Therapeutic uses of furin and its inhibitors: a patent review

Abstract

Introduction: 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.

Area covered: 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.

Expert opinion: 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.

Keywords:

• α-1 antitrypsin Portland
• furin
• peptide and peptidomimetic inhibitors
• proprotein convertase

Acknowledgement

F Couture and A Kwiatkowska contributed equally to this work.

Declaration of interest

R Day is an inventor of patents WO2009023306 and WO2013029182. YL Dory is an inventor of patent WO2013029182. The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in orinancial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Notes

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