Table 2 Existing lactylation-related drugs
From: Lactylation modification in cancer: mechanisms, functions, and therapeutic strategies
Cancers | Drugs | Trial | Outcomes | Adverse effect | PMID |
|---|---|---|---|---|---|
Soild cancer | 2-DG | Phase I/II | 2DG at 63 mg/kg in combination with weekly docetaxel was well-tolerated in this study and is the recommended phase II dose for daily 2DG administrationr | Fatigue, Sweating, Dizziness and Nausea | [123] |
NSCLC | Fargesin | In vitro/In vivo | Targeting PKM2 to disrupt histone H3 lactylation inhibits tumorigenesis in NSCLC. | —— | [124] |
Glioblastoma Multiforme | Dexmedetomidine | In vitro | Inhibit the lactylation of c-Myc reduces protein stability, thereby suppressing the migration, invasion, and glycolysis of GBM cells. | Hypertension, Hypotension, or Bradycardia | [125] |
Ovarian cancer | Tanshinone I | In vitro/In vivo | Inhibition of lactate production reduces the level of H3K18la, thereby decreasing the expression of tumor-associated genes. | —— | [126] |
HCC | Royal jelly acid | In vitro/In vivo | Disrupt lactate production and inhibit the lactylation of H3K9la and H3K14la sites to suppress the development of HCC. | —— | [132] |
HCC | Demethylzeylasteral | In vitro/In vivo | Inhibiti the lactylation of histone H3 to suppress the tumorigenicity induced by liver cancer stem cells. | Potential hepatotoxicity | [133] |
Prostate cancer | Evodiamine | In vitro/In vivo | Restricting histone lactylation and the expression of HIF1A in PCa cells significantly blocks lactate-induced angiogenesis. | Hepatotoxicity | [134] |
HCC | Honokiol | Phase I (NSCLC) | Activating SIRT3 induces apoptosis in HCC by regulating the level of Kla on CCNE2. | Hepatotoxicity | [135] |