Cancer-Cell-Specific Drug Delivery by a Tumor-Homing CPP-Gossypol Conjugate Employing a Tracelessly Cleavable Linker |
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| Authors: | Dr Suman Kumar Maity Paul Stahl Dr Astrid Hensel Prof?Dr Shirley Knauer Dr Christoph Hirschhäuser Prof?Dr Carsten Schmuck |
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| Institution: | 1. Institute of Organic Chemistry, University of Duisburg-Essen, Universitatsstrasse 7, 45117 Essen, Germany;2. Institute for Biology, University of Duisburg-Essen, 45117 Essen, Germany |
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| Abstract: | 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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| Keywords: | cleavable linker drug delivery gossypol imine linkage tumor-homing peptide |
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