Phospho-serine-118 estrogen receptor-alpha detection in human breast tumors in vivo

Clin Cancer Res. 2004 Feb 15;10(4):1354-9. doi: 10.1158/1078-0432.ccr-03-0112.

Abstract

Purpose: To determine whether estrogen receptor (ER)-alpha specifically phosphorylated at Ser(118) is detectable in multiple human breast cancer biopsy samples. To gain insight into possible roles for P-Ser(118)-ERalpha in human breast cancer in vivo.

Experimental design: A specific antibody for P-Ser(118)-ERalpha was validated for immunohistochemistry (IHC), and Western blot analysis confirmed IHC results. IHC was used to determine the relationship of P-Ser(118)-ERalpha to known prognostic markers and active mitogen-activated protein kinase (MAPK; erk1/2) expression.

Results: P-Ser(118)-ERalpha was significantly correlated with the expression of total ER, determined by ligand binding assay (r = 0.442, P = 0.002), but not with progesterone receptor expression or nodal status. P-Ser(118)-ERalpha was inversely correlated with histological grade (r = -0.34, P = 0.023), reflecting a similar trend for total ER (r = -0.287, P = 0.056). Categorical contingency analysis confirmed that P-Ser(118)-ERalpha was more frequently associated with lower than higher grade breast tumors (P = 0.038). In addition P-Ser(118)-ERalpha was significantly associated with detection of active MAPK (Erk1/2; Spearman r = 0.649, P < 0.0001; Fisher's exact test, P = 0.0004).

Conclusions: P-Ser(118)-ERalpha detection is associated with a more differentiated phenotype and other markers of good prognosis in human breast cancer. P-Ser(118)-ERalpha is correlated with active MAPK in human breast tumor biopsies, suggesting the possibility that active MAPK either directly or indirectly has a role in the regulation of P-Ser(118)-ERalpha expression in vivo. These data provide evidence for a role of P-Ser(118)-ERalpha in human breast cancer in vivo.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Biomarkers, Tumor
  • Biopsy
  • Blotting, Western
  • Breast Neoplasms / metabolism*
  • Cell Differentiation
  • Cell Line, Tumor
  • Enzyme Inhibitors / pharmacology
  • Estrogen Receptor alpha
  • Flavonoids / pharmacology
  • Humans
  • Immunohistochemistry
  • Ligands
  • Lymphatic Metastasis
  • MAP Kinase Signaling System
  • Mitogen-Activated Protein Kinase 1 / metabolism
  • Mitogen-Activated Protein Kinase 3
  • Mitogen-Activated Protein Kinases / metabolism
  • Phenotype
  • Phosphorylation
  • Phosphoserine / chemistry*
  • Prognosis
  • Receptors, Estrogen / biosynthesis*
  • Serine / chemistry

Substances

  • Biomarkers, Tumor
  • Enzyme Inhibitors
  • Estrogen Receptor alpha
  • Flavonoids
  • Ligands
  • Receptors, Estrogen
  • Phosphoserine
  • Serine
  • Mitogen-Activated Protein Kinase 1
  • Mitogen-Activated Protein Kinase 3
  • Mitogen-Activated Protein Kinases
  • 2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one