Table 1 Summary of mitochondrial targets for cancer therapy

Mitochondrial ETC and OXPHOS

Complex I

Piericidin [220]; rotenone [221]; deguelin [222]; tamoxifen [123, 223]; metformin [224]; ME-344 [225]

Complex II

α-TOS [226]; MitoVES [227]

Complex III

Resveratrol [228];

Complex IV

Fenretinide [229];

Complex V

BZ-423 [230]

Targeting the mitochondrial metabolic pathway

Heme synthesis

Cyclopamine tartrate (CycT) [231]; HasA [232]

1C metabolism (SHMT1 and SHMT2)

AGF291, AGF320, and AGF347 [233, 234]; lometrexol [235]

DHODH

leflunomide [236, 237]

Nucleotide biosynthesis

IACS-010759 [238]

TCA cycle (α-ketoglutarate dehydrogenase (α-KGDH) and pyruvate dehydrogenase (PDH)

CPI-613 [239]

Glutaminase (GLS)

CB-839 [240], bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl) ethyl sulfide (BPTES) [241]

Glutamate-pyruvate transaminase 2 (GPT2)

Aminooxyacetate (AOA) [54]

Redox balance

NADH:ubiquinone oxidoreductase

SMIP004-7 [242];

Ca²⁺ homeostasis

VDACs and ANT

lonidamine[243], steroid analogs [244]

Na⁺/Ca²⁺ exchanger

CGP-37157 [245]

Bcl-2

Gossypol [246]

S100A4

Niclosamide [247]

Mitochondrial membrane proteins

Hexokinase II

3-bromopyruvate [248]; 2-Deoxyglucose (2-DG) [249]