische Universität Graz - Research portal
Selected Publication:
SHR Neuro Cancer Cardio Lipid Metab Microb
Mayer, N; Schweiger, M; Fuchs, E; Migglautsch, AK; Doler, C; Grabner, GF; Romauch, M; Melcher, MC; Zechner, R; Zimmermann, R; Breinbauer, R.
Structure-activity relationship studies for the development of inhibitors of murine adipose triglyceride lipase (ATGL).
Bioorg Med Chem. 2020; 28(16): 115610
Doi: 10.1016/j.bmc.2020.115610
Web of Science
PubMed
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- Co-authors Med Uni Graz
- Grabner Gernot
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- Abstract:
- High serum fatty acid (FA) levels are causally linked to the development of insulin resistance, which eventually progresses to type 2 diabetes and non-alcoholic fatty liver disease (NAFLD) generalized in the term metabolic syndrome. Adipose triglyceride lipase (ATGL) is the initial enzyme in the hydrolysis of intracellular triacylglycerol (TG) stores, liberating fatty acids that are released from adipocytes into the circulation. Hence, ATGL-specific inhibitors have the potential to lower circulating FA concentrations, and counteract the development of insulin resistance and NAFLD. In this article, we report about structure-activity relationship (SAR) studies of small molecule inhibitors of murine ATGL which led to the development of Atglistatin. Atglistatin is a specific inhibitor of murine ATGL, which has proven useful for the validation of ATGL as a potential drug target.
- Find related publications in this database (using NLM MeSH Indexing)
- Animals - administration & dosage
- Drug Discovery - administration & dosage
- Enzyme Inhibitors - chemistry, pharmacology
- Lipase - antagonists & inhibitors, chemistry, metabolism
- Lipolysis - drug effects
- Mice - administration & dosage
- Phenylurea Compounds - chemistry, pharmacology
- Structure-Activity Relationship - administration & dosage
- Triglycerides - blood
- Find related publications in this database (Keywords)
- PNPLA2
- Lipolysis
- NAFLD
- Atglistatin
- Small molecule inhibitor