| http://purl.uniprot.org/citations/24678947 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/24678947 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/24678947 | http://www.w3.org/2000/01/rdf-schema#comment | "Oxysterols have recently been identified as natural ligands for a G protein-coupled receptor called EBI2 (aka GPR183) ( Nature 2011 , 475 , 524 ; 519 ). EBI2 is highly expressed in immune cells ( J. Biol. Chem. 2006 , 281 , 13199 ), and its activation has been shown to be critical for the adaptive immune response and has been genetically linked to autoimmune diseases such as type I diabetes ( Nature 2010 , 467 , 460 ). Here we describe the isolation of a potent small molecule antagonist for the EBI2 receptor. First, we identified a small molecule agonist NIBR51 (1), which enabled identification of inhibitors of receptor activation. One antagonist called NIBR127 (2) was used as a starting point for a medicinal chemistry campaign, which yielded NIBR189 (4m). This compound was extensively characterized in binding and various functional signaling assays. Furthermore, we have used 4m to block migration of a monocyte cell line called U937, suggesting a functional role of the oxysterol/EBI2 pathway in these immune cells."xsd:string |
| http://purl.uniprot.org/citations/24678947 | http://purl.org/dc/terms/identifier | "doi:10.1021/jm4019355"xsd:string |
| http://purl.uniprot.org/citations/24678947 | http://purl.org/dc/terms/identifier | "doi:10.1021/jm4019355"xsd:string |
| http://purl.uniprot.org/citations/24678947 | http://purl.uniprot.org/core/author | "Rosenkilde M.M."xsd:string |
| http://purl.uniprot.org/citations/24678947 | http://purl.uniprot.org/core/author | "Rosenkilde M.M."xsd:string |
| http://purl.uniprot.org/citations/24678947 | http://purl.uniprot.org/core/author | "Sailer A.W."xsd:string |
| http://purl.uniprot.org/citations/24678947 | http://purl.uniprot.org/core/author | "Sailer A.W."xsd:string |
| http://purl.uniprot.org/citations/24678947 | http://purl.uniprot.org/core/author | "Yin H."xsd:string |
| http://purl.uniprot.org/citations/24678947 | http://purl.uniprot.org/core/author | "Yin H."xsd:string |
| http://purl.uniprot.org/citations/24678947 | http://purl.uniprot.org/core/author | "Chen Y.A."xsd:string |
| http://purl.uniprot.org/citations/24678947 | http://purl.uniprot.org/core/author | "Chen Y.A."xsd:string |
| http://purl.uniprot.org/citations/24678947 | http://purl.uniprot.org/core/author | "Laurent S."xsd:string |
| http://purl.uniprot.org/citations/24678947 | http://purl.uniprot.org/core/author | "Laurent S."xsd:string |
| http://purl.uniprot.org/citations/24678947 | http://purl.uniprot.org/core/author | "Seuwen K."xsd:string |
| http://purl.uniprot.org/citations/24678947 | http://purl.uniprot.org/core/author | "Seuwen K."xsd:string |
| http://purl.uniprot.org/citations/24678947 | http://purl.uniprot.org/core/author | "Preuss I."xsd:string |
| http://purl.uniprot.org/citations/24678947 | http://purl.uniprot.org/core/author | "Preuss I."xsd:string |
| http://purl.uniprot.org/citations/24678947 | http://purl.uniprot.org/core/author | "Endres R."xsd:string |
| http://purl.uniprot.org/citations/24678947 | http://purl.uniprot.org/core/author | "Endres R."xsd:string |
| http://purl.uniprot.org/citations/24678947 | http://purl.uniprot.org/core/author | "Gessier F."xsd:string |
| http://purl.uniprot.org/citations/24678947 | http://purl.uniprot.org/core/author | "Gessier F."xsd:string |
| http://purl.uniprot.org/citations/24678947 | http://purl.uniprot.org/core/author | "Marsilje T.H."xsd:string |
| http://purl.uniprot.org/citations/24678947 | http://purl.uniprot.org/core/author | "Marsilje T.H."xsd:string |