Publication | Closed Access
A Photoactivatable Platinum(IV) Complex Targeting Genomic DNA and Histone Deacetylases
94
Citations
26
References
2015
Year
Histone ModificationsEpigenetic ChangeToxic EffectsMolecular BiologyEpigeneticsTumor BiologyPhototoxicityBioimagingAnti-cancer AgentPhotoactivatable PlatinumRadiation OncologyCancer ResearchHealth SciencesPhotochemistryPhotodynamic TherapyNuclear OrganizationTumor TargetingCancer CellsPharmacologyCell BiologyChromatinChromatin RemodelingConjugate ExertsEpigenomicsMedicine
Abstract 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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