DAGLβ Inhibition Perturbs a Lipid Network Involved in Macrophage Inflammatory Responses

@inproceedings{Hsu2012DAGLIP,
  title={DAGLβ Inhibition Perturbs a Lipid Network Involved in Macrophage Inflammatory Responses},
  author={Ku-Lung Hsu and Katsunori Tsuboi and Alexander Adibekian and Holly M Pugh and Kim R Masuda and Benjamin F Cravatt},
  booktitle={Nature chemical biology},
  year={2012}
}
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 negative-control and activity-based probes, for the functional analysis of DAGLβ in living systems. Optimized inhibitors showed high selectivity for DAGLβ over other serine hydrolases, including DAGL… CONTINUE READING