title: Therapeutic uses of furin and its inhibitors: a patent review.
abstract: BACKGROUND
  Since the discovery of furin, numerous reports have studied its role in health and diseases, including cancer, inflammatory and infectious diseases. This interest has led to the development of both large protein- and peptide-based inhibitors aiming to control furin activity to treat these disorders. The most recent advances include the development of potent peptidomimetic furin inhibitors, considerably expanding the field of therapeutic applications.
  
  
  METHODS
  In this review, the use of furin or its inhibitors for therapeutic conditions is described through the patent literature since 1994. Only compounds with biological efficacy or augmented properties demonstrated within the patent literature or the associated publications concerning their claimed uses are discussed.
  
  
  CONCLUSIONS
  Considering the diseases that may benefit from furin inhibition, several patents detail the use of the restricted number of furin inhibitors. However, there have been recent reports of new scaffolds, and even the use of furin itself, as a therapeutic agent. Despite considerable evidence of in vivo efficacy, limited confirmation from clinical trials supports or refutes the further use of these compounds in a therapeutic context. The most advanced application is the use of furin knockdown in the generation of an autologous cancer vaccine, which has initiated clinical trials.
authors.affiliation: Université de Sherbrooke, Institut de Pharmacologie de Sherbrooke, Department of Surgery/Urology Division, Faculté de Médecine et des Sciences de la Santé , 3001 12e Ave. Nord, Sherbrooke, Québec, J1H 5N4 , Canada +1 819 564 5428 ; +1 819 564 5400 ; robert.day@usherbrooke.ca.
authors.forename: Frédéric
authors.initials: F
authors.lastname: Couture
authors.forename: Anna
authors.initials: A
authors.lastname: Kwiatkowska
authors.forename: Yves L
authors.initials: YL
authors.lastname: Dory
authors.forename: Robert
authors.initials: R
authors.lastname: Day
mesh_terms: D000818:Animals; D019496:Cancer Vaccines / Q000494:pharmacology; D002986:Clinical Trials as Topic; D015195:Drug Design; D045683:Furin / Q000037:antagonists & inhibitors / Q000378:metabolism* / Q000627:therapeutic use; D055785:Gene Knockdown Techniques; D006801:Humans; D010330:Patents as Topic; D057786:Peptidomimetics / Q000494:pharmacology*
chemical_list: D019496:Cancer Vaccines; D057786:Peptidomimetics; D045683:Furin
keywords: furin; peptide and peptidomimetic inhibitors; proprotein convertase; α-1 antitrypsin Portland