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Gene Regulation, Bone, and Inflammation Research Lilly Research Laboratories Lilly Corporate Center Indianapolis, Indiana 46285
Nuclear receptors (NRs) require coactivators to
efficiently activate transcription of their target genes. Many
coactivators including the p160 proteins utilize a short NR box motif
to recognize the ligand-binding domain of the NR when it is activated
by ligand. To investigate the ability of various ligands to specify the
affinity of NR boxes for a ligand-bound NR, we compared the capacity of
p160 NR boxes to be recruited to estrogen receptor (ER
) and ERß in
the presence of 17ß-estradiol, diethylstilbestrol, and genestein. A
time-resolved fluorescence-based binding assay was used to determine
the dissociation constants for the 10 NR boxes derived from the three
p160 coactivators for both ER subtypes in the presence of the each of
the agonists. While the affinity of some NR boxes for ER was
independent of the agonist, we identified several NR boxes that had
significantly different affinities for ER depending on which agonist
was bound to the receptor. Therefore, an agonist may specify the
affinity of an NR for various NR boxes and thus regulate the
coactivator selectivity of the receptor.
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