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Estrogen-related receptor

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{{STRUCTURE_2gpu| PDB=2gpu | SIZE=400| SCENE= |right|CAPTION=Human estrogen-related receptor γ complex with 4-hydroxytamoxifen, [[2gpu]] }}
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<StructureSection load='2gpv' size='350' side='right' scene='50/501401/Cv/1' caption='Human estrogen-related receptor γ ligand-binding domain (cyan, grey, green, yellow, pink, purple) complex with nuclear receptor corepressor 2 peptide (dark red, orange) and 4-hydroxytamoxifen (PDB code [[2gpv]]) '>
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== Function ==
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'''Estrogen-related receptor''' (ERR) binds to estrogen response elements on DNA and modulates transcription in response to [[Hormone|hormone]]. It is a [[Nuclear receptors|nuclear receptor]]. There are 3 classes of ERR : ERRα, ERRβ and ERRγ.
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'''Estrogen-related receptor''' (ERR) binds to estrogen response elements on DNA and modulates transcription. ERR plays a role in energy homeostasis and cancer. There are 3 classes of ERR : ERRα, ERRβ and ERRγ.
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See also [[Intracellular receptors]]
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==3D structures of estrogen-related receptor==
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== Relevance ==
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===ERRα===
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ERR plays a role in energy homeostasis and cancer<ref>PMID:16515477</ref>. ERRα and ERRγ are overexpressed in breast cancer and can serve as prognostic markers or therapeutic targets.
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[[1xb7]], [[3d24]] – hERR ligand-binding domain + peroxisome proliferator activated receptor coactivator 1 peptide – human<br />[[2pjl]] - hERR ligand-binding domain (mutant) + inverse agonist<br />
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== Structural insights ==
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[[3k6p]] - hERR ligand-binding domain + ligand
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<scene name='50/501401/Cv/4'>Binding of nuclear receptor corepressor 2 peptide and 4-hydroxytamoxifen</scene> to human estrogen-related receptor γ. The chemotherapeutic drugs bisphenol and <scene name='50/501401/Cv/5'>tamoxifen</scene> are nestled between 4 alpha helices in the ERR active site <ref>PMID:16990259</ref>.
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==3D structures of estrogen-related receptor==
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[[Estrogen-related receptor 3D structures]]
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===ERRβ===
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</StructureSection>
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[[1lo1]] – hERR DNA-binding domain + DNA
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== References ==
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<references/>
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===ERRγ===
 
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[[2gp7]], [[2zbs]] - hERR ligand-binding domain<br />
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[[Category:Topic Page]]
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[[1kv6]], [[1tfc]] – hERR ligand-binding domain + steroid receptor coactivator 1 2nd NR-Box <br />
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[[2gpo]], [[2gpp]] - hERR ligand-binding domain + nuclear receptor-interacting protein 1 peptide<br />
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[[2ewp]] - hERR ligand-binding domain + tamoxifen analog<br />
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[[2gpu]], [[2p7z]] - hERR ligand-binding domain + 4-hydroxytamoxifen<br />
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[[2e2r]], [[2p7g]] - hERR ligand-binding domain + bisphenol A<br />
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[[2zkc]] - hERR ligand-binding domain + bisphenol Z<br />
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[[2zas]] - hERR ligand-binding domain + bisphenol A derivative<br />
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[[2p7a]] - hERR ligand-binding domain + methyl phenol<br />
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[[2gpv]] - hERR ligand-binding domain + nuclear receptor corepressor 2 peptide + 4-hydroxytamoxifen<br />
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[[1s9p]] - mERR ligand-binding domain + diethylstilbesterol – mouse<br />
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[[1vjb]] - mERR ligand-binding domain + 4-hydroxytamoxifen<br />
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Current revision

Human estrogen-related receptor γ ligand-binding domain (cyan, grey, green, yellow, pink, purple) complex with nuclear receptor corepressor 2 peptide (dark red, orange) and 4-hydroxytamoxifen (PDB code 2gpv)

Drag the structure with the mouse to rotate

References

  1. ↑ Ariazi EA, Jordan VC. Estrogen-related receptors as emerging targets in cancer and metabolic disorders. Curr Top Med Chem. 2006;6(3):203-15. PMID:16515477
  2. ↑ Wang L, Zuercher WJ, Consler TG, Lambert MH, Miller AB, Orband-Miller LA, McKee DD, Willson TM, Nolte RT. X-ray crystal structures of the estrogen-related receptor-gamma ligand binding domain in three functional states reveal the molecular basis of small molecule regulation. J Biol Chem. 2006 Dec 8;281(49):37773-81. Epub 2006 Sep 21. PMID:16990259 doi:http://dx.doi.org/10.1074/jbc.M608410200

Proteopedia Page Contributors and Editors (what is this?)

Michal Harel, Alexander Berchansky, Wayne Decatur

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