Cancer‐Cell‐Specific Drug Delivery by a Tumor‐Homing CPP‐Gossypol Conjugate Employing a Tracelessly Cleavable Linker | Zendy

Maity Suman Kumar | Zendy; Stahl Paul | Zendy; Hensel Astrid | Zendy; Knauer Shirley | Zendy; Hirschhäuser Christoph | Zendy; Schmuck Carsten | Zendy

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Cancer‐Cell‐Specific Drug Delivery by a Tumor‐Homing CPP‐Gossypol Conjugate Employing a Tracelessly Cleavable Linker

Author(s) -

Maity Suman Kumar,

Stahl Paul,

Hensel Astrid,

Knauer Shirley,

Hirschhäuser Christoph,

Schmuck Carsten

Publication year - 2020

Publication title -

chemistry – a european journal

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.687

H-Index - 242

eISSN - 1521-3765

pISSN - 0947-6539

DOI - 10.1002/chem.201905159

Subject(s) - linker , homing (biology) , conjugate , drug delivery , cancer research , drug , medicine , pharmacology , chemistry , biology , computer science , mathematics , organic chemistry , mathematical analysis , ecology , operating system

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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