Two-step activity-based protein profiling of diacylglycerol lipase

Eva J. Van Rooden, Roy Kreekel, Thomas Hansen, Antonius P.A. Janssen, Annelot C.M. Van Esbroeck, Hans Den Dulk, Richard J.B.H.N. Van Den Berg, Jeroen D.C. Codée, Mario Van Der Stelt*

*Corresponding author for this work

Research output: Contribution to JournalArticleAcademicpeer-review


Diacylglycerol lipases (DAGL) produce the endocannabinoid 2-arachidonoylglycerol, a key modulator of neurotransmitter release. Chemical tools that visualize endogenous DAGL activity are desired. Here, we report the design, synthesis and application of a triazole urea probe for DAGL equipped with a norbornene as a biorthogonal handle. The activity and selectivity of the probe was assessed with activity-based protein profiling. This probe was potent against endogenous DAGLα (IC50 = 5 nM) and it was successfully applied as a two-step activity-based probe for labeling of DAGLα using an inverse electron-demand Diels-Alder ligation in living cells.

Original languageEnglish
Pages (from-to)5250-5253
Number of pages4
JournalOrganic and Biomolecular Chemistry
Issue number29
Publication statusPublished - 1 Jan 2018


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