Brand  (β version)

PDB ID: 1L2I

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Ligands
Code Name Style Show Link
CL Chloride ion PoSSuM
ETC (R,R)-5,11-cis-diethyl-5,6,11,12-tetrahydrochrysene-2,8-diol PoSSuM
Non-standard Residues
Code Name Show
CCS Carboxymethylated cysteine
Glycosylation
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Modification
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Structure summary

Code : 1L2I   PDBj   RCSB PDB   PDBe
Header : TRANSCRIPTION RECEPTOR/COACTIVATOR
Title : Human Estrogen Receptor alpha Ligand-binding Domain in Complex with (R,R)-5,11-cis-diethyl-5,6,11,12-tetrahydrochrysene-2,8-diol and a Glucocorticoid Receptor Interacting Protein 1 NR box II Peptide
Release Data : 2002-05-01
Compound :
mol_id molecule chains synonym
1 ESTROGEN RECEPTOR A,B ER-ALPHA, OESTROGEN RECEPTOR ALPHA
fragment: ligand-binding domain (residues 297-554)
mol_id molecule chains synonym
2 GLUCOCORTICOID RECEPTOR-INTERACTING PROTEIN 1 C,D NUCLEAR RECEPTOR COACTIVATOR 2, GRIP1
fragment: NR box II (residues 686-698)
Source :
mol_id organism_scientific organism_common expression_system
1 Homo sapiens  (taxid:9606) Human Escherichia coli  (taxid:562)
expression_system_strain: BL21(DE3)pLysS
expression_system_vector_type: plasmid
expression_system_plasmid: pET23D
mol_id organism_scientific
2
synthetic: yes
other_details: The peptide was chemically synthesized. This sequence occurs naturally in mice.
Authors : Shiau, A.K., Barstad, D., Radek, J.T., Meyers, M.J., Nettles, K.W., Katzenellenbogen, B.S., Katzenellenbogen, J.A., Agard, D.A., Greene, G.L.
Keywords : nuclear receptor, transcription factor, estrogen, agonist, coactivator, TRANSCRIPTION RECEPTOR-COACTIVATOR COMPLEX
Exp. method : X-RAY DIFFRACTION ( 1.95 Å )
Citation :

Structural characterization of a subtype-selective ligand reveals a novel mode of estrogen receptor antagonism.

Shiau, A.K.,Barstad, D.,Radek, J.T.  et al.
(2002)  Nat.Struct.Biol.  9 : 359 - 364

PubMed: 11953755

The Structural Basis of Estrogen Receptor/Coactivator Recognition and the Antagonism of this Interaction by Tamoxifen

Shiau, A.K.,Barstad, D.,Loria, P.M.  et al.
(1998)  Cell(Cambridge,Mass.)  95 : 927 - 937

DOI: 10.1016/S0092-8674(00)81717-1

Estrogen Receptor Subtype-selective Ligands: Asymmetric Synthesis and Biological Evaluation of cis- and trans-5,11-dialkyl-5,6,11,12-tetrahydrochrysenes

Meyers, M.J.,Sun, J.,Carlson, K.E.  et al.
(1999)  J.Med.Chem.  42 : 2456 - 2468

DOI: 10.1021/jm990101b

Reaction

Chain : A, B
UniProt : P03372 (ESR1_HUMAN)
Reaction : -
Chain : C, D
UniProt : Q61026 (NCOA2_MOUSE)
Reaction : -