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Table 2 Drugs targeting CSC metabolism

From: Crosstalk between autophagy and metabolic regulation of cancer stem cells

Metabolism-based strategies Compound Mechanism of action CSC or tumor type Reference
Glycolysis inhibition 2-Deoxy-D-glucose Glycolysis inhibitor Breast CSCs [21]
3-BP Glycolysis inhibitor Glioblastoma CSCs, PDACs [56]
DCA Metabolic shift from glycolysis to OXPHOS GBM cells [57]
Inhibition of mitochondrial respiration Metformin Complex I inhibitor Pancreatic CSCs, CSCs of HT29 cell line derived from colorectal cancer [32, 58]
Phenformin
Rotenone
Antimycin-A Complex III inhibitor Lung CSCs [59,60,61,62]
Bedaquiline Complex V inhibitor Breast CSCs
Oligomycin Complex V inhibitor Glioblastomas
Salinomycin analogs Lysosomal iron sequestration Breast CSCs [63]
Impairs autophagic flux Breast CSCs [64]
Interference with ABC transporters Breast, AML, lung, gastric, osteosarcoma, colorectal, pancreatic and prostate CSCs [65]
Activation of the Wnt/β-catenin signaling pathway
188Re-Liposome Mitophagy inhibitor Ovarian CSCs [66]
Doxycycline Mitochondrial biogenesis inhibitor and inducer of apoptosis Breast and cervical CSCs [67, 68]
XCT-790 ETC uncoupler, mitochondrial biogenesis inhibitor, inhibitor of ERRα-PGC-1 signaling pathway Breast CSCs [31]
Mdivi-1 Fission inhibitor, inhibitor of assembly of Drp1 and its GTPase activity Breast CSC, brain tumor initiating cells [69, 70]
Redox homeostasis and antioxidant signaling Zaprinast Inhibition of glutathione biosynthesis, glutaminase inhibitor Non-small lung and glutamine-addicted pancreatic cancer cell lines [30, 59, 71]
BPTES
968
BSO
Apigenin Neutralizer of ROS-induced NRF2 activity, STAT3 signaling pathway inhibitor, inhibitor of the NRF2 and NF-ƙB pathways Ovarian and prostate CSCs, triple-negative breast cancers, leukemia stem-like cells [72,73,74,75,76]
ATRA
Brusatol
Disulfiram
Trigonelline
Lipid metabolism 2M14NQ Blocks CD36 activity and fatty acid uptake Glioblastoma CSCs [77]
Soraphen A Inhibitor of ACC Breast CSCs [78,79,80]
Chloroquine Inhibition of autophagy Breast CSCs [15, 64]
TVB-2640 FASN inhibitor Breast CSCs [78]
MF-438 SCD-1 inhibitor, inhibitor of FAO Lung CSCs, liver cancer, glioblastoma and AML cells [81, 82]
SSI-4
A939572
Etomoxir
ST1326 Inhibition of FAO AML cells [83, 84]
Avocatin B
Emodin ACLY inhibitor Lung CSCs [85]
TVB-2640 Inhibitor of HMG-COAR, inhibitor of cholesterol synthesis through the mevalonate pathway Breast and brain CSCs [34, 86]