Androgen receptor: A promising therapeutic target in breast cancer

Crit Rev Clin Lab Sci. 2019 May;56(3):200-223. doi: 10.1080/10408363.2019.1575643. Epub 2019 Mar 1.

Abstract

Breast cancer (BCa) is the second most common cancer worldwide and the most prevalent cancer in women. The majority of BCa cases are positive (+) for the estrogen receptor (ER+, 80%) and progesterone receptor (PR+, 65%). Estrogen and progesterone hormones are known to be involved in cancer progression, and thus hormonal deprivation is used as an effective treatment for ER+PR+ BCa subtypes. However, some ER+PR+ BCa patients develop resistance to such therapies. Meanwhile, chemotherapy is the only available treatment for ER-PR- BCa tumors. Another hormone receptor known as the androgen receptor (AR) has also been found to be widely expressed in human breast carcinomas. However, the mechanisms of AR and its endogenous androgen ligands is not well-understood in BCa and its biological role in this hormone-related disease remains unclear. In this review, we aim to address the importance of the AR in BCa diagnosis and prognosis, current AR-targeting approaches in BCa, and the potential for AR-downstream molecules to serve as therapeutic targets.

Keywords: Breast cancer; androgen receptor; androgens; hormonal therapy/signaling pathway; targeted therapy.

Publication types

  • Review

MeSH terms

  • Androgens / metabolism
  • Androgens / therapeutic use
  • Antineoplastic Agents / metabolism
  • Antineoplastic Agents / therapeutic use
  • Breast / chemistry
  • Breast / metabolism
  • Breast Neoplasms* / chemistry
  • Breast Neoplasms* / drug therapy
  • Breast Neoplasms* / metabolism
  • Drug Discovery
  • Female
  • Humans
  • Receptors, Androgen*
  • Receptors, Estrogen / genetics
  • Receptors, Progesterone / genetics
  • Signal Transduction

Substances

  • AR protein, human
  • Androgens
  • Antineoplastic Agents
  • Receptors, Androgen
  • Receptors, Estrogen
  • Receptors, Progesterone