918793-01-8Relevant articles and documents
Selective Photoaffinity Probe That Enables Assessment of Cannabinoid CB2 Receptor Expression and Ligand Engagement in Human Cells
Soethoudt, Marjolein,Stolze, Sara C.,Westphal, Matthias V.,Van Stralen, Luuk,Martella, Andrea,Van Rooden, Eva J.,Guba, Wolfgang,Varga, Zoltan V.,Deng, Hui,Van Kasteren, Sander I.,Grether, Uwe,Ijzerman, Adriaan P.,Pacher, Pal,Carreira, Erick M.,Overkleeft, Herman S.,Ioan-Facsinay, Andreea,Heitman, Laura H.,Van Der Stelt, Mario
supporting information, p. 6067 - 6075 (2018/05/26)
Chemical tools and methods that report on G protein-coupled receptor (GPCR) expression levels and receptor occupancy by small molecules are highly desirable. We report the development of LEI121 as a photoreactive probe to study the type 2 cannabinoid receptor (CB2R), a promising GPCR to treat tissue injury and inflammatory diseases. LEI121 is the first CB2R-selective bifunctional probe that covalently captures CB2R upon photoactivation. An incorporated alkyne serves as ligation handle for the introduction of reporter groups. LEI121 enables target engagement studies and visualization of endogenously expressed CB2R in HL-60 as well as primary human immune cells using flow cytometry. Our findings show that strategically functionalized probes allow monitoring of endogenous GPCR expression and engagement in human cells using tandem photoclick chemistry and hold promise as biomarkers in translational drug discovery.
BIARYL KINASE INHIBITORS
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Page/Page column 288; 289, (2017/05/07)
The present disclosure is directed to biaryl compounds of formula (I) which can inhibit AAKl (adaptor associated kinase 1), compositions comprising such compounds and their use for treating e.g. pain, Alzheimer's disease, Parkinson's disease and schizophrenia.
FUNGICIDE HYDROXIMOYL-TETRAZOLE DERIVATIVES
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Page/Page column 82, (2009/10/22)
The present invention relates to hydroximoyl-tetrazole derivatives, their process of preparation, preparation intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of p