AR, Overview

Travis Van der Steen, Lucy J. Schmidt, Donald J. Tindall

Research output: Chapter in Book/Report/Conference proceedingChapter

Abstract

The androgen receptor (AR) is a nuclear hormone receptor that plays a key role in the development of the prostate and progression of prostate cancer (PCa). AR is the initial target for treatment in hormone dependent PCa, where inhibition of AR activity results in a decrease in tumor volume and increased survival. However, PCa often returns as castration-resistant prostate cancer (CRPC) due to several factors including AR overexpression, reactivation of the full-length receptor (ARFL), and expression of constitutively activate truncated AR-variants (AR-Vs) that lack the ligand binding domain. Upon reactivation of AR-FL and expression of AR-Vs, traditional methods of treatment targeting the ligand binding domain are ineffective. Targeting the evolutionarily conserved N-terminal domain, DNA binding domain (DBD) or using transcription factors that interact with AR will be key in developing new treatments for PCa.

Original languageEnglish (US)
Title of host publicationCancer Therapeutic Targets
PublisherSpringer New York
Pages967-975
Number of pages9
Volume2-2
ISBN (Electronic)9781441907172
ISBN (Print)9781441907165
DOIs
StatePublished - Jan 1 2017

Keywords

  • Androgen deprivation therapy (ADT)
  • Androgen receptor (AR)
  • Androgen receptor variants (AR-Vs)
  • Androgen response element (ARE)
  • Castration-resistant prostate cancer (CRPC)
  • DNA-binding domain (DBD)
  • Phosphorylation
  • Prostate cancer (PCa)
  • Reactivation of AR

ASJC Scopus subject areas

  • Medicine(all)
  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)

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  • Cite this

    Van der Steen, T., Schmidt, L. J., & Tindall, D. J. (2017). AR, Overview. In Cancer Therapeutic Targets (Vol. 2-2, pp. 967-975). Springer New York. https://doi.org/10.1007/978-1-4419-0717-2_111