Inhibiting Heat Shock Factor 1 in Cancer: A Unique Therapeutic Opportunity

Trends Pharmacol Sci. 2019 Dec;40(12):986-1005. doi: 10.1016/j.tips.2019.10.008. Epub 2019 Nov 11.

Abstract

The ability of cancer cells to cope with stressful conditions is critical for their survival, proliferation, and metastasis. The heat shock transcription factor 1 (HSF1) protects cells from stresses such as chemicals, radiation, and temperature. These properties of HSF1 are exploited by a broad spectrum of cancers, which exhibit high levels of nuclear, active HSF1. Functions for HSF1 in malignancy extend well beyond its central role in protein quality control. While HSF1 has been validated as a powerful target in cancers by genetic knockdown studies, HSF1 inhibitors reported to date have lacked sufficient specificity and potency for clinical evaluation. We review the roles of HSF1 in cancer, its potential as a prognostic indicator for cancer treatment, evaluate current HSF1 inhibitors and provide guidelines for the identification of selective HSF1 inhibitors as chemical probes and for clinical development.

Keywords: inhibitors; non-oncogene addiction; stress protection.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / therapeutic use
  • Cell Proliferation / drug effects
  • Heat Shock Transcription Factors / antagonists & inhibitors*
  • Heat Shock Transcription Factors / genetics
  • Heat Shock Transcription Factors / metabolism
  • Humans
  • Molecular Targeted Therapy
  • Neoplasms / drug therapy*
  • Neoplasms / genetics
  • Neoplasms / metabolism
  • Neoplasms / pathology
  • Signal Transduction / drug effects

Substances

  • Antineoplastic Agents
  • Heat Shock Transcription Factors