Comparative analysis of senolytic drugs reveals mitochondrial determinants of efficacy and resistance

作者信息Masahiro Wakita, Koyu Ito, Kaho Fujii, Dai Sakamoto, Takumi Mikawa, Sho Sugawara, Xiangyu Zhou, Jeong Hoon Park, Hideka Miyagawa, Daisuke Motooka, Emi Ogasawara, Naotada Ishihara, Akiko Takahashi, Hiroshi Kondoh, Eiji Hara
PMID41611832
期刊Nat Aging
发布时间2026-01-29
DOI10.1038/s43587-025-01057-z
查看来源

摘要

Cellular senescence contributes to aging and disease, and senolytic drugs that selectively eliminate senescent cells hold therapeutic promise. Although over 20 candidates have been reported, their relative efficacies remain unclear. Here we systematically compared 21 senolytic agents using a senolytic specificity index, identifying the Bcl-2 inhibitor ABT263 and the BET inhibitor ARV825 as most effective senolytics across fibroblast and epithelial senescence models. However, even upon extended treatment with these most potent senolytics, a proportion of senescent cells remained viable. We found that senolytic resistance was driven by maintenance of mitochondrial integrity through V-ATPase-mediated clearance of damaged mitochondria. Imposing mitochondrial stress via metabolic workload enhanced the senolytic efficacies of ABT263 and ARV825 in vitro, and in mouse models, ketogenic diet adoption or SGLT2 inhibition similarly potentiated ABT263-induced and ARV825-induced senolysis, reducing metastasis and tumor growth. These findings suggest that mitochondrial quality control is a key determinant of resistance to ABT263-induced and ARV825-induced senolysis, providing a possible framework for rational combination senotherapies.

实验方法

产品清单

名称品牌货号
Freestyle血糖监测系统Abbott Laboratories71386-80, 80224-75
一体式荧光显微镜 (BZ-710)KeyenceBZ-710
ImageQuant 800CytivaImageQuant 800
Seahorse XFe24细胞外通量分析仪Agilent Technologies--
XFe24细胞培养微孔板Agilent Technologies--
StepOnePlus PCR系统Applied Biosystems--
Illumina NovaSeq 6000测序仪Illumina--
Illumina NovaSeq X Plus平台Illumina--
Agilent生物分析仪Agilent--