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Issue 7, 2017
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Ruthenium-containing P450 inhibitors for dual enzyme inhibition and DNA damage

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Abstract

Cytochrome P450s are key players in drug metabolism, and overexpression in tumors is associated with significant resistance to many medicinal agents. Consequently, inhibition of P450s could serve as a strategy to restore drug efficacy. However, the widespread expression of P450s throughout the human body and the critical roles they play in various biosynthetic pathways motivates the development of P450 inhibitors capable of controlled local administration. Ruthenium complexes containing P450 inhibitors as ligands were synthesized in order to develop pro-drugs that can be triggered to release the inhibitors in a spatially and temporally controlled fashion. Upon light activation the compounds release ligands that directly bind and inhibit P450 enzymes, while the ruthenium center is able to directly damage DNA.

Graphical abstract: Ruthenium-containing P450 inhibitors for dual enzyme inhibition and DNA damage

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Publication details

The article was received on 21 Nov 2016, accepted on 16 Jan 2017 and first published on 17 Jan 2017


Article type: Paper
DOI: 10.1039/C6DT04405K
Citation: Dalton Trans., 2017,46, 2165-2173

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    Ruthenium-containing P450 inhibitors for dual enzyme inhibition and DNA damage

    A. Zamora, C. A. Denning, D. K. Heidary, E. Wachter, L. A. Nease, J. Ruiz and E. C. Glazer, Dalton Trans., 2017, 46, 2165
    DOI: 10.1039/C6DT04405K

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