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Sentences for "corepressor "
However, additional studies suggest that corepressor binding to the apo-RAR component of the heterodimer blocks rexinoid induced binding of coactivators to RXR [ 7 ] .
The NRs regulate transcription by binding to response elements in the promoters of target genes and acting as scaffolds for the assembly of large coactivator and corepressor complexes [ 4 ] .
Both N-CoR and SMRT repress transcription, at least in part, by binding to histone de-acetylases (HDACs) either directly or indirectly through other corepressor complex components.
Generally, NR transcriptional activity is dictated by the balance between coactivator and corepressor recruitment, and one of the most important factors that influences this balance is the absence or presence of agonist ligands (reviewed in [ 4 ] ).
Unliganded NRs such as thyroid (TRs) and retinoid receptors (RARs) bind corepressors, and ligand promotes release of corepressor and subsequent binding of coactivators.
In other cases, however, the balance of coactivator and corepressor recruitment is regulated by direct competition for the AF-2 surface, rather than ligand-dependent coregulator exchange.
Similar agonist-dependent interactions could be observed between ERß and the alternate NR corepressor SMRT in vitro (Fig.
Conclusions NRs generally interact with the corepressors N-CoR and SMRT either in the absence of ligand, or in the presence of receptor antagonists, and agonists promote corepressor release [ 4 ] .
Our attempts to identify ERß mutants that differentiate between GRIP1 and N-CoR binding to analyze the role of agonist-dependent corepressor binding have not yet been successful (probably because ERß utilizes the same surface to bind both cofactors).
The finding that estrogens suppress N-CoR binding to ER?
[ 39 ] , but promote N-CoR binding to ERß represents the first demonstration of a corepressor that shows completely distinct modes of hormone-dependent interaction with the ER isoforms.
Consistent with this notion, the apparent weak transcriptional activity of the ERß LBD is a consequence of corepressor HDAC activity at some level (Fig.
LBD Ligand binding domain NR Nuclear receptor NTD Amino terminal domain N-CoR Nuclear receptor corepressor PBS Phosphate buffered saline PCR Polymerase chain reaction PERC PGC-1 related estrogen receptor coactivator PGC-1 Peroxisome proliferator activated receptor gamma coactivator 1.
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