title: Targeting the androgen receptor in metastatic castrate-resistant prostate cancer: A review.
abstract: Despite recent advances in the treatment of advanced prostate cancer (PCa), metastatic castrate-resistant PCa remains incurable at this time. The androgen receptor (AR) plays a key role in the development and progression of PCa, continuing to be active in most patients even after the development of castration resistance. Here, we aim to more closely review the mechanisms by which AR signaling is maintained, including AR overexpression/overamplification, intracrine androgen synthesis, AR mutations, and the development of AR splice variants. We also review therapies targeting each of these mechanisms. We also discuss the potential role of AR-CAG repeats and AR splice variants as potential biomarkers of response to hormonal manipulation therapies.
authors.affiliation: Genitourinary Medical Oncology Program, UCSF Helen Diller Family Comprehensive Cancer Center, San Francisco, CA.
authors.forename: Archana
authors.initials: A
authors.lastname: Anantharaman
authors.affiliation: Genitourinary Medical Oncology Program, UCSF Helen Diller Family Comprehensive Cancer Center, San Francisco, CA. Electronic address: terence.friedlander@ucsf.edu.
authors.forename: Terence W
authors.initials: TW
authors.lastname: Friedlander
mesh_terms: D059002:Androgen Receptor Antagonists / Q000627:therapeutic use*; D018450:Disease Progression; D006801:Humans; D008297:Male; D064129:Prostatic Neoplasms, Castration-Resistant / Q000188:drug therapy*; D020033:Protein Isoforms / Q000378:metabolism; D011944:Receptors, Androgen / Q000378:metabolism*; D015398:Signal Transduction
chemical_list: D059002:Androgen Receptor Antagonists; D020033:Protein Isoforms; D011944:Receptors, Androgen
keywords: Androgen receptor; Castration-resistant prostate cancer