A cell-penetrating peptidic GRP78 ligand for tumor cell-specific prodrug therapy.
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.
Yoneda
Yoshiyuki
Y
Department of Chemistry, The Skaggs Institute for Chemical Biology, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.
Steiniger
Sebastian C J
SC
Capková
Katerina
K
Mee
Jenny M
JM
Liu
Ying
Y
Kaufmann
Gunnar F
GF
Janda
Kim D
KD
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*
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