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|3ert, resolution 1.90Å ()|
|Gene:||ESTROGEN RECEPTOR ALPHA (Homo sapiens)|
HUMAN ESTROGEN RECEPTOR ALPHA LIGAND-BINDING DOMAIN IN COMPLEX WITH 4-HYDROXYTAMOXIFEN
Ligand-dependent activation of transcription by nuclear receptors (NRs) is mediated by interactions with coactivators. Receptor agonists promote coactivator binding, and antagonists block coactivator binding. Here we report the crystal structure of the human estrogen receptor alpha (hER alpha) ligand-binding domain (LBD) bound to both the agonist diethylstilbestrol (DES) and a peptide derived from the NR box II region of the coactivator GRIP1 and the crystal structure of the hER alpha LBD bound to the selective antagonist 4-hydroxytamoxifen (OHT). In the DES-LBD-peptide complex, the peptide binds as a short alpha helix to a hydrophobic groove on the surface of the LBD. In the OHT-LBD complex, helix 12 occludes the coactivator recognition groove by mimicking the interactions of the NR box peptide with the LBD. These structures reveal the two distinct mechanisms by which structural features of OHT promote this "autoinhibitory" helix 12 conformation.
The structural basis of estrogen receptor/coactivator recognition and the antagonism of this interaction by tamoxifen., Shiau AK, Barstad D, Loria PM, Cheng L, Kushner PJ, Agard DA, Greene GL, Cell. 1998 Dec 23;95(7):927-37. PMID:9875847
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
About this Structure
3ert is a 1 chain structure with sequence from Homo sapiens. This structure supersedes the now removed PDB entry 2ert. The September 2003 RCSB PDB Molecule of the Month feature on Estrogen Receptor by David S. Goodsell is 10.2210/rcsb_pdb/mom_2003_9. Full crystallographic information is available from OCA.
- Shiau AK, Barstad D, Loria PM, Cheng L, Kushner PJ, Agard DA, Greene GL. The structural basis of estrogen receptor/coactivator recognition and the antagonism of this interaction by tamoxifen. Cell. 1998 Dec 23;95(7):927-37. PMID:9875847