Clinical significance of estrogen receptor phosphorylation

Endocr Relat Cancer. 2011 Jan 19;18(1):R1-14. doi: 10.1677/ERC-10-0070. Print 2011 Feb.

Abstract

Multiple sites of phosphorylation on human estrogen receptor α (ERα) have been identified by a variety of methodologies. Now with the emerging availability of phospho-site-specific antibodies to ERα, the relevance of phosphorylation of ERα in human breast cancer in vivo is being explored. Multiple phosphorylated sites in ERα can be detected in multiple breast tumor biopsy samples, providing evidence of their relevance to human breast cancer in vivo. Published data suggest that the detection in primary breast tumors of phosphorylation at some sites in ERα is associated with a better clinical outcome while phosphorylation at other sites is associated with a poorer clinical outcome most often in patients who have been treated with tamoxifen. This suggests the hypothesis that phospho-profiling of ERα in human breast tumors to establish an 'ERα phosphorylation code', may be a more accurate marker of prognosis and/or response to endocrine therapy in human breast cancer.

Publication types

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

MeSH terms

  • Antineoplastic Agents, Hormonal / pharmacology
  • Antineoplastic Agents, Hormonal / therapeutic use
  • Biopsy
  • Breast Neoplasms / drug therapy
  • Breast Neoplasms / metabolism*
  • Carcinoma / drug therapy
  • Carcinoma / metabolism*
  • Disease Progression
  • Drug Resistance, Neoplasm
  • Estrogen Receptor alpha / metabolism*
  • Estrogen Receptor alpha / physiology
  • Estrogens*
  • Female
  • Gene Expression Regulation, Neoplastic
  • Humans
  • Neoplasm Proteins / metabolism*
  • Neoplasm Proteins / physiology
  • Neoplasms, Hormone-Dependent / drug therapy
  • Neoplasms, Hormone-Dependent / metabolism*
  • Phosphorylation
  • Proteasome Endopeptidase Complex / metabolism
  • Protein Kinases / metabolism
  • Protein Processing, Post-Translational*
  • Selective Estrogen Receptor Modulators / pharmacology
  • Selective Estrogen Receptor Modulators / therapeutic use
  • Signal Transduction
  • Structure-Activity Relationship
  • Tamoxifen / pharmacology
  • Tamoxifen / therapeutic use
  • Treatment Outcome

Substances

  • Antineoplastic Agents, Hormonal
  • ESR1 protein, human
  • Estrogen Receptor alpha
  • Estrogens
  • Neoplasm Proteins
  • Selective Estrogen Receptor Modulators
  • Tamoxifen
  • Protein Kinases
  • Proteasome Endopeptidase Complex