This old version of Proteopedia is provided for student assignments while the new version is undergoing repairs. Content and edits done in this old version of Proteopedia after March 1, 2026 will eventually be lost when it is retired in about June of 2026.
Apply for new accounts at the new Proteopedia. Your logins will work in both the old and new versions.
Estrogen receptor
From Proteopedia
(Difference between revisions)
| (20 intermediate revisions not shown.) | |||
| Line 1: | Line 1: | ||
<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). | + | (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. 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>== | ||
| Line 10: | Line 12: | ||
==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 | + | <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== | ||
| + | [[Estrogen receptor 3D structures]] | ||
| + | |||
</StructureSection> | </StructureSection> | ||
| Line 16: | Line 22: | ||
==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 | ||
| - | |||
| - | **[[4n1y]] - ERα LBD – pacific oyster<br /> | ||
| - | **[[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 /> | ||
| - | **[[2bj4]], [[2jf9]], [[2jfa]], [[1pcg]] - hERα LBD + peptide antagonist<br /> | ||
| - | **[[2yja]] - hERα LBD + stapled peptide<br /> | ||
| - | **[[5hyr]] - hERα LBD (mutant) + stapled peptide + estradiol<br /> | ||
| - | **[[2q6j]], [[2p15]], [[3erd]], [[1l2i]] - hERα LBD + GRIP peptide<br /> | ||
| - | **[[5krh]] - hERα LBD + NCAO2 peptide + benzylidene estrone<br /> | ||
| - | **[[5kri]], [[5krj]], [[5krk]], [[5krl]], [[5krm]], [[5kro]] - hERα LBD (mutant) + NCAO2 peptide + anti-hormone<br /> | ||
| - | **[[5kcf]], [[5kct]], [[5kcu]], [[5kcw, [[5kd9]], [[5kcc]], [[5kcd]] - hERα LBD (mutant) + NCAO2 peptide + OBHS derivative<br /> | ||
| - | **[[5kr9]] - hERα LBD (mutant) + NCAO2 peptide + coumestrol<br /> | ||
| - | **[[5krf]] - hERα LBD (mutant) + peptide + anti-hormone<br /> | ||
| - | **[[2yat]] - hERα LBD (mutant) + EST derivative<br /> | ||
| - | **[[5fqp]], [[5fqr]], [[5fqs]], [[5fqt]], [[5fqv]] - hERα LBD (mutant) + antagonist<br /> | ||
| - | **[[3uuc]] - hERα LBD + bisphenol<br /> | ||
| - | **[[3q97]] - hERα LBD + LXXLL motif (mutant) + ethoxy triphenylethylene<br /> | ||
| - | **[[1gwr]] - hERα LBD + TIF2 peptide + EST<br /> | ||
| - | **[[2ocf]] - hERα LBD (mutant) + fibronectin domain 10 + EST<br /> | ||
| - | |||
| - | *''ERα LBD ternary complex with steroid receptor coactivator 1 peptide'' | ||
| - | |||
| - | **[[3uu7]], [[3uua]], [[3uud]] - hERα LBD (mutant) + nuclear receptor coactivator 1 peptide<br /> | ||
| - | **[[4dma]] - hERα LBD (mutant) + nuclear receptor coactivator 1 peptide + inhibitor<br /> | ||
| - | **[[4mg5]], [[4mg6]], [[4mg7]], [[4mg8]], [[4mg9]], [[4mga]], [[4mgb]], [[4mgc]], [[4mgd]] - hERα LBD (mutant) + nuclear receptor coactivator 1 peptide + ligand<br /> | ||
| - | **[[4tuz]] - hERα LBD (mutant) + steroid receptor coactivator 1 peptide + toxin<br /> | ||
| - | **[[4tv1]] - hERα LBD (mutant) + steroid receptor coactivator 1 peptide + preservative<br /> | ||
| - | |||
| - | *''ERα LBD ternary complex with steroid receptor coactivator 2 peptide'' | ||
| - | |||
| - | **[[2b23]] - hERα LBD (mutant) + nuclear receptor coactivator 2 peptide<br /> | ||
| - | **[[3q95]] - hERα LBD (mutant) + nuclear receptor coactivator 2 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) + nuclear receptor coactivator 2 peptide + inhibitor<br /> | ||
| - | **[[2g5o]] - hERα LBD + nuclear receptor coactivator 2 peptide + EST derivative<br /> | ||
| - | **[[2qgt]] - hERα LBD (mutant) + nuclear receptor coactivator 2 peptide + EST derivative<br /> | ||
| - | **[[5kce]] - hERα LBD (mutant) + nuclear receptor coactivator 2 peptide + OBHS derivative<br /> | ||
| - | **[[1gwq]], [[2fai]], [[2g44]], [[2qzo]] - hERα LBD + nuclear receptor coactivator 2 peptide + ligand<br /> | ||
| - | **[[3l03]], [[3hm1]], [[3hlv]], [[1zky]], [[2b1v]], [[2b1z]], [[2qa6]], [[2qab]], [[2qgw]], [[2qh6]], [[2qr9]], [[2qse]], [[2qxm]] - hERα LBD (mutant) + nuclear receptor coactivator 2 peptide + ligand<br /> | ||
| - | **[[2qa8]] - hERα LBD (mutant) + steroid receptor coactivator 2 peptide + genistein<br /> | ||
| - | **[[4pp6]], [[4ppp]], [[4pps]] - hERα LBD (mutant) + steroid receptor coactivator peptide 2 + resveratrol derivative<br /> | ||
| - | |||
| - | *''ERα LBD ternary complex with steroid receptor coactivator 3 peptide'' | ||
| - | |||
| - | **[[1x7r]] - hERα LBD + steroid receptor coactivator 3 peptide + genistein<br /> | ||
| - | **[[1x7e]] - hERα LBD + nuclear receptor coactivator 3 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]] - hERβ LBD + ligand<br /> | ||
| - | **[[2yly]] - hERβ LBD + sulfonamide agonist<br /> | ||
| - | **[[2fsz]] - hERβ LBD (mutant) + ligand<br /> | ||
| - | **[[2yja]], [[2yjd]] - hERβ LBD + stapled peptide<br /> | ||
| - | **[[4j24]], [[4j26]] - hERβ LBD + peptide<br /> | ||
| - | |||
| - | *''ERβ LBD ternary complex with steroid receptor coactivator peptide'' | ||
| - | |||
| - | **[[1l2j]] - hERβ LBD + steroid receptor coactivator peptide + nonsteroidal EST<BR /> | ||
| - | **[[2j7x]], [[3oll]], [[3ols]] - hERβ LBD + steroid receptor coactivator peptide + EST<BR /> | ||
| - | **[[1u9e]] - hERβ LBD + steroid receptor coactivator peptide<br /> | ||
| - | **[[1x76]], [[1x78]], [[1x7b]], [[1yy4]], [[1yye]], [[1zaf]], [[2j7y]], [[2nv7]], [[3omo]], [[3omp]], [[3omq]] - hERβ LBD + steroid receptor coactivator peptide + ligand<br /> | ||
| - | **[[1x7j]] - hERβ LBD + steroid receptor coactivator peptide + genistein | ||
| - | |||
| - | *Estrogen receptor α DNA binding domain | ||
| - | |||
| - | **[[1hcp]] – hERα DBD – NMR<br /> | ||
| - | **[[1hcq]], [[4aa6]] – hERα DBD + DNA<br /> | ||
<br /> | <br /> | ||
| Line 104: | Line 33: | ||
<references/> | <references/> | ||
[[Category:Topic Page]] | [[Category:Topic Page]] | ||
| + | [[Category:Hormone]] | ||
Current revision
| |||||||||||
For more details see
Hormone
Ivan Koutsopatriy estrogen receptor
C-di-GMP receptors with PilZ domain
Estrogens
For more details on ERβ see Student Project 10 for UMass Chemistry 423 Spring 2015
For more details on ER-Tamoxifen complex see Tamoxifen.
Reference
- ↑ Li MJ, Greenblatt HM, Dym O, Albeck S, Pais A, Gunanathan C, Milstein D, Degani H, Sussman JL. Structure of estradiol metal chelate and estrogen receptor complex: The basis for designing a new class of selective estrogen receptor modulators. J Med Chem. 2011 Apr 7. PMID:21473635 doi:10.1021/jm200192y
