Androgen Receptor in Hormone Receptor-Positive Breast Cancer

dc.contributor.authorKhan, Ashfia Fatima
dc.contributor.authorKarami, Samaneh
dc.contributor.authorPeidl, Anthony S.
dc.contributor.authorWaiters, Kacie D.
dc.contributor.authorBabajide, Mariam Funmi
dc.contributor.authorBawa-Khalfe, Tasneem
dc.description.abstractBreast cancer subtypes expressing hormone receptors (HR+ BCa) have a good prognosis and respond to first-line endocrine therapy (ET). However, the majority of HR+ BCa patients exhibit intrinsic or acquired ET resistance (ET-R) and rapid onset of incurable metastatic BCa. With the failure of conventional ET, limited targeted therapy exists for ET-R HR+ BCa patients. The androgen receptor (AR) in HR-negative BCa subtypes is emerging as an attractive alternative target for therapy. The AR drives Luminal AR (LAR) triple-negative breast cancer progression, and LAR patients consistently exhibit positive clinical benefits with AR antagonists in clinical trials. In contrast, the function of the AR in HR+ BCa is more conflicting. AR in HR+ BCa correlates with a favorable prognosis, and yet, the AR supports the development of ET-R BCa. While AR antagonists were ineffective, ongoing clinical trials with a selective AR modulator have shown promise for HR+ BCa patients. To understand the incongruent actions of ARs in HR+ BCa, the current review discusses how the structure and post-translational modification impact AR function. Additionally, completed and ongoing clinical trials with FDA-approved AR-targeting agents for BCa are presented. Finally, we identify promising investigational small molecules and chimera drugs for future HR+ BCa therapy.
dc.identifierdoi: 10.3390/ijms25010476
dc.identifier.citationInternational Journal of Molecular Sciences 25 (1): 476 (2024)
dc.titleAndrogen Receptor in Hormone Receptor-Positive Breast Cancer


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