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

Ana Zamora, Catherine A. Denning, David K. Heidary, Erin Wachter, Leona A. Nease, José Ruiz, Edith C. Glazer

Research output: Contribution to journalArticlepeer-review

64 Scopus citations

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.

Original languageEnglish
Pages (from-to)2165-2173
Number of pages9
JournalDalton Transactions
Volume46
Issue number7
DOIs
StatePublished - 2017

Bibliographical note

Publisher Copyright:
© The Royal Society of Chemistry.

ASJC Scopus subject areas

  • Inorganic Chemistry

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