beta-cyclodextrin/epoxysuccinyl peptide conjugates: new drug targeting system for tumor cells

beta-Cyclodextrin is known to form inclusion complexes with hydrophobic dru gs. Several tumor cell lines are known to secrete and/or contain membrane-a ssociated cathepsin B which is possibly involved in invasion and metastasis . Based on these informations. our recently developed endo-epoxysuccinyl pe ptide inhibitor MeO-Gly-Gly-Leu-(2S,3S)-tEps-Leu-Pro-OH for cathepsin B was conjugated with beta-cyclodextrin to obtain a site-directed drug carrier s ystem. Furthermore, the conjugate was shown to form an inclusion complex wi th the cytotoxic drug methotrexate. (C) 2000 Elsevier Science Ltd. All righ ts reserved.