2jf9 | pdb_00002jf9

ESTROGEN RECEPTOR ALPHA LBD IN COMPLEX WITH A TAMOXIFEN-SPECIFIC PEPTIDE ANTAGONIST

spinqualitylabelsall models 2jf9, resolution 2.10Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 2jf9 is a 6 chain structure with sequence from Human. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: BCT, CA, EDO, OHT Related: 1a52, 1akf, 1ere, 1err, 1g50, 1gwq, 1gwr, 1hcp, 1hcq, 1l2i, 1pcg, 1qkt, 1qku, 1r5k, 1sj0, 1uom, 1x7e, 1x7r, 1xp1, 1xp6, 1xp9, 1xpc, 1xqc, 1yim, 1yin, 1zky, 2ayr, 2b1v, 2bj4, 2fai, 3erd, 3ert, 2jfa Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Evolutionary Conservation Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf. Publication Abstract from PubMed Direct recruitment of transcriptional corepressors to estrogen receptors (ER) is thought to contribute to the tissue-specific effects of clinically important ER antagonists. Here, we present the crystal structures of two affinity-selected peptides in complex with antagonist-bound ERalpha ligand-binding domain. Both peptides adopt helical conformations, bind along the activation function 2 coregulator interaction surface, and mimic corepressor (CoRNR) sequence motif binding. Peptide binding is weak in a wild-type context but significantly enhanced by removal of ER helix 12. This region contains a previously unrecognized CoRNR motif that is able to compete with corepressors for binding to activation function 2, thereby providing a structural explanation for the poor ability of ER to directly interact with classical corepressors. Furthermore, the ability of other sequence motifs to mimic corepressor binding raises the possibility that coregulators do not necessarily require CoRNR motifs for direct recruitment to antagonist-bound ER. Structural insights into corepressor recognition by antagonist-bound estrogen receptors.,Heldring N, Pawson T, McDonnell D, Treuter E, Gustafsson JA, Pike AC J Biol Chem. 2007 Apr 6;282(14):10449-55. Epub 2007 Feb 5. PMID:17283072 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Estrogen receptor 3D structures

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