Reprogramming the oncogenic response: SET protein as a potential therapeutic target in cancer

Expert Opin Ther Targets. 2017 Jul;21(7):685-694. doi: 10.1080/14728222.2017.1336226. Epub 2017 Jun 6.

Abstract

SET is a multitask oncoprotein that promotes the initiation and progression of cancer. Overexpression of SET has been characterized as being tumor-specific and is associated with adverse clinical outcomes in many different human malignant diseases. Notably, SET has been shown to promote the development of therapeutic resistance in cancer cells. Area covered: In this review, we summarized the currently available evidence relating to the oncogenic roles, biological functions and clinical relevance of SET protein in cancer. The anti-cancer effects of three different SET antagonists undergoing preclinical investigation are also discussed. Expert opinion: Emerging evidence supports the critical role of SET in regulating various different cancer hallmarks. Targeting the SET-associated protein interfaces may be a potential anti-cancer strategy for future development. However, more studies are required to clarify the best strategy to combine SET antagonists with other anti-cancer treatments and to explore possible biomarkers that predict responsiveness.

Keywords: PP2A; SET; cancer; oncoprotein; target therapy.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Biomarkers, Tumor / metabolism
  • DNA-Binding Proteins
  • Disease Progression
  • Drug Design
  • Drug Resistance, Neoplasm
  • Histone Chaperones / antagonists & inhibitors
  • Histone Chaperones / metabolism*
  • Humans
  • Molecular Targeted Therapy
  • Neoplasms / drug therapy*
  • Neoplasms / pathology
  • Transcription Factors / antagonists & inhibitors
  • Transcription Factors / metabolism*

Substances

  • Antineoplastic Agents
  • Biomarkers, Tumor
  • DNA-Binding Proteins
  • Histone Chaperones
  • SET protein, human
  • Transcription Factors