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. 2021 May 14;14:79. doi: 10.1186/s13045-021-01087-1

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]