Small Molecule Inhibitors of HSF1-Activated Pathways as Potential Next-Generation Anticancer Therapeutics

Molecules. 2018 Oct 24;23(11):2757. doi: 10.3390/molecules23112757.

Abstract

Targeted therapy is an emerging paradigm in the development of next-generation anticancer drugs. Heat shock factor 1 (HSF1) has been identified as a promising drug target because it regulates several pathways responsible for cancer cell growth, metastasis, and survival. Studies have clearly demonstrated that HSF1 is an effective drug target. Herein, we provide a concise yet comprehensive and integrated overview of progress in developing small molecule inhibitors of HSF1 as next-generation anticancer chemotherapeutics while critically evaluating their potential and challenges. We believe that this review will provide a better understanding of important concepts helpful for outlining the strategy to develop new chemotherapeutic agents with promising anticancer activities by targeting HSF1.

Keywords: HSF1; HSF1 inhibitors; HSPs; anticancer agents.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / therapeutic use
  • Biological Products / chemistry
  • Biological Products / pharmacology
  • Biological Products / therapeutic use
  • Heat Shock Transcription Factors / antagonists & inhibitors*
  • Heat Shock Transcription Factors / chemistry
  • Heat Shock Transcription Factors / metabolism*
  • Humans
  • Molecular Targeted Therapy*
  • Neoplasms / drug therapy
  • Neoplasms / metabolism*
  • Prodrugs / chemistry
  • Prodrugs / pharmacology
  • Prodrugs / therapeutic use
  • Signal Transduction / drug effects*
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Biological Products
  • Heat Shock Transcription Factors
  • Prodrugs