Role of estrogen receptor coregulators in endocrine resistant breast cancer

Kristin A. Altwegg, Ratna K. Vadlamudi

Research output: Contribution to journalReview articlepeer-review


Breast cancer (BC) is the most ubiquitous cancer in women. Approximately 70-80% of BC diagnoses are positive for estrogen receptor (ER) alpha (ERα). The steroid hormone estrogen [17β-estradiol (E2)] plays a vital role both in the initiation and progression of BC. The E2-ERα mediated actions involve genomic signaling and non-genomic signaling. The specificity and magnitude of ERα signaling are mediated by interactions between ERα and several coregulator proteins called coactivators or corepressors. Alterations in the levels of coregulators are common during BC progression and they enhance ligand-dependent and ligand-independent ERα signaling which drives BC growth, progression, and endocrine therapy resistance. Many ERα coregulator proteins function as scaffolding proteins and some have intrinsic or associated enzymatic activities, thus the targeting of coregulators for blocking BC progression is a challenging task. Emerging data from in vitro and in vivo studies suggest that targeting coregulators to inhibit BC progression to therapy resistance is feasible. This review explores the current state of ERα coregulator signaling and the utility of targeting the ERα coregulator axis in treating advanced BC.

Original languageEnglish (US)
Pages (from-to)385-400
Number of pages16
JournalExploration of Targeted Anti-tumor Therapy
Issue number4
StatePublished - 2021


  • coregulators
  • endocrine therapy resistance
  • estrogen
  • Estrogen receptor
  • hormonal action
  • signal transduction
  • transcriptional activation

ASJC Scopus subject areas

  • Cancer Research
  • Oncology


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