Eighty Years of Targeting Androgen Receptor Activity in Prostate Cancer: The Fight Goes on

Eva Estébanez-Perpiñá, Charlotte L Bevan, Iain J McEwan* (Corresponding Author)

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

29 Citations (Scopus)
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Prostate cancer (PCa) is the most common cancer in men in the West, other than skin cancer, accounting for over a quarter of cancer diagnoses in US men. In a seminal paper from 1941, Huggins and Hodges demonstrated that prostate tumours and metastatic disease were sensitive to the presence or absence of androgenic hormones. The first hormonal therapy for PCa was thus castration. In the subsequent eighty years, targeting the androgen signalling axis, where possible using drugs rather than surgery, has been a mainstay in the treatment of advanced and metastatic disease. Androgens signal via the androgen receptor, a ligand-activated transcription factor, which is the direct target of many such drugs. In this review we discuss the role of the androgen receptor in PCa and how the combination of structural information and functional screenings is continuing to be used for the discovery of new drug to switch off the receptor or modify its function in cancer cells.

Original languageEnglish
Article number509
Number of pages19
Issue number3
Publication statusPublished - 29 Jan 2021

Bibliographical note

Funding Information:
The authors gratefully acknowledge funding support from: Prostate Cancer UK, Cancer Research UK Imperial Centre and Prostate Cancer Foundation (Bevan Lab); grants BFU2017-86906-R and SAF2017-90604REDT-NuRCaMeIn from the Spanish Ministry of Economy and Competitivity (MINECO, Gobierno de Espa?a), Caixa Impulse CI2018-00018 from La Caixa and Llavor-Generalitat de Catalunya (Estebañez-Perpiña Lab); Friends of Anchor, Prostate Cancer Research and Medical Research Council, grant MR/T02559X/1 (McEwan Lab).


  • Androgen ablation therapy
  • Androgen receptor
  • Antiandrogens
  • Prostate cancer


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