Estrogen-related receptor

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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.
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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== Structural insights ==
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The chemotherapeutic drugs bisphenol and tamoxifen are nestled between 4 alpha helices in the ERR active site <ref>PMID:16990259</ref>.
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Revision as of 15:23, 20 January 2016

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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3D structures of estrogen-related receptor

Updated on 20-January-2016

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

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Michal Harel, Alexander Berchansky, Wayne Decatur

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