A Photoactivatable Platinum(IV) Complex Targeting Genomic DNA and Histone Deacetylases | Zendy

Kasparkova Jana | Zendy; Kostrhunova Hana | Zendy; Novakova Olga | Zendy; Křikavová Radka | Zendy; Vančo Ján | Zendy; Trávníček Zdeněk | Zendy; Brabec Viktor | Zendy

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A Photoactivatable Platinum(IV) Complex Targeting Genomic DNA and Histone Deacetylases

Author(s) -

Kasparkova Jana,

Kostrhunova Hana,

Novakova Olga,

Křikavová Radka,

Vančo Ján,

Trávníček Zdeněk,

Brabec Viktor

Publication year - 2015

Publication title -

angewandte chemie

Language(s) - English

Resource type - Journals

eISSN - 1521-3757

pISSN - 0044-8249

DOI - 10.1002/ange.201506533

Subject(s) - chemistry , histone deacetylase , histone , histone deacetylase inhibitor , vorinostat , platinum , cancer cell , hydroxamic acid , cytotoxicity , conjugate , dna , drug , epigenetics , biochemistry , cancer research , pharmacology , cancer , biology , stereochemistry , gene , in vitro , genetics , catalysis , mathematical analysis , mathematics

We report toxic effects of a photoactivatable platinum(IV) complex conjugated with suberoyl‐bis‐hydroxamic acid in tumor cells. The conjugate exerts, after photoactivation, two functions: activity as both a platinum(II) anticancer drug and histone deacetylase (HDAC) inhibitor in cancer cells. This approach relies on the use of a Pt IV pro‐drug, acting by two independent mechanisms of biological action in a cooperative manner, which can be selectively photoactivated to a cytotoxic species in and around a tumor, thereby increasing selectivity towards cancer cells. These results suggest that this strategy is a valuable route to design new platinum agents with higher efficacy for photodynamic anticancer chemotherapy.

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