Estrogen receptor
From Proteopedia
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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). | + | (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 | + | <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]] | + | [[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]]. | ||
Current revision
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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
