The Pan-Sirtuin Inhibitor MC2494 Regulates Mitochondrial Function in a Leukemia Cell Line

Frontiers in Oncology
Vincenzo CarafaLucia Altucci

Abstract

The involvement of sirtuins (SIRTs) in modulating metabolic and stress response pathways is attracting growing scientific interest. Some SIRT family members are located in mitochondria, dynamic organelles that perform several crucial functions essential for eukaryotic life. Mitochondrial dysfunction has emerged as having a key role in a number of human diseases, including cancer. Here, we investigated mitochondrial damage resulting from treatment with a recently characterized pan-SIRT inhibitor, MC2494. MC2494 was able to block mitochondrial biogenesis and function in terms of ATP synthesis and energy metabolism, suggesting that it might orchestrate cell response to metabolic stress and thereby interfere with cancer promotion and progression. Targeting mitochondrial function could thus be considered a potential anticancer strategy for use in clinical therapy.

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Citations

Dec 15, 2020·World Journal of Stem Cells·Xu Gao, Qiong-Zhu Dong
Jun 9, 2021·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Yi WangBo Liu

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Datasets Mentioned

BETA
PXD017508

Methods Mentioned

BETA
FACS
Assay
Protein Assay
Profiler
aminoacylation
fluorescence-activated cell sorting
acetylation

Software Mentioned

CellQuest
Bipartite
Profiler
Leica
Seahorse
SEQUEST HT
GOSt
Proteome Discoverer
GraphPad Prism
FunRich

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