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

  • Bioorg Med Chem Lett. 2008 Mar 1;18(5):1632-6. doi: 10.1016/j.bmcl.2008.01.060.
Yoshiyuki Yoneda  1 ,  Sebastian C J Steiniger ,  Katerina Capková ,  Jenny M Mee ,  Ying Liu ,  Gunnar F Kaufmann ,  Kim D Janda
Affiliations
  • 1. Department of Chemistry, The Skaggs Institute for Chemical Biology, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.
PMID: 18243696 DOI: 10.1016/j.bmcl.2008.01.060
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.

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