Abstract: YIGSR peptidomimetics and methods for making and using the same are provided. The subject YIGSR peptidomimetics are non-peptidic, biodegradation-resistant molecules that mimic the pentapeptide tyrosine-isoleucine-glycine-serine-arginine (YIGSR) binding site for the 67 kiloDalton (kDa) laminin binding protein (LBP). The subject peptidomimetics include a rigid or substantially rigid non-peptidic scaffold that effectively presents or positions a tyrosine or tyrosine-like group, an isoleucine or isoleucine-like group, a serine or serine-like group, and an arginine or arginine-like group in substantially the same manner as occurs in the YIGSR peptide itself. The subject peptidomimetics find use in a variety of different applications, including diagnostic and therapeutic applications.