Targeting the Androgen Receptor in Breast Cancer

  title={Targeting the Androgen Receptor in Breast Cancer},
  author={Kee Ming Chia and Megan O'Brien and Myles A Brown and Elgene Lim},
  journal={Current Oncology Reports},
The androgen receptor (AR) is expressed in the majority of breast cancer and across the three main breast cancer subtypes. Historically, the oncogenic role of AR has best been described in molecular apocrine breast cancers, an estrogen receptor (ER)−/AR+ subtype which has a steroid response signature similar to that in the ER-positive breast cancer. The signalling effect of AR is likely to be different across breast cancer subtypes, and particularly important is its interaction with ER… 

AR Signaling in Breast Cancer

The literature on the biology of AR in breast cancer and its prognostic and predictive roles are reviewed and the thoughts on therapeutic strategies are presented.

Androgen receptor signaling pathways as a target for breast cancer treatment.

An overview of AR signaling pathways in different breast cancer subtypes, providing evidence that its oncogenic role is likely to be different in distinct biological and clinical scenarios and representing the rationale for AR-targeting treatment as a potentially new target therapy in breast cancer subset using androgen agonists in some AR-positive/ER-positive tumors.

Androgen Receptor-Targeted Therapy for Breast Cancer

The role of AR across the differing subtypes of BC is discussed and the most recent clinical trial data for the use of androgen-directed therapy in the treatment of AR+ breast cancer is summarized, with a particular emphasis on TNBC.

Pushing estrogen receptor around in breast cancer.

This review will focus on the established and emerging clinical evidence for activating PR or AR in ER-positive breast cancer to inhibit the tumour growth-promoting functions of ER.

Androgen receptor: A promising therapeutic target in breast cancer

This review aims to address the importance of the androgen receptor in BCa diagnosis and prognosis, current AR-targeting approaches inBCa, and the potential for AR-downstream molecules to serve as therapeutic targets.

A review of estrogen receptor/androgen receptor genomics in male breast cancer.

This review critically discusses the recent developments in the study of male breast cancer in relation to ERα and AR action and highlights the potential future studies to further elucidate the genomic regulation of this rare disease.

Androgen receptor function and targeted therapeutics across breast cancer subtypes

The current state of the art regarding AR-targeted approaches for BC as monotherapy or in combination with radiotherapy is described and the importance of categorizing BC subtypes effectively, in relation to determining AR activity is demonstrated.

Hormone signaling via androgen receptor affects breast cancer and prostate cancer in a male patient: A case report

Findings indicate that estrogen exposure after estrogen depletion likely causes apoptosis of ER-positive breast cancer cells, and this also applies to the environment in male body.

The Other Side of the Coin: May Androgens Have a Role in Breast Cancer Risk?

This review aims to elucidate whether androgens might influence the susceptibility for breast cancer, and the possibility to exploit the AR as a useful marker to predict the disease will be also evaluated.



Role of the androgen receptor in breast cancer and preclinical analysis of enzalutamide

This preclinical study supports the initiation of clinical studies evaluating enzalutamide for treatment of AR+ tumors regardless of ER status, since it blocks both androgen- and estrogen- mediated tumor growth.

Androgen receptor overexpression induces tamoxifen resistance in human breast cancer cells

A role for AR overexpression as a novel mechanism of hormone resistance, so that AR may offer a new clinical therapeutic target in human breast cancers is suggested.

Androgen receptor inhibits estrogen receptor-alpha activity and is prognostic in breast cancer.

It is concluded that, by binding to a subset of EREs, the AR can prevent activation of target genes that mediate the stimulatory effects of 17beta-estradiol on breast cancer cells.

Synergy between inhibitors of androgen receptor and MEK has therapeutic implications in estrogen receptor-negative breast cancer

In vivo, in vitro and in vivo synergies between AR and MEK inhibitors in molecular apocrine breast cancer are demonstrated and it is shown that combination therapy with these inhibitors can overcome trastuzumab resistance in Molecular apocrine cells.

Androgen receptor expression is significantly associated with better outcomes in estrogen receptor-positive breast cancers.

  • S. ParkJ. Koo K. Lee
  • Medicine, Biology
    Annals of oncology : official journal of the European Society for Medical Oncology
  • 2011
The results suggest that AR could be an additional marker for endocrine responsiveness in ER-positive cancers and a candidate for therapeutic targeting of ER-negative tumors.

Androgen receptor driven transcription in molecular apocrine breast cancer is mediated by FoxA1

Findings show that AR binds and regulates ER cis‐regulatory elements in molecular apocrine tumours, resulting in a transcriptional programme reminiscent of ER‐mediated transcription in luminal breast cancers.

Androgen receptor (AR) expression in 400 breast carcinomas: is routine AR assessment justified?

The relatively high proportion of AR+ tumors among the 50 triple negative carcinomas is an important finding in support of routine assessment of AR in at least all TNBCs and apocrine carcinomas as a potential target for therapy.

Androgen Receptor Expression and Breast Cancer Survival in Postmenopausal Women

The association of AR status and breast cancer survival is dependent on ER status, and AR expression was associated with a more favorable prognosis among women with ER-positive tumors.

Androgen receptor expression is a significant prognostic factor in estrogen receptor positive breast cancers

AR expression is an independent prognostic factor of better outcome in patients with ER-positive breast cancers, and was a significant marker of good prognosis for TTR and DSS.