title: Beta-cyclodextrin/epoxysuccinyl peptide conjugates: a new drug targeting system for tumor cells.
abstract: Beta-cyclodextrin is known to form inclusion complexes with hydrophobic drugs. Several tumor cell lines are known to secrete and/or contain membrane-associated cathepsin B which is possibly involved in invasion and metastasis. Based on these information, our recently developed endo-epoxysuccinyl peptide 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 system. Furthermore, the conjugate, was shown to form an inclusion complex with the cytotoxic drug methotrexate.
authors.affiliation: Max-Planck-Institut für Biochemie, Martinsried, Germany.
authors.forename: N
authors.initials: N
authors.lastname: Schaschke
authors.forename: I
authors.initials: I
authors.lastname: Assfalg-Machleidt
authors.forename: W
authors.initials: W
authors.lastname: Machleidt
authors.forename: T
authors.initials: T
authors.lastname: Lassleben
authors.forename: C P
authors.initials: CP
authors.lastname: Sommerhoff
authors.forename: L
authors.initials: L
authors.lastname: Moroder
mesh_terms: D000964:Antimetabolites, Antineoplastic / Q000494:pharmacology; D003505:Cyclodextrins / Q000138:chemical synthesis / Q000494:pharmacology*; D004337:Drug Carriers / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism; D016503:Drug Delivery Systems; D004852:Epoxy Compounds / Q000138:chemical synthesis / Q000494:pharmacology*; D006801:Humans; D002479:Inclusion Bodies / Q000378:metabolism; D008727:Methotrexate / Q000494:pharmacology; D010455:Peptides / Q000138:chemical synthesis / Q000494:pharmacology*; D014407:Tumor Cells, Cultured; D047392:beta-Cyclodextrins
chemical_list: D000964:Antimetabolites, Antineoplastic; D003505:Cyclodextrins; D004337:Drug Carriers; D004852:Epoxy Compounds; D010455:Peptides; D047392:beta-Cyclodextrins; C031215:betadex; D008727:Methotrexate