Issue 29, 2018

Two-step activity-based protein profiling of diacylglycerol lipase

Abstract

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.

Graphical abstract: Two-step activity-based protein profiling of diacylglycerol lipase

Supplementary files

Article information

Article type
Communication
Submitted
25 Jun 2018
Accepted
09 Jul 2018
First published
13 Jul 2018

Org. Biomol. Chem., 2018,16, 5250-5253

Two-step activity-based protein profiling of diacylglycerol lipase

E. J. van Rooden, R. Kreekel, T. Hansen, A. P. A. Janssen, A. C. M. van Esbroeck, H. den Dulk, R. J. B. H. N. van den Berg, J. D. C. Codée and M. van der Stelt, Org. Biomol. Chem., 2018, 16, 5250 DOI: 10.1039/C8OB01499J

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