Therapeutic modulators of STAT signalling for human diseases

Nat Rev Drug Discov. 2013 Aug;12(8):611-29. doi: 10.1038/nrd4088.


The signal transducer and activator of transcription (STAT) proteins have important roles in biological processes. The abnormal activation of STAT signalling pathways is also implicated in many human diseases, including cancer, autoimmune diseases, rheumatoid arthritis, asthma and diabetes. Over a decade has passed since the first inhibitor of a STAT protein was reported and efforts to discover modulators of STAT signalling as therapeutics continue. This Review discusses the outcomes of the ongoing drug discovery research endeavours against STAT proteins, provides perspectives on new directions for accelerating the discovery of drug candidates, and highlights the noteworthy candidate therapeutics that have progressed to clinical trials.

Publication types

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

MeSH terms

  • Animals
  • Clinical Trials as Topic
  • Disease
  • Drug Discovery / methods*
  • Drugs, Investigational / chemistry
  • Drugs, Investigational / pharmacology
  • Drugs, Investigational / therapeutic use
  • Humans
  • Models, Molecular
  • Molecular Targeted Therapy / methods*
  • STAT Transcription Factors / antagonists & inhibitors
  • STAT Transcription Factors / genetics
  • STAT Transcription Factors / metabolism*
  • Signal Transduction / drug effects*
  • Small Molecule Libraries
  • Structure-Activity Relationship


  • Drugs, Investigational
  • STAT Transcription Factors
  • Small Molecule Libraries