Patent ID: 7432044

Claim:
A method of identifying a candidate inhibitor substance that inhibits hepsin activation of HGF, said method comprising: a) contacting a candidate substance with a first sample comprising hepsin and a pro-HGF substrate, wherein the pro-HGF substrate is a polypeptide comprising pro-HGF or a fragment thereof comprising a wild type form of the R494-V495 peptide linkage and capable of being cleaved by hepsin, wherein the hepsin is a native hepsin or a hepsin variant having at least about 90% identity to a native hepsin and capable of activating pro-HGF, and wherein hepsin in the sample is in an effective amount for activating said pro-HGF substrate, and (b) comparing amount of pro-HGF substrate activation in the sample with amount of pro-HGF substrate activation in a reference sample comprising similar amounts of hepsin and pro-HGF substrate as the first sample but that has not been contacted with said candidate substance, whereby a decrease in amount of pro-HGF substrate activation in the first sample compared to the reference sample indicates that the candidate substance is capable of inhibiting hepsin activation of single chain HGF (pro-HGF ).