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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]