Small-molecule Transcription Factor Inhibitors in Oncology
Chapter 6: Targeting Signal Transducer and Activator of Transcripion (STAT) 3 with Small Molecules
Published:05 Sep 2018
Special Collection: 2018 ebook collectionSeries: Drug Discovery
A. E. Shouksmith and P. T. Gunning, in Small-molecule Transcription Factor Inhibitors in Oncology, ed. K. M. Rahman and D. E. Thurston, The Royal Society of Chemistry, 2018, ch. 6, pp. 147-168.
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Signal transducer and activator of transcription 3 (STAT3) protein, a member of the STAT family of cytosolic signalling proteins, controls the transcription of genes that facilitate and promote several known hallmarks of cancer, including uncontrolled cell proliferation and immortality. Significant efforts have been made to inhibit the action of this oncogenic protein with small molecules, peptides, peptidomimetics, oligonucleotides and organometallic agents. This chapter will describe the progress toward a nanomolar binding, STAT3-selective drug with pharmacological properties suitable for clinical trials and ultimately application in clinical settings against human diseases.