Estrogen receptor
Estrogen receptors (ER) are activated by the hormone estrogen (EST). The activated ER binds DNA and regulates the activity of many genes. There are 2 forms of ER: α and β and ER dimers can be of αα, ββ and αβ. ER is composed of 5 domains: N terminal A/B domain can transactivate transcription without binding estrogen; C domain (DBD) binds to Estrogen response elements of DNA; D domain is a hinge region; E domain is ligand binding (LBD) as well as binding the coactivator and corepressor proteins and transactivates gene transcription.
3D structures of estrogen receptor3D structures of estrogen receptor
Estrogen receptor α ligand binding domain
3ltx - ERα LBD – pacific oyster
1a52, 1g50 - hERα LBD - human
1ere, 1qku - hERα LBD + EST
1qkt - hERα LBD (mutant) + EST
1uom, 2ayr, 2q70, 2qe4, 2pog, 2r6w, 2r6y, 2qxs - hERα LBD (mutant) + ligand
1err, 3ert, 1sj0, 1yim, 1r5k, 1xp1, 1xp6, 1xp9, 1xpc, 1xqc, 1yin, 2ouz, 2iog, 2iok, 3dt3, 3os8, 3os9, 3osa - hERα LBD + ligand
2bj4, 2jf9, 2jfa - hERα LBD + peptide antagonist
2yja - hERα LBD + stapled peptide
2yat - hERα LBD (mutant) + EST derivative
ERα LBD ternary complex with steroid receptor coactivator peptide
2b23 - hERα LBD (mutant) + nuclear receptor coactivator peptide
3erd, 1l2i - hERα LBD + nuclear receptor coactivator peptide + nonsteroidal EST
1gwr - hERα LBD + nuclear receptor coactivator peptide + EST
3q95 - hERα LBD (mutant) + nuclear receptor coactivator peptide + EST
2g5o - hERα LBD + nuclear receptor coactivator peptide + EST derivative
2p15, 2qgt - hERα LBD (mutant) + nuclear receptor coactivator peptide + EST derivative
1gwq, 1x7e, 2fai, 2g44, 2q6j, 2qzo - hERα LBD + nuclear receptor coactivator peptide + ligand
1zky, 2b1v, 2b1z, 2qa6, 2qab, 2qgw, 2qh6, 2qr9, 2qse, 2qxm, 3hlv, 3hm1, 3l03, 3q97, 3dma - hERα LBD (mutant) + nuclear receptor coactivator peptide + ligand
1x7r - hERα LBD + steroid receptor coactivator peptide + genistein
2qa8 - hERα LBD (mutant) + steroid receptor coactivator peptide + genistein
2ocf - hERα LBD (mutant) + fibronectin domain 10 + EST
Estrogen receptor β ligand binding domain
1qkm - hERβ LBD + genistein
1qkn, 1hj1 - ERβ LBD + ligand – rat
1nde, 1u3q, 1u3r, 1u3s, 2giu, 2i0g, 2i0j, 2jj3, 2z4b, 2qtu - hERβ LBD + ligand
2fsz - hERβ LBD (mutant) + ligand
2yja - hERβ LBD + stapled peptide
ERβ LBD ternary complex with steroid receptor coactivator peptide
1l2j - hERβ LBD + steroid receptor coactivator peptide + nonsteroidal EST
2j7x, 3oll, 3ols - hERβ LBD + steroid receptor coactivator peptide + EST
1u9e - hERβ LBD + steroid receptor coactivator peptide
1x76, 1x78, 1x7b, 1yy4, 1yye, 1zaf, 2j7y, 2nv7, 3omo, 3omp, 3omq - hERβ LBD + steroid receptor coactivator peptide + ligand
1x7j - hERβ LBD + steroid receptor coactivator peptide + genistein
Estrogen receptor α DNA binding domain