2. Academic Validation
  3. A cell-penetrating peptidic GRP78 ligand for tumor cell-specific prodrug therapy

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

Affiliation

  • 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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