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Dalton Trans. 2017 Feb 14;46(7):2165-2173. doi: 10.1039/c6dt04405k.

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

Author information

1
Departamento de Química Inorgánica and Regional Campus of International Excellence "Campus Mare Nostrum", Universidad de Murcia, and Institute for Bio-Health Research of Murcia (IMIB-Arrixaca), E-30071 Murcia, Spain.
2
Department of Chemistry, University of Kentucky, 505 Rose Street, Lexington, KY 40506, USA. ec.glazer@uky.edu.

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.

PMID:
28121322
DOI:
10.1039/c6dt04405k
[Indexed for MEDLINE]

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