Ligand modulation of the Epstein-Barr virus-induced seven-transmembrane receptor EBI2: identification of a potent and efficacious inverse agonist
T Benned-Jensen, C Smethurst, PJ Holst… - Journal of Biological …, 2011 - jbc.org
The Epstein-Barr virus-induced receptor 2 (EBI2) is a constitutively active seven-
transmembrane receptor, which was recently shown to orchestrate the positioning of B cells
in the follicle. To date, no ligands, endogenously or synthetic, have been identified that
modulate EBI2 activity. Here we describe an inverse agonist, GSK682753A, which
selectively inhibited the constitutive activity of EBI2 with high potency and efficacy. In cAMP-
response element-binding protein-based reporter and guanosine 5′-3-O-(thio) …
transmembrane receptor, which was recently shown to orchestrate the positioning of B cells
in the follicle. To date, no ligands, endogenously or synthetic, have been identified that
modulate EBI2 activity. Here we describe an inverse agonist, GSK682753A, which
selectively inhibited the constitutive activity of EBI2 with high potency and efficacy. In cAMP-
response element-binding protein-based reporter and guanosine 5′-3-O-(thio) …
