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Biotinylated Cell-penetrating Peptides to Study Intracellular Protein-protein Interactions
Published on: December 20, 2017
Biotinylated Pt(IV) prodrugs with elevated lipophilicity and cytotoxicity
Daniil Spector1,2, Alexander Erofeev1,2, Peter Gorelkin1,2
1Chemistry Department, Lomonosov Moscow State University, Leninskie gory 1, 3, Moscow, 119991, Russia. Krasnovskayao@gmail.com.
Abstract:
A design of Pt(IV) prodrugs with tumor cell targeting moieties leading to increased selectivity is of interest. Herein, we designed a novel Pt(IV) prodrugs with COX-inhibitor naproxen, long-chain hydrophobic stearic acid moiety and biotin as axial ligands. We have established that for Pt(IV) prodrugs with biotin and naproxen or stearate in axial position, the lipophilicity rather than biotin receptors expression is the main factor of cytotoxicity. We also monitored the reduction speed of Pt(IV) prodrug 3 with naproxen and biotin in axial positions in A549 cells using XANES and demonstrated that the prodrug gradually releases cisplatin within 20 hours of incubation.
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