Effects of ligand structure on EBI2 activation

The potency and efficacy of 7α,25-OHC, 7α,27-OHC, and 7α,27-dihydroxy-4-cholesten-3-one in activating EBI2 in [35S]GTPγS binding assays were compared. EC50 values are the concentrations of compounds that stimulated 50% of the maximal response of wild-type EBI2. Emax values are expressed as percentages of the maximal response of wild-type EBI2 activated by 7α,25-OHC. The assays were performed in triplicate, and values represent mean ± S.E.M.

nM% of wild-type response
7α,25-OHC0.11 ± 0.03100
7α,27-OHC0.97 ± 0.2480.84 ± 4.62
  • N.D., not determined, because the assay did not reach saturation.