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Prostate cancer

Proprotein convertase subtilisin/kextin type 6 (PCSK6; PACE4)

In vitro studies identified a selective PACE4 inhibitor that could help treat prostate cancer. SAR studies identified a peptide sequence that selectively inhibited the cancer-associated PACE4 with more than 20-fold selectivity over furin, a closely related proprotein convertase required by normal tissues. In PACE4-expressing prostate cancer cell lines, the peptide decreased cell proliferation compared with vehicle and induced cell cycle arrest. Next steps include toxicity and pharmacokinetic studies.

SciBX 5(46); doi:10.1038/scibx.2012.1205
Published online Nov. 29, 2012

Patent applications filed; undisclosed partner has option to license technology; unavailable for licensing

Levesque, C. et al. J. Med. Chem.; published online Nov. 5, 2012;
Contact: Robert Day, University of Sherbrooke, Sherbrooke, Quebec, Canada