Words similar to coactivator
Example sentences for: coactivator
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Decreased growth factor and growth factor receptor expression has been proposed as a potential growth inhibitory mechanism [ 14 ] . Additionally, RA mediated inhibition of AP-1 activity is believed to be important in cellular growth control by this ligand [ 13 ] . AP-1 inhibition via direct interaction between RARs and AP-1 proteins has been proposed [ 16 ] . RA inhibition of jun N-terminal kinase was shown to prevent c-jun phosphorylation, resulting in decreased AP-1 activity [ 17 ] . Competition between RAR and AP-1 for limiting amounts of the nuclear receptor coactivator CBP may also account for decreases in AP-1 transcriptional activity [ 5 ] . In the present study we have described a new mechanism by which RA can inhibit cellular proliferation.
Cells transfected with either coactivator or Stat3C showed comparable and higher luciferase activity in response to R1881 than cells treated with hormone alone in the presence of empty vector (Fig.
The unliganded LBD recognizes hydrophobic motifs, termed interaction domains (IDs), which are reiterated three times in N-CoR and twice in SMRT and conform to the consensus L/IXXIIXXXL [ 4 ] (see also [ 16 ] ). By contrast, the liganded LBD binds shorter hydrophobic motifs termed NR boxes that are reiterated several times within each coactivator and conform to the consensus LXXLL.
The LBD utilizes a large hydrophobic cleft composed of residues along H3 and H5 to bind IDs [ 17 ] , and a smaller hydrophobic cleft that is composed of residues in the upper part of H3 and H5 and H12 (and corresponds to AF-2) to bind NR boxes [ 18 ] . Thus, agonists promote coregulator exchange by promoting the packing of H12 over the lower part of the ID binding region, an event that simultaneously completes the coactivator binding surface.
The effect of ligands on coactivator binding was evaluated using the BIAcore instrument as described [ 25 26 ] . For interaction of CAR, RXR and CAR/RXR heterodimer with SRC-3, a GST-SRC-3 fusion protein containing the receptor interaction domain of the coactivator was expressed in bacteria and purified.
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