Litcius/Paper detail

Impact of Mitochondrial Targeting Antibiotics on Mitochondrial Function and Proliferation of Cancer Cells

Edward J. Cochrane, James Hulit, Franz P. Lagasse, Tanguy Lechertier, Brett Stevenson, Corina Tudor, Diana Trebicka, Tim Sparey, Andrew J. Ratcliffe

2021ACS Medicinal Chemistry Letters31 citationsDOIOpen Access PDF

Abstract

Some marketed antibiotics can cause mitochondria dysfunction via inhibition of the mitochondrial translation process. There is great interest in exploiting such effects within a cancer setting. To enhance accumulation of antibiotics within the mitochondria of cancer cells, and therefore delivery of a greater potency payload, a mitochondrial targeting group in the form of a triphenylphosphonium (TPP) cation was appended via an alkyl chain length consisting of 7 to 11 carbons to the ribosomal antibiotics azithromycin and doxycycline. Using MDA-MB-231 cells, the effects of each subseries on mitochondrial translation, mitochondrial bioenergetics, and cell viability are described.

Topics & Concepts

MitochondrionDoxycyclineMitochondrial ribosomeAntibioticsMitochondrial DNARibosomal RNACancer cellBioenergeticsChemistryAzithromycinBiologyCell biologyCancerBiochemistryRibosomeGeneGeneticsRNAMitochondrial Function and PathologyATP Synthase and ATPases ResearchCancer, Hypoxia, and Metabolism