Provided are
fibroblast activation
protein alpha (FAPα)-cleavable pro-peptides that find use in treating conditions associated with FAPα expression. The FAPα-cleavable pro-peptides also find use in imaging locations of FAPα activity
in vivo. In some embodiments, a pro-
peptide of the present disclosure comprises a membrane interacting domain, a masking domain, and a FAPα cleavage site. The masking domain, when linked to the membrane interacting domain, is effective to inhibit interaction of the membrane interacting domain with a
phospholipid bilayer. The FAPα cleavage site is disposed between the membrane interacting domain and the masking domain. The membrane interacting domain may be conjugated to one or more therapeutic agents, non-limiting examples of which include radioisotopes. Also provided are methods of treating a condition associated with FAPα expression in a subject in need thereof, such methods comprising administering an effective amount of a pro-
peptide of the present disclosure to the subject.