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Publication and contact information

Endocrine/metabolic disease

Dyslipidemia; metabolic disease

Patatin-like phospholipase domain containing 2 (PNPLA2; ATGL)

In vitro and mouse studies have identified an inhibitor of ATGL that might help treat dyslipidemia and metabolic disorders. Lead optimization of lipase inhibitors yielded a compound that inhibited ATGL with an IC50 of about 700 nM. In lysates from ATGL-overexpressing Escherichia coli and mouse white adipose tissue, the ATGL inhibitor decreased triglyceride hydrolase activity compared with vehicle. In fasted mice, the inhibitor produced a time- and concentration-dependent decrease in the release of fatty acids and glycerol compared with vehicle. Next steps include optimizing the inhibitor for human ATGL and testing it in diet-induced models of metabolic disease.

SciBX 6(46); doi:10.1038/scibx.2013.1321
Published online Dec. 5, 2013

Patent application filed; available for licensing

Mayer, N. et al. Nat. Chem. Biol.; published online Oct. 6, 2013;
Contact: Rolf Breinbauer,
Graz University of Technology,
Graz, Austria

Contact: Robert Zimmermann, same affiliation as above