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Structure paper

TitleEstrogen receptor alpha somatic mutations Y537S and D538G confer breast cancer endocrine resistance by stabilizing the activating function-2 binding conformation.
Journal, issue, pagesElife, Vol. 5, Year 2016
Publish dateMar 24, 2014 (structure data deposition date)
AuthorsFanning, S.W. / Mayne, C.G. / Dharmarajan, V. / Carlson, K.E. / Martin, T.A. / Novick, S.J. / Toy, W. / Green, B. / Panchamukhi, S. / Katzenellenbogen, B.S. ...Fanning, S.W. / Mayne, C.G. / Dharmarajan, V. / Carlson, K.E. / Martin, T.A. / Novick, S.J. / Toy, W. / Green, B. / Panchamukhi, S. / Katzenellenbogen, B.S. / Tajkhorshid, E. / Griffin, P.R. / Shen, Y. / Chandarlapaty, S. / Katzenellenbogen, J.A. / Greene, G.L.
External linksElife / PubMed:26836308
MethodsX-ray diffraction
Resolution1.9 - 3.07 Å
Structure data

PDB-4pxm:
The Estrogen Receptor Alpha Ligand Binding Domain D538G Mutant in Complex with Estradiol and a glucocorticoid receptor-interacting protein 1 NR box II peptide
Method: X-RAY DIFFRACTION / Resolution: 1.9 Å

PDB-4q13:
Apo Estrogen Receptor Alpha Ligand Binding Domain D538G Mutant with a glucocorticoid receptor-interacting protein 1 NR box II peptide
Method: X-RAY DIFFRACTION / Resolution: 2.24 Å

PDB-4q50:
The Estrogen Receptor Alpha Ligand Binding Domain D538G Mutant in Complex with 4-hydroxytamoxifen
Method: X-RAY DIFFRACTION / Resolution: 3.07 Å

Chemicals

ChemComp-EST:
ESTRADIOL / hormone*YM

ChemComp-HOH:
WATER

ChemComp-OHT:
4-HYDROXYTAMOXIFEN

ChemComp-SO4:
SULFATE ION

Source
  • homo sapiens (human)
  • synthetic construct (others)
KeywordsHormone/Peptide / Metastatic Breast Cancer / Activating Mutation / ER alpha / Alpha Helical / Nuclear Hormone Receptor / Hormone-Peptide complex / Hormone binding protein/peptide / Activating Point Mutation / Drug Resistance / SERM resistance / Alpha Helix / Hormone binding protein-peptide complex / hormone binding protein / Acquired SERM-Resistance / Breast Cancer / SERM-ER structure

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