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Two-step activity-based protein profiling of diacylglycerol lipase

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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

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Publication details

The article was received on 25 Jun 2018, accepted on 09 Jul 2018 and first published on 13 Jul 2018


Article type: Communication
DOI: 10.1039/C8OB01499J
Citation: Org. Biomol. Chem., 2018, Advance Article
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    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, Advance Article , DOI: 10.1039/C8OB01499J

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