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<StructureSection load='1gwr' size='275' side='right' scene='' caption='Human estrogen receptor-ligand binding domain (grey) complex with transcription intermediate factor-2 peptide (pink) and estradiol (PDB code [[1gwr]])'>
<StructureSection load='1gwr' size='275' side='right' scene='' caption='Human estrogen receptor-ligand binding domain (grey) complex with transcription intermediate factor-2 peptide (pink) and estradiol (PDB code [[1gwr]])'>
[[Image:2yat.png|left|200px|thumb|Crystal structure of estradiol derived metal chelate and estrogen receptor-ligand binding domain complex '''[[2yat]]''']]
[[Image:2yat.png|left|200px|thumb|Crystal structure of estradiol derived metal chelate and estrogen receptor-ligand binding domain complex '''[[2yat]]''']]
{{Clear}}
__TOC__
__TOC__
==Estrogen receptors==  
==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.<br />
(ER) are activated by the hormone estrogen (EST). It is a [[Nuclear receptors|nuclear receptor]]. 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.  The 2 forms differ in the tissues in which they are found.  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.<br />


See also [[Intracellular receptors]]


==Structure of estradiol metal chelate and  estrogen receptor complex: The basis for designing a new class of SERMs <ref>PMID: 21473635</ref>==
==Structure of estradiol metal chelate and  estrogen receptor complex: The basis for designing a new class of SERMs <ref>PMID: 21473635</ref>==
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==Estrogen receptor α complexed with raloxifene and a corepressor peptide==  
==Estrogen receptor α complexed with raloxifene and a corepressor peptide==  
<scene name='Estrogen_receptor/Cv/1'>Click here to see the difference between conformations</scene> of estrogen receptor α complexed with raloxifene and a corepressor peptide (morph was taken from [http://molmovdb.org/cgi-bin/movie.cgi Gallery of Morphs] of the [http://molmovdb.org Yale Morph Server]).  
<scene name='Estrogen_receptor/Cv/1'>Click here to see the difference between conformations</scene> of estrogen receptor α complexed with its modulator [[Raloxifene]] and a corepressor peptide (morph was taken from [http://molmovdb.org/cgi-bin/movie.cgi Gallery of Morphs] of the [http://molmovdb.org Yale Morph Server]).  


==3D structures of estrogen receptor==
==3D structures of estrogen receptor==
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==For more details see==
==For more details see==
[[Hormone]]<br />
[[Ivan Koutsopatriy estrogen receptor]]<br />
[[Ivan Koutsopatriy estrogen receptor]]<br />
[[C-di-GMP receptors with PilZ domain]]<br />
[[C-di-GMP receptors with PilZ domain]]<br />
[[Estrogens]]<br />
For more details on ERβ see [[Student Project 10 for UMass Chemistry 423 Spring 2015]]<br />
For more details on ERβ see [[Student Project 10 for UMass Chemistry 423 Spring 2015]]<br />
For more details on ER-Tamoxifen complex see [[Tamoxifen]].
For more details on ER-Tamoxifen complex see [[Tamoxifen]].


==3D structures of estrogen receptor==
Updated on {{REVISIONDAY2}}-{{MONTHNAME|{{REVISIONMONTH}}}}-{{REVISIONYEAR}}
{{#tree:id=OrganizedByTopic|openlevels=0|
*Estrogen receptor α ligand binding domain residues 245-554
**[[1a52]], [[1g50]] - hERα LBD - human<br />
**[[1ere]], [[1qku]] - hERα LBD + EST<BR />
**[[1qkt]] - hERα LBD (mutant) + EST<BR />
**[[1uom]], [[2ayr]], [[2q70]], [[2qe4]], [[2pog]], [[2r6w]], [[2r6y]], [[2qxs]], [[5u2b]], [[5tn9]], [[5tnb]] - hERα LBD (mutant) + ligand<br />
**[[1err]], [[3ert]], [[1sj0]], [[1yim]], [[1r5k]], [[1xp1]], [[1xp6]], [[1xp9]], [[1xpc]], [[1xqc]], [[1yin]], [[2ouz]], [[2iog]], [[2iok]], [[3dt3]], [[3os8]], [[3os9]], [[3osa]], [[5t92]], [[5t97]] - hERα LBD + ligand<br />
**[[4xi3]] - hERα LBD + bazedoxifene<br />
**[[2bj4]], [[2jf9]], [[2jfa]], [[1pcg]], [[5gtr]], [[5gs4]] - hERα LBD + peptide antagonist<br />
**[[2q6j]], [[2p15]], [[3erd]], [[1l2i]] - hERα LBD + GRIP peptide<br />
**[[6d0f]], [[6czn]] - hERα LBD (mutant) + GRIP peptide<br />
**[[6cbz]], [[5wgq]], [[5wgd]] - hERα LBD (mutant) + GRIP peptide + estradiol<br />
**[[4q13]] - hERα LBD (mutant) + glucocorticoid receptor-interacting protein peptide<br />
**[[5krf]] - hERα LBD (mutant) + peptide + anti-hormone<br />
**[[2yat]] - hERα LBD (mutant) + EST derivative<br />
**[[6iar]], [[6dfn]], [[6df6]] - hERα LBD + antagonist<br />
**[[5fqp]], [[5fqr]], [[5fqs]], [[5fqt]], [[5fqv]], [[5aau]], [[5aav]], [[5acc]], [[5ak2]], [[5di7]], [[5did]], [[5die]], [[5dig]], [[5dk9]], [[5dkb]], [[5dke]], [[5dkg]], [[5dks]], [[5dl4]], [[5dlr]], [[5dmc]], [[5dmf]], [[5dp0]], [[6chz]], [[6chw]], [[6c42]], [[6b0f]], [[5w9d]], [[5ufx]], [[5ufw]] - hERα LBD (mutant) + antagonist<br />
**[[6owc]] - hERα LBD (mutant) + pyridine derivative<br />
**[[4q50]], [[5w9c]] - hERα LBD (mutant) + tamoxifen derivative<br />
**[[3uuc]] - hERα LBD + bisphenol<br />
**[[5t1z]] - hERα LBD + LXXLL motif (mutant) + ethoxy triphenylethylene<br />
**[[1gwr]] - hERα LBD + TIF2 peptide + EST<br />
**[[2ocf]] - hERα LBD (mutant) + fibronectin domain 10 + EST<br />
**[[2yja]] - hERα LBD + NCAO2 peptide<br />
**[[2b23]] - hERα LBD (mutant) + NCAO2 peptide<br />
**[[4n1y]] - ERα LBD – pacific oyster<br />
*''ERα LBD ternary complex with nuclear receptor coactivator 2 peptide (NCAO2)''
**[[2yja]] - hERα LBD + NCAO2 peptide<br />
**[[5hyr]], [[5dx3]], [[5dxb]], [[4pxm]], [[3q95]] - hERα LBD (mutant) + NCAO2 peptide + estradiol<br />
**[[5dxb]] - hERα LBD (mutant) + NCAO2 peptide + stilbestrol derivative<br />
**[[4zn7]] - hERα LBD + NCAO2 peptide + benzylidene estrone<br />
**[[5kri]], [[5krj]], [[5krk]], [[5krl]], [[5krm]], [[5kro]] - hERα LBD (mutant) + NCAO2 peptide + anti-hormone<br />
**[[5egv]], [[ehj]], [[5ei1]], [[5eit]], [[5dxk]], [[5dxe]], [[5dxg]], [[5kro]] - hERα LBD (mutant) + NCAO2 peptide + anti-hormone<br />
**[[5dxe]], [[5dxg]], [[5dxk]], [[5dxm]], [[5dxp]], [[5dxq]], [[5dxr]], [[5dy8]], [[5dyb]], [[5dyd]], [[5dz0]], [[5dz1]], [[5dz3]], [[5dzh]], [[5dzi]], [[5e0w]], [[5e0x]], [[5e14]], [[5e15]], [[5e19]], [[5e1c]], [[5drj]], [[5drm]], [[5dtv]], [[5du5]], [[5due]], [[5dug]], [[5duh]], [[5dvs]], [[5dvv]], [[5dwe]], [[5dwg]], [[5dwi]], [[5dwj]], [[4iu7]], [[4iui]], [[4iv2]], [[4iv4]], [[4ivw]], [[4ivy]], [[4iw6]], [[4iw8]], [[4iwc]], [[4iwf]], [[5u2d]], [[5tld]], [[5tlf]], [[5tlg]], [[5tll]], [[5tlm]], [[5tlo]], [[5tlp]], [[5tlt]], [[5tlu]], [[5tlv]], [[5tlx]], [[5tly]], [[5tm1]], [[5tm2]], [[5tm3]], [[5tm4]], [[5tm5]], [[5tm6]], [[5tm7]], [[5tm8]], [[5tm9]], [[5tml]], [[5tmo]], [[5tmm]], [[5tmq]], [[5tmr]], [[5tms]], [[5tmt]], [[5tmu]], [[5tmv]], [[5tmw]], [[5tmz]], [[5tn1]], [[5tn3]], [[5tn4]], [[5tn5]], [[5tn6]], [[5tn7]], [[5tn8]], [[5ehj]] - hERα LBD (mutant) + NCAO2 peptide + antagonist<br />
**[[5kcf]], [[5kct]], [[5kcu]], [[5kcw]], [[5kd9]], [[5kcc]], [[5kcd]], [[5kce]], [[4zn9]], [[4znh]], [[4zns]], [[4znt]], [[4znu]], [[4znv]], [[4znw]] - hERα LBD (mutant) + NCAO2 peptide + OBHS derivative<br />
**[[5kr9]] - hERα LBD (mutant) + NCAO2 peptide + coumestrol<br />
**[[2g5o]] - hERα LBD + NCAO2 peptide + EST derivative<br />
**[[2qgt]], [[5krh]], [[5krc]], [[5kra]] - hERα LBD (mutant) + NCAO2 peptide + EST derivative<br />
**[[1gwq]], [[2fai]], [[2g44]], [[2qzo]] - hERα LBD + NCAO2 peptide + ligand<br />
**[[3l03]], [[3hm1]], [[3hlv]], [[1zky]], [[2b1v]], [[2b1z]], [[2qa6]], [[2qab]], [[2qgw]], [[2qh6]], [[2qr9]], [[2qse]], [[2qxm]] - hERα LBD (mutant) + NCAO2 peptide + ligand<br />
**[[2qa8]] - hERα LBD (mutant) + NCAO2 peptide + genistein<br />
**[[4pp6]], [[4ppp]], [[4pps]] - hERα LBD (mutant) + NCAO2 peptide  + resveratrol derivative<br />
*''ERα LBD ternary complex with steroid receptor coactivator 1 peptide''
**[[3uu7]], [[3uua]], [[3uud]] - hERα LBD (mutant) + NCAO1 peptide<br />
**[[4dma]] - hERα LBD (mutant) + NCAO1 peptide + inhibitor<br />
**[[4mg5]], [[4mg6]], [[4mg7]], [[4mg8]], [[4mg9]], [[4mga]], [[4mgb]], [[4mgc]], [[4mgd]] - hERα LBD (mutant) + NCAO1 peptide + ligand<br />
**[[4tuz]] - hERα LBD (mutant) + NCAO1 peptide + toxin<br />
**[[4tv1]] - hERα LBD (mutant) + NCAO1 peptide + preservative<br />
**[[5jmm]] - hERα LBD (mutant) + NCAO1 peptide + biochanin<br />
*''ERα LBD ternary complex with steroid receptor coactivator 2 peptide''
**[[2b23]] - hERα LBD (mutant) + NCAO2 peptide<br />
**[[3q95]] - hERα LBD (mutant) + NCAO2 peptide + EST<br />
**[[4iu7]], [[4iui]], [[4iv2]], [[4iv4]], [[4ivw]], [[4ivy]], [[4iw6]], [[4iw8]], [[4iwc]], [[4iwf]], [[5u2d]], [[5tld]], [[5tlf]], [[5tlg]], [[5tll]], [[5tlm]], [[5tlo]], [[5tlp]], [[5tlt]], [[5tlu]], [[5tlv]], [[5tlx]], [[5tly]], [[5tm1]], [[5tm2]], [[5tm3]], [[5tm4]], [[5tm5]], [[5tm6]], [[5tm7]], [[5tm8]], [[5tm9]], [[5tml]], [[5tmo]], [[5tmm]], [[5tmq]], [[5tmr]], [[5tms]], [[5tmt]], [[5tmu]], [[5tmv]], [[5tmw]], [[5tmz]], [[5tn1]], [[5tn3]], [[5tn4]], [[5tn5]], [[5tn6]], [[5tn7]], [[5tn8]] - hERα LBD (mutant) + NCAO2 peptide + inhibitor<br />
**[[2g5o]] - hERα LBD + NCAO2 peptide + EST derivative<br />
**[[2qgt]] - hERα LBD (mutant) + NCAO2 peptide + EST derivative<br />
**[[5kce]] - hERα LBD (mutant) + NCAO2 peptide + OBHS derivative<br />
**[[1gwq]], [[2fai]], [[2g44]], [[2qzo]] - hERα LBD + NCAO2 peptide + ligand<br />
**[[3l03]], [[3hm1]], [[3hlv]], [[1zky]], [[2b1v]], [[2b1z]], [[2qa6]], [[2qab]], [[2qgw]], [[2qh6]], [[2qr9]], [[2qse]], [[2qxm]] - hERα LBD (mutant) + NCAO2 peptide + ligand<br />
**[[2qa8]] - hERα LBD (mutant) + NCAO2 peptide + genistein<br />
**[[4pp6]], [[4ppp]], [[4pps]] - hERα LBD (mutant) + NCAO2 + resveratrol derivative<br />
*''ERα LBD ternary complex with steroid receptor coactivator 3 peptide''
**[[1x7r]] - hERα LBD + NCAO3 peptide + genistein<br />
**[[1x7e]] - hERα LBD + NCAO3 peptide + ligand<br />
*Estrogen receptor β ligand binding domain
**[[1qkm]] - hERβ LBD + genistein<br />
**[[1qkn]], [[1hj1]] - ERβ LBD + ligand – rat<br />
**[[1nde]], [[1u3q]], [[1u3r]], [[1u3s]], [[2giu]], [[2i0g]], [[2i0j]], [[2jj3]], [[2z4b]], [[2qtu]], [[5toa]] - hERβ LBD + ligand<br />
**[[2yly]] - hERβ LBD + sulfonamide agonist<br />
**[[2fsz]] - hERβ LBD (mutant) + ligand<br />
**[[2yja]], [[2yjd]] - hERβ LBD + NCAO peptide<br />
**[[4zi1]] - hERβ LBD + NCAO5 peptide + antagonist<br />
**[[4j24]], [[4j26]] - hERβ LBD + peptide<br />
*''ERβ LBD ternary complex with steroid receptor coactivator peptide''
**[[1l2j]] - hERβ LBD + NCAO peptide + nonsteroidal EST<BR />
**[[2j7x]], [[3oll]], [[3ols]] - hERβ LBD + NCAO peptide + EST<BR />
**[[1u9e]] - hERβ LBD + NCAO peptide<br />
**[[1x76]], [[1x78]], [[1x7b]], [[1yy4]], [[1yye]], [[1zaf]], [[2j7y]], [[2nv7]], [[3omo]], [[3omp]], [[3omq]] - hERβ LBD + NCAO peptide + ligand<br />
**[[1x7j]] - hERβ LBD + NCAO peptide + genistein
*Estrogen receptor α DNA binding domain residues 182-252
**[[1hcp]] – hERα DBD – NMR<br />
**[[1hcq]], [[4aa6]] – hERα DBD + DNA<br />
}}
<br />
<br />
'''Reference'''
'''Reference'''
<references/>
<references/>
[[Category:Topic Page]]
[[Category:Topic Page]]
[[Category:Hormone]]

Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

Michal Harel, Alexander Berchansky, Joel L. Sussman
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