Obesity is characterised by an oversupply of lipids and consequent metabolic dysfunctions, increasing the risk of developing comorbidities such as type 2 diabetes and nonalcoholic fatty liver disease. Lipid droplets (LDs) are dynamic storage organelles for lipids and are enveloped with a wide array of proteins that control lipid metabolism. A subset of LD proteins are involved in lipolysis and are regulated at the posttranslational level by protein kinase A (PKA)-mediated phosphorylation, key of which are adipose triglyceride lipase (ATGL), and perilipin 5 (PLIN5). 17β-hydroxysteroid dehydrogenase 11 (HSD17β11) is a lipid droplet-associated protein whose deletion results in defects in lipolysis and resulting cellular lipid accumulation. Notably, HSD17β11 contains a conserved PKA consensus sites on its serine-33 residue.
Here, we sought to identify PKA phosphorylation sites on HSD17β11 and test whether S33 is a functionally important site for its role in lipid metabolism. To address this aim, we generated a loss of function serine-to-alanine mutant of HSD17β11 at serine-33 (HSD17β11S33A) by re-expression of mutant protein in HSD17β11KO HEK293T cells. Metabolic studies were then performed in HSD17β11S33A and cells expressing wild-type HSD17β11 (HSD17β11FLAG).
Radiometric tracing studies revealed an increase in lipolysis in HSD17β1lS33A cells, with a slight reduction in LD size compared to HSD17β11FLAG cells. Mechanistically, FLIM-FRET analysis revealed a robust interaction between HSD17β11 and PLIN5, which was reduced in response to forskolin stimulation. We then show phosphorylation of HSD17β11 at serine-33 results in ubiquitination and degradation of the protein, and that this effect was ameliorated in HSD17β11S33A cells. Taking this into consideration, our findings suggest that HSD17β11 is a novel regulator of lipolysis, and hence lipid metabolism.