DAGL[beta] inhibition perturbs a lipid network involved in macrophage inflammatory responses

• Published in: Nature chemical biology Vol. 8; no. 12; p. 999
• Main Authors: Hsu, Ku-lung, Tsuboi, Katsunori, Adibekian, Alexander, Pugh, Holly, Masuda, Kim, Cravatt, Benjamin F
• Format: Journal Article
• Language: English
• Published: Cambridge Nature Publishing Group 01.12.2012
• Subjects: Biosynthesis; Enzymes; Inactivation; Inhibitors; Lipids; Molecular chemistry; Probes; Rodents; Urea

The endocannabinoid 2-arachidonoylglycerol (2-AG) is biosynthesized by diacylglycerol lipases DAGLα and DAGLβ. Chemical probes to perturb DAGLs are needed to characterize endocannabinoid function in biological processes. Here we report a series of 1,2,3-triazole urea inhibitors, along with paired ne...