Estrogen-related receptor

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spinqualitylabelsall models 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) Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image Function Estrogen-related receptor (ERR) binds to estrogen response elements on DNA and modulates transcription in response to hormone. There are 3 classes of ERR : ERRα, ERRβ and ERRγ. Relevance ERR plays a role in energy homeostasis and cancer[1]. ERRα and ERRγ are overexpressed in breast cancer and can serve as prognostic markers or therapeutic targets. Structural insights The chemotherapeutic drugs bisphenol and tamoxifen are nestled between 4 alpha helices in the ERR active site [2].

3D structures of estrogen-related receptor

Updated on 24-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