Acute treatment with chemical PPARGC1a1 activators in brown fat cells

The peroxisome proliferator-activated receptor-coactivator-11 (PGC-11) regulates genes involved in energy metabolism. Increasing adipose tissue energy expenditure through PGC-11 activation has been suggested to be beneficial for systemic metabolism. Pharmacological PGC-11 activators could be valuable tools in the fight against obesity and metabolic disease. Finding such compounds has been challenging partly because PGC-11 is a transcriptional coactivator with no known ligand-binding activities. Importantly, PGC-11 activation is regulated by several mechanisms but protein stabilization is a limiting step as the protein has a short half-life under unstimulated conditions.

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Pettersson-Klein AT, Izadi M, Ferreira DMS, Cervenka I, Correia JC, Martinez-Redondo V, Southern M, Cameron M, Kamenecka T, Agudelo LZ, Porsmyr-Palmertz M, Martens U, Lundgren B, Otrocka M, Jenmalm-Jensen A, Griffin PR, Ruas JL