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ID: ALA1141627

Journal: Bioorg Med Chem Lett

Title: A cell-penetrating peptidic GRP78 ligand for tumor cell-specific prodrug therapy.

Authors: Yoneda Y, Steiniger SC, Capková K, Mee JM, Liu Y, Kaufmann GF, Janda KD.

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.

CiteXplore: 18243696

DOI: 10.1016/j.bmcl.2008.01.060