Corepressors in ER Physiology and Pharmacology
Compressor | Full Name | Function/Activity | Repression of ER | Interaction with ER |
---|---|---|---|---|
NCoR | Nuclear receptor corepressor | HDAC (Histone deacetylase) | Pharmacological | Binds ERs AF-2 through CoRNR box motifs |
SMRT | Silencing mediator for retinoid and thyroid receptors | HDAC | Pharmacological | Binds ERs AF-2 through CoRNR box motifs |
RIP140 (NRIP) | Receptor interacting protein of 140 kDa | Competes for AF-2 coactivator binding; associates with HDACs | Physiological and Pharmacological | Binds ERs AF-2 through LXXLL motifs |
REA | Repressor of estrogen receptor activity | Interferes with SRC-1 access to the ERs | Physiological | Indirect |
RTA | Repressor of tamoxifen transcriptional activity | Interferes with SRC-1 access to the ERs RNA binding; represses tamoxifen agonist activity through ERα | Pharmacological | Binds ER AF-1 |
mSiah2 | Mammalian homolog of Drosophila Seven in absentia (sina) | Mediates cell-specific repression of NRs by targeting NCoR for proteasomal degradation | Pharmacological | Associates with ER indirectly through binding NCoR |