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Biomolecular Concepts

Editor-in-Chief: Di Cera, Enrico

Covered by Web of Science (BIOSIS Previews)

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CiteScore 2018: 3.35

SCImago Journal Rank (SJR) 2018: 1.475
Source Normalized Impact per Paper (SNIP) 2018: 0.825

ICV 2018: 124.31

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Volume 2, Issue 5


On the cutting edge of proprotein convertase pharmacology: from molecular concepts to clinical applications

Frédéric Couture
  • Institut de Pharmacologie de Sherbrooke, Université de Sherbrooke, Sherbrooke J1H 5N4, Québec, Canada
  • Other articles by this author:
  • De Gruyter OnlineGoogle Scholar
/ François D'Anjou
  • Institut de Pharmacologie de Sherbrooke, Université de Sherbrooke, Sherbrooke J1H 5N4, Québec, Canada
  • Other articles by this author:
  • De Gruyter OnlineGoogle Scholar
/ Robert Day
Published Online: 2011-08-13 | DOI: https://doi.org/10.1515/BMC.2011.034


There is increasing interest in the therapeutic targeting of proteases for the treatment of important diseases. Additionally new protein-based therapeutic strategies have the potential to widen the available treatments against these pathologies. In the last decade, accumulated evidence has confirmed that the family of proteases known as proprotein convertases (PCs) are potential targets for viral infections, osteoarthritis, cancer and cardiovascular disease, among others. Nevertheless, there are still many unanswered questions about the relevance of targeting PCs in a therapeutic context, especially regarding the anticipated secondary effects of treatment, considering the observed embryonic lethality of some PC knockout mice. In this review, the benefits of PCs as pharmacological targets will be discussed, with focus on concepts and strategies, as well as on the state of advancement of actual and future inhibitors.

Keywords: drug design; inhibitors; peptidomimetics; peptides as drugs; proprotein convertases; therapeutic applications; translational medicine

About the article

Corresponding author

Received: 2011-03-30

Accepted: 2011-07-01

Published Online: 2011-08-13

Published in Print: 2011-10-01

Citation Information: BioMolecular Concepts, Volume 2, Issue 5, Pages 421–438, ISSN (Online) 1868-503X, ISSN (Print) 1868-5021, DOI: https://doi.org/10.1515/BMC.2011.034.

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