877309-59-6Relevant academic research and scientific papers
Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors
Kettle, Jason G.,Anjum, Rana,Barry, Evan,Bhavsar, Deepa,Brown, Crystal,Boyd, Scott,Campbell, Andrew,Goldberg, Kristin,Grondine, Michael,Guichard, Sylvie,Hardy, Christopher J.,Hunt, Tom,Jones, Rhys D. O.,Li, Xiuwei,Moleva, Olga,Ogg, Derek,Overman, Ross C.,Packer, Martin J.,Pearson, Stuart,Schimpl, Marianne,Shao, Wenlin,Smith, Aaron,Smith, James M.,Stead, Darren,Stokes, Steve,Tucker, Michael,Ye, Yang
supporting information, p. 8797 - 8810 (2018/10/05)
While the treatment of gastrointestinal stromal tumors (GISTs) has been revolutionized by the application of targeted tyrosine kinase inhibitors capable of inhibiting KIT-driven proliferation, diverse mutations to this kinase drive resistance to establish
Two-step activity-based protein profiling of diacylglycerol lipase
Van Rooden, Eva J.,Kreekel, Roy,Hansen, Thomas,Janssen, Antonius P. A.,Van Esbroeck, Annelot C. M.,Den Dulk, Hans,Van Den Berg, Richard J. B. H. N.,Codée, Jeroen D. C.,Van Der Stelt, Mario
supporting information, p. 5250 - 5253 (2018/08/03)
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.
