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Fibroblast activation protein (FAP)

In vitro studies identified a boronic acid-based inhibitor of FAP that could be useful for treating cancer. Increased FAP activity is associated with various cancers. In cellular and enzymatic assays, the boronic acid-based molecule ARI-3009 inhibited FAP endopeptidase activity with low nanomolar potency and showed selectivity for the enzyme over dipeptidyl peptidases (DPPs) and prolyl endopeptidase (PREP). Next steps include testing the inhibitor in animal disease models.
Vantia Therapeutics Ltd. has the FAP inhibitor VA999260 in preclinical testing to treat cancer.

SciBX 6(20); doi:10.1038/scibx.2013.487
Published online May 23, 2013

Covered by issued and filed patents; licensed to Arisaph Pharmaceuticals Inc.; available for partnering

Poplawski, S.E. et al. J. Med. Chem.; published online April 17, 2013;
Contact: William W. Bachovchin, Tufts University Sackler School of Biomedical Sciences, Boston, Mass.