Table 3.
Potential druggable targets in reprogramming metabolism
Drug | Target | Effect | Function | Refs. |
---|---|---|---|---|
Depletion of Zeb1 | Zeb1 | Weakened aerobic glycolysis | Reprogrammed TAM polarization | [150] |
SGLT1 inhibitor | SGLT1 | Decreased glycolysis | Inhibited M2 polarization | [152] |
MIF-CD74 blockade | MIF-CD74 | Decreased lactate production | Promoted M1 infiltration | [156] |
TLR9 agonist CpG ODN | Wnt2b/β-catenin | Decreased glycolysis | Suppressed M2 polarization | [159] |
Rapamycin | mTOR | Remodelled glycolysis metabolism | Reprogrammed M2 to M1 | [161] |
GARP or integrin inhibitors | GARP/integrin | Upregulated glucose metabolism and OXPHOS gene expression | Restored M1 anti-tumour effect | [163] |
Nanoplatform deliver MGLL siRNA and CB-2 siRNA | MGLL/CB-2 | Inhibited free fatty acid production | Reprogrammed TAMs to polarize into M1 macrophages | [164] |
ABHD5 inhibitor | ABHD5/SRM | Inhibited lipolysis of triglycerides into diglycerides and free fatty acids | Reprogrammed TAM polarization | [165, 166] |
PERK inhibitor | PERK | Inhibited glutamine utilization and α-KG concentration | Reduced TAM activity | [167] |
Slit2 activator | Slit2 | Increased glycolysis, reduced FAO, reduced α-KG-to-succinic acid ratio | Promoted M1 polarization | [168,169] |
Nanotherapeutics loaded with TLR7/8 agonist and FAO inhibitor | TLR7/8 | Inhibited TCA cycle, upregulated glycolytic metabolic pathway | Reprogrammed M2 to M1 | [35] |
RIPK3 upregulation | RIPK3 | Increased anaerobic glycolysis | Contributed to M1 polarization | [171,172] |