Novel inhibitors of signal transducer and activator of transcription 3 signaling pathway: an update on the recent patent literature

Expert Opin Ther Pat. 2014 Apr;24(4):383-400. doi: 10.1517/13543776.2014.877443. Epub 2014 Jan 16.

Abstract

Introduction: The signal transducer and activator of transcription 3 (STAT3) is a transcription factor that plays a key role in normal cell growth and is constitutively activated in about 70% of solid and hematological cancers. Thus, the development of potent and selective inhibitors that target STAT3 is of interest especially in the cancer therapeutic area.

Areas covered: This review updates new patents claiming STAT3 inhibitors and their uses published from 2011 to 2013. Pre-2011 patents have been extensively covered in previous reviews. Comments on the context of each chemical series are given where applicable to orientate the readers on the bewildering array of molecular designs now available.

Expert opinion: The growing number of preclinical studies in numerous malignances as well as the first clinical trials of STAT3 inhibitors suggest that STAT3 remains a valid target for the treatment of human cancers as well as inflammatory diseases and/or autoimmune disorders. So, the future looks bright for patients because many new drugs are being developed and now combinations of STAT3 inhibitors with other targeted agents can diminish the resistance to traditional chemotherapy. These advances are expected to lead to further significant progress improving patient outcomes and quality of life.

Publication types

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

MeSH terms

  • Animals
  • Humans
  • Molecular Structure
  • Neoplasms / drug therapy*
  • Oligonucleotides / pharmacology
  • Patents as Topic*
  • Protein Multimerization
  • STAT3 Transcription Factor / antagonists & inhibitors*
  • STAT3 Transcription Factor / chemistry
  • STAT3 Transcription Factor / physiology
  • Signal Transduction / drug effects*

Substances

  • Oligonucleotides
  • STAT3 Transcription Factor