Constitutively Active Androgen Receptor in Hepatocellular Carcinoma

Int J Mol Sci. 2022 Nov 9;23(22):13768. doi: 10.3390/ijms232213768.

Abstract

Hepatocellular carcinoma (HCC) is the predominant type of liver cancer and a leading cause of cancer-related death globally. It is also a sexually dimorphic disease with a male predominance both in HCC and in its precursors, non-alcoholic fatty liver disease (NAFLD)/non-alcoholic steatohepatitis (NASH). The role of the androgen receptor (AR) in HCC has been well documented; however, AR-targeted therapies have failed to demonstrate efficacy in HCC. Building upon understandings of AR in prostate cancer (PCa), this review examines the role of AR in HCC, non-androgen-mediated mechanisms of induced AR expression, the existence of AR splice variants (AR-SV) in HCC and concludes by surveying current AR-targeted therapeutic approaches in PCa that show potential for efficacy in HCC in light of AR-SV expression.

Keywords: androgen receptor C-terminal truncated isoforms; androgen receptor degraders; androgen receptor splice variants; antiandrogens; liver cancer; nuclear hormone receptor.

Publication types

  • Review

MeSH terms

  • Carcinoma, Hepatocellular* / metabolism
  • Female
  • Humans
  • Liver Neoplasms* / metabolism
  • Male
  • Non-alcoholic Fatty Liver Disease* / pathology
  • Receptors, Androgen / genetics
  • Receptors, Androgen / metabolism

Substances

  • Receptors, Androgen