Journal
CHEMISTRY-A EUROPEAN JOURNAL
Volume 26, Issue 14, Pages 3010-3015Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.201905159
Keywords
cleavable linker; drug delivery; gossypol; imine linkage; tumor-homing peptide
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Funding
- Alexander von Humboldt foundation
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Tumor-targeted drug delivery is highly important for improving chemotherapy, as it reduces the dose of cytotoxic agents and minimizes the death of healthy tissues. Towards this goal, a conjugate was synthesized of gossypol and a MCF-7 cancer cell specific CPP (cell penetrating peptide), thus providing a selective drug delivery system. Utilizing the aldehyde moiety of gossypol, the tumor homing CPP RLYMRYYSPTTRRYG was attached through a semi-labile imine linker, which was cleaved in a traceless fashion under aqueous conditions and had a half-life of approximately 10 hours. The conjugate killed MCF-7 cells to a significantly greater extent than HeLa cells or healthy fibroblasts.
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