Table 5.
Potential pre-clinical lysosome-targeted interventions for tumors
| Classification | Intervention | Outcome | Reference |
|---|---|---|---|
| Autophagy activator | Rapamycin | Rapamycin suppresses M2 macrophage polarization | [253] |
| Sorafenib | Sorafenib suppresses classical macrophage activation | [324] | |
| Autophagy inhibitor | Hydroxychloroquine | Chloroquine and hydroxychloroquine switches TAMs from M2 to M1 phenotype | [275, 276] |
| Chloroquine | |||
| Bafilomycin A1 | Bafilomycin A1-induced M1-like polarization by preventing NF-κB degradation | [256] | |
| 3-Methyladenine | 3-Methyladenine prevents cross-talk between cancer cells and CAF through autophagy | [305] | |
| Cathepsin B inhibitor | CA074Me | CA074Me inhibits cell invasion and inflammasome activation | [192, 289] |
| CA-074 | CA-074 inhibits EMT | [195] | |
| Cathepsin S inhibitor | Fsn0503 | Fsn0503 inhibits cell invasion | [286] |
| Cathepsin L inhibitor | Z-FY-CHO | Z-FY-CHO inhibits radio-resistance | [214] |
| KGP94 | KGP94 and KGP207 inhibits cancer cell invasion and M2-like TAMs | [284] | |
| KGP207 | |||
| General cysteine cathepsin inhibitor | E64 | E64 inhibits cell invasion | [283] |
| JPM-OEt | JPM-OEt inhibits drug resistance, tumorigenesis, angiogenesis, proliferation, and invasion | [197, 254, 279] | |
| Transfection vehicle | Ghost | Ghost is applied for transfection of LAMP2A siRNA in TAMs | [260] |
| PEG = MT/PC NPs | PEG = MT/PC NPs is applied for transfection of VEGF and PIGF siRNA | [330] | |
| Porous silicon micro-particles | Porous silicon micro-particles is applied for delivering HER2 antigen into DCs | [334] | |
| Lipid-coated calcium phosphate nanoparticles | Lipid-coated calcium phosphate nanoparticles is applied for delivering antigen TRP2 mRNA and PD-1 siRNA | [335] | |
| Metal–organic framework | Metal–organic framework is applied for delivering tumor-associated antigens into macrophages | [336] | |
| TAM remover | M-chlorin | M-chlorin can enter lysosomes and delete M2 macrophages | [430] |
| DOX-SPCL | DOX-SPCL concentrates in lysosomes and delete macrophages | [332] | |
| MEN 4901/T-0128 | MEN 4901/T-0128 releases cytotoxic T-2513 in lysosomes | [333] | |
| TLR3 agonist | Poly(I:C) | Poly(I:C) activates M1 macrophages | [262] |
| TLR4 agonist | LPS | LPS activates M1 macrophages | [262] |
| Polyethyleneimine | Polyethyleneimine reverses M2-like polarization | [264] | |
| Cationic dextran | Cationic dextran reverses M2-like polarization | [264] | |
| Multiwalled carbon nanotubes | Multiwalled carbon nanotubes reverses M2-like polarization | [265] | |
| TLR7 agonist | CL264 | CL264 reverses M2-like polarization | [262] |
| 1V270 | 1V270 reverses M2-like polarization | [266] | |
| Gardiquimod | Gardiquimod increases M1-like polarization | [267] | |
| Let-7b | Let-7b reverses M2-like polarization and suppresses IL-10 production | [268] | |
| R848 | R848 increases M1-like polarization | [269] | |
| R837 | R837 enhances anti-tumor immunity | [338] | |
| TLR9 agonist | CpG ODN | CpG ODN potentiates antigen presentation in macrophages | [270] |
| Other | Spermine modified pullulan | Spermine modified pullulan can enter lysosomes and reprogram M2 macrophages to M1 | [337] |