Targeting Nuclear Receptors for Cancer Therapy: Premises, Promises, and Challenges

Trends Cancer. 2021 Jun;7(6):541-556. doi: 10.1016/j.trecan.2020.11.007. Epub 2020 Dec 16.

Abstract

Nuclear receptors are a family of transcription factors localized in cell nuclei, sensing specific ligands and fine-tuning a variety of cell physiological events. They have been intensively investigated in cancer biology. With their excellent properties of druggability and actionability, nuclear receptors have demonstrated much promise as novel therapeutic targets for different cancer types. Accumulating evidence has highlighted the essential roles of certain nuclear receptors in tumor immunology, suggesting the possibility for them to serve as cancer immunotherapeutic targets. Here, we summarize the roles of nuclear receptors in cancer biology and tumor immunology, and underscore the current advances of clinical trials for nuclear receptor-based cancer therapeutics.

Keywords: cancer therapy; nuclear receptors; tumor immunology.

Publication types

  • Historical Article
  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Antineoplastic Combined Chemotherapy Protocols / pharmacology*
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use
  • Cell Nucleus / metabolism
  • Clinical Trials as Topic
  • History, 20th Century
  • History, 21st Century
  • Humans
  • Immune Checkpoint Inhibitors / pharmacology*
  • Immune Checkpoint Inhibitors / therapeutic use
  • Immune Checkpoint Proteins / metabolism*
  • Medical Oncology / history
  • Medical Oncology / trends
  • Molecular Targeted Therapy / methods
  • Neoplasms / drug therapy*
  • Neoplasms / immunology
  • Neoplasms / pathology
  • Receptors, Cytoplasmic and Nuclear / antagonists & inhibitors*
  • Receptors, Cytoplasmic and Nuclear / metabolism

Substances

  • Immune Checkpoint Inhibitors
  • Immune Checkpoint Proteins
  • Receptors, Cytoplasmic and Nuclear