Two-step activity-based protein profiling of diacylglycerol lipase?
Organic & Biomolecular Chemistry Pub Date: 2018-07-13 DOI: 10.1039/C8OB01499J
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.
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Journal Name：Organic & Biomolecular Chemistry
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CAS no.: 89640-58-4
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