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A STAT inhibitor patent review: progress since 2011.
Ping-Shan Lai1, David A Rosa1, Ahmed Magdy Ali1
1a University of Toronto Mississauga, Department of Chemical and Physical Sciences , 3359 Mississauga Road North, Mississauga, Ontario L5L 1C6, Canada +1 90 55 69 45 88 ; +1 90 55 69 49 29 ; patrick.gunning@utoronto.ca.
Expert Opinion on Therapeutic Patents
|September 24, 2015
Summary
Directly targeting STAT3 and STAT5 proteins for cancer treatment shows promise, with numerous patented inhibitors emerging. However, no direct STAT3 inhibitor is currently in clinical use, indicating further research is needed.
Area of Science:
- Medicinal Chemistry
- Drug Discovery
- Oncology
Background:
- The clinical utility of direct STAT3 and STAT5 inhibitors for various diseases, including cancer, is well-established.
- STAT proteins play crucial roles in cellular signaling pathways implicated in disease pathogenesis.
Purpose of the Study:
- To review STAT inhibitor patent literature from 2011-2015, focusing on STAT3, STAT5a/b, and STAT1.
- To analyze the mode of inhibition, target sites, evaluated indications, and relative potency of patented STAT inhibitors.
Main Methods:
- Comprehensive review of patent literature concerning STAT inhibitors.
- Analysis of inhibition mechanisms, target domains (SH2, DNA-binding, N-terminal), and chemical classes.
- Evaluation of therapeutic indications and inhibitor potency.
Main Results:
- Multiple STAT3 and STAT5 inhibitors across diverse chemotypes have been patented.
- The SH2 domain is a common but not exclusive target; DNA-binding and N-terminal regions are emerging targets.
- No direct STAT3 inhibitor has reached clinical approval yet.
Conclusions:
- Significant progress has been made in patenting STAT3 and STAT5 inhibitors, but clinical translation remains a challenge.
- Future research should explore novel inhibition sites beyond the SH2 domain.
- Further development is required to bring effective direct STAT inhibitors to the clinic.
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