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Diacylglycerol lipase-b (DAGLB); tumor necrosis factor-a (TNF-a)

Mouse and in vitro studies suggest inhibiting DAGLB could help prevent inflammation. In vitro studies identified a 1,2,3-triazole urea-based molecule that selectively inhibited the serine hydrolase DAGLB with midnanomolar IC50 values. In mice, the DAGLB inhibitor decreased levels of arachidonic acid-derived prostaglandins in macrophages compared with an inactive control compound. In lipopolysaccharide (LPS)-stimulated macrophages isolated from DAGLB inhibitor-treated mice, Tnf-a production was lower than that in macrophages obtained from mice treated with the control compound. Next steps include looking at the phenotype of pharmacological and genetic disruption of DAGLB models of inflammation and optimizing DAGLB, DAGLA, and dual DAGLB and DAGLA inhibitors.
Corresponding author Benjamin Cravatt is a founder of Abide Therapeutics Inc., which is developing serine hydrolase inhibitors.

SciBX 5(46); doi:10.1038/scibx.2012.1211
Published online Nov. 29, 2012

Patented; licensed to an undisclosed company

Hsu, K.-L. et al. Nat. Chem. Biol.; published online Oct. 28, 2012;
Contact: Benjamin F. Cravatt, The Scripps Research Institute, La Jolla, Calif.