title: A STAT inhibitor patent review: progress since 2011.
abstract: BACKGROUND
  The clinical utility of effective direct STAT inhibitors, particularly STAT3 and STAT5, for treating cancer and other diseases is well studied and known.
  
  
  METHODS
  This review will highlight the STAT inhibitor patent literature from 2011 to 2015 inclusive. Emphasis will be placed on inhibitors of the STAT3, STAT5a/b, and STAT1 proteins for cancer treatment. The review will, where suitably investigated, describe the mode and the site of inhibition, list indications that were evaluated, and rank the inhibitor's relative potency among compounds in the same class. The reader will gain an understanding of the diverse set of approaches, used both in academia and industry, to target STAT proteins.
  
  
  CONCLUSIONS
  There is still much work to be done to directly target the STAT3 and STAT5 proteins. As yet, there is still no direct STAT3 inhibitor in the clinic. While the SH2 domain remains a popular target for therapeutic intervention, the DNA-binding domain and N-terminal region are now attracting attention as possible sites for inhibition. Multiple putative STAT3 and STAT5 inhibitors have now been patented across a broad spectrum of chemotypes, each with their own advantages and limitations.
authors.affiliation: a 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.
authors.forename: Ping-Shan
authors.initials: PS
authors.lastname: Lai
authors.affiliation: a 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.
authors.forename: David A
authors.initials: DA
authors.lastname: Rosa
authors.affiliation: a 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.
authors.forename: Ahmed
authors.initials: A
authors.lastname: Magdy Ali
authors.affiliation: a 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.
authors.forename: Rodolfo F
authors.initials: RF
authors.lastname: Gómez-Biagi
authors.affiliation: a 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.
authors.forename: Daniel P
authors.initials: DP
authors.lastname: Ball
authors.affiliation: a 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.
authors.forename: Andrew E
authors.initials: AE
authors.lastname: Shouksmith
authors.affiliation: a 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.
authors.forename: Patrick T
authors.initials: PT
authors.lastname: Gunning
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology; D015195:Drug Design; D006801:Humans; D058990:Molecular Targeted Therapy; D009369:Neoplasms / Q000188:drug therapy / Q000473:pathology; D010330:Patents as Topic; D050794:STAT1 Transcription Factor / Q000037:antagonists & inhibitors*; D050796:STAT3 Transcription Factor / Q000037:antagonists & inhibitors*; D050799:STAT5 Transcription Factor / Q000037:antagonists & inhibitors*
chemical_list: D000970:Antineoplastic Agents; D050794:STAT1 Transcription Factor; D050796:STAT3 Transcription Factor; D050799:STAT5 Transcription Factor
keywords: JAK/STAT pathway; anti-cancer drugs; cancer therapeutics; molecular therapeutics; oncogene; protein–protein interactions; signal transducer and activator of transcription 3 (STAT3)