Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 5, Pages 1632-1636Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.01.060
Keywords
cell-penetrating peptide; prodrug; chemotherapy; doxorubicin
Categories
Funding
- NCI NIH HHS [R01 CA094193, R01 CA094193-02, R01 CA094193-03, R01 CA094193-01A2, R01 CA094193-04, CA 094193] Funding Source: Medline
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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. (c) 2008 Elsevier Ltd. All rights reserved.
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