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Publication Date:
13 08 2011
ISSN:
1868-503X
DOI:
10.1515/BMC.2011.034

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Editor-in-Chief: Jollès, Pierre / Jörnvall, Hans / Mansuy, Isabelle

null Avila, Jesus / Bollen, Mathieu / Bonetto, Valentina / Cera, Enrico / Jorgensen, Erik / Lagasse, Eric / Norman, Robert / Pinna, Lorenzo / Raghavan, K. Vijay / Venetianer, Pal / Wahli, Walter

6 Issues per year

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

Couture, Frédéric 1 / D'Anjou, François 1 / 1

1Institut de Pharmacologie de Sherbrooke, Université de Sherbrooke, Sherbrooke J1H 5N4, Québec, Canada

Corresponding author

Citation Information: BioMolecular Concepts. Volume 2, Issue 5, Pages 421–438, ISSN (Online) 1868-503X, ISSN (Print) 1868-5021, DOI: 10.1515/BMC.2011.034, August 2011

Publication History:

Received: 30/03/2011;
Accepted: 01/07/2011;
Published Online: 26/02/2012

Abstract

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

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