title: A cell-penetrating peptidic GRP78 ligand for tumor cell-specific prodrug therapy.
abstract: Tumor targeting peptides are promising vehicles for site-directed cancer therapy. Pep42, a cyclic 13-mer oligopeptide that specifically binds to glucose-regulated protein 78 (GRP78) and internalized into cancer cells, represents an excellent vehicle for tumor cell-specific chemotherapy. Here, we report the synthesis and evaluation of Pep42-prodrug conjugates that contain a cathepsin B-cleavable linker, resulting in the traceless release of drug inside the cancer cells.
authors.affiliation: Department of Chemistry, The Skaggs Institute for Chemical Biology, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.
authors.forename: Yoshiyuki
authors.initials: Y
authors.lastname: Yoneda
authors.forename: Sebastian C J
authors.initials: SC
authors.lastname: Steiniger
authors.forename: Katerina
authors.initials: K
authors.lastname: Capková
authors.forename: Jenny M
authors.initials: JM
authors.lastname: Mee
authors.forename: Ying
authors.initials: Y
authors.lastname: Liu
authors.forename: Gunnar F
authors.initials: GF
authors.lastname: Kaufmann
authors.forename: Kim D
authors.initials: KD
authors.lastname: Janda
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D004305:Dose-Response Relationship, Drug; D000091342:Endoplasmic Reticulum Chaperone BiP; D006360:Heat-Shock Proteins / Q000737:chemistry*; D006801:Humans; D008024:Ligands; D018832:Molecular Chaperones / Q000737:chemistry*; D015394:Molecular Structure; D010456:Peptides, Cyclic / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D000091342:Endoplasmic Reticulum Chaperone BiP; C000717247:HSPA5 protein, human; D006360:Heat-Shock Proteins; D008024:Ligands; D018832:Molecular Chaperones; C513552:Pep42 peptide; D010456:Peptides, Cyclic