Patent ID: 6896870

Claim:
A UPA active site-targeting peptide compound that binds to the endosite and one or more exosites of (i) tcupA or (ii) a fragment or subunit of tcupA, which fragment or subunit retains the UPA (1) enzymatic endosite and (2) a uPAR-binding epitope, such that said peptide compound covalently modifies the endosite; said peptide compound being a member of the group consisting of: (a) (Chelator)-(Xaa) 2-6 -(Lys,Arg)-(alkylating group)-uPA; (b) (Label-Chelator)-(Xaa) 2-6 -(Lys,Arg)-(alkylating group)-uPA; (c) (Labels (Xaa) 2-6 -(Lys,Arg)-(alkylating group)-uPA; and (d) (Therapeutic moiety)-(Xaa) 2-6 -(Lys,Arg)-(alkylating group)-uPA; wherein Label is a detectable label, each Xaa is independently an amino acid; and wherein the peptide compound localizes said chelator, detectable label or therapeutic moiety to the uPA active site.