Table 4.
Therapeutic compounds used for autophagy induction or inhibition in cancer.
| Compound | Target | Model system | Autophagy evaluation | References |
|---|---|---|---|---|
| GSK2606414 | PERK | Basal cell carciona (BCC/KMC1) Gastric Adenocarcinoma (AGS) Melanoma (A375) Imiquimod |
↓LC3-II ↓EGFP-LC3-II puncta |
(71) |
| Celastrol | mTOR | Glioma (U251, U87 and C6) Pre-treatment CQ |
↑LC3, BECN1,p62 ↑LC3 puncta ≠LC3-II |
(85) |
| LY294002 UCN-01 (7-hydroxystaurosporine) |
PI3K Akt |
Glioma (U87-MG, U373-MG and T98G) Rapamycin |
↑MDC stain | (86) |
| Rapamycin RAD001 (rapalogue) KU-0063794 (catalytic mTOR inhibitor) WYE-354 (catalytic mTOR inhibitor) |
mTOR | Bladder carcinona (RT112) osteosarcoma (U2OS) neuroblastoma (SK-N-SH) squamous cell carcinoma (HN10) |
↑LC3 punctate (all treatments) ↑LC3 punctate (only with catalytic mTOR inhibitors) |
(87) |
| AZD8055 | mTOR | lung cancer H838 and A549 +E64d/pepstatinA |
↑LC3-II ↑LC3 puncta ↑Acridine orange stain ↑↑LC3-II |
(93) |
| Metformin | AMPK | Melanoma (A375, and SKMel28) Xenograft model |
↑LC3-II, BECN1 ↑LC3 puncta ↑Autophagosomes (TEM) ↑ CatB activity ↑LC3-II ↑LC3 puncta |
(94) |
| Metformin | mTOR | Esophageal squamous cancer cells (ESCC) Pre-treatment 3-MA or CQ Xenograft |
↑LC3-II, BECN1 ↑GFP-LC3 puncta ↑ Autophagosomes (TEM) ↑ Acridine orange and MDC stain ↓LC3-II, BECN1 ↓LC3-II, ↓p62 (IHC) |
(95) |
| Akt inhibitor (1L-6-hydroxymethyl-chiro-inositol 2(R)-2-O-methyl-3-O-octadecylcarbonate) |
AKT | Glioma U87-MG U87-MG ΔEGFR |
↑GFP-LC3 punctate ↑autophagosomes (TEM), ↑Acridine orange stain | (91) |
| Curcumin | Akt/mTOR/p70S6K/4E-BP | Glioma U87-MG and U373-MG Xenograft |
↑GFP-LC3 puncta ↑LC3-II ↑autophagosomes (TEM) ↑ Acridine orange stain ↑LC3-II, ↑LC3 (IHC) |
(92) |
| Quercetin | Akt-mTOR | Breast cancer MCF-7 and MB-231 |
↑LC3-II, LC3 puncta | (89) |
| Quercetin | Akt-mTOR | Gastric adenocarcinoma AGS and MKN28 | ↑ LC3-II, BECN1, ATG7, ATG5/12 ↑ GFP-LC3 puncta ↑ Autophagosomes (TEM) ↑ Acridine orange stain |
(88) |
| AZD1208 | pan-PIM kinase inhibitor | Chronic lymphocytic leukemia (CLL) BafA1 |
↑Acridine orange stain, ↑LC3-II ↑↑LC3-II |
(96) |
| Parthenolide | Oxidative stress downregulation of 4E-BP1 | See Table 2 | See Table 2 | (38) |
| Selenite | eIF2alpha phosphorylation by ROS or ER stress | See Table 2 | See Table 2 | (41, 42) |
| Erastin | Ferroptosis inducer | See Table 2 | See Table 2 | (49, 54) |