Table 3.
Tumor-targeted drug therapy based on m6A methylation
Drug name | Targeting | Tumor | Functions | References |
---|---|---|---|---|
Curcumin | ALKHB5 | NA | Curcumin reduces ALKHB5 (m6A demethylase) expression in a m6A methylation-dependent manner to inhibit adipogenesis | [329] |
Quercetin | METTL3 | Cervical cancer | Quercetin acts synergistically with cisplatin to inhibit migration and invasion of cervical cancer cells by suppressing expression of METTL3 | [330] |
Baicalin | FTO/ALKBH5 | Nasopharyngeal carcinoma | Baicalein affects genomic stability to inhibit tumor growth by mediating increase in METTL3 and METTL14 and decreases in FTO and ALKBH5 | [331] |
Saikosaponin | FTO | Myelomonocytic leukemia | Saikosaponin sensitizes myelomonocytic leukemia cells to tyrosine kinase inhibitors by suppressing FTO to rescue m6A hypermethylation in MYC and RARA | [332] |
Simvastatin | METTL3 | Lung cancer | Simvastatin mediates METTL3 downregulation and affects epithelial mesenchymal transition through m6A methylation of EZH2 mRNA, thereby inhibiting malignant progression of lung cancer | [333] |
DAC51 | FTO | Melanoma | Dac51 blocks FTO-mediated regulation of glycolytic metabolism and prevents tumor immune evasion by inhibiting FTO activity | [129] |
Meclofenamic acid | FTO | Cervical cancer | Selective inhibition of FTO demethylation of ALKBH5 via m6A methylation | [276] |
Alk-04 | ALKBH5 | Melanoma | Inhibition of ALKBH5 to regulate Mct4/Slc16a3 expression and lactate content in TME and the composition of tumor-infiltrating Treg and MDSCs | [157] |
miR-4429 | METTL3 | Gastric cancer | miR-4429 prevents gastric cancer progression by targeting METTL3 to inhibit m6A methylation-induced stabilization of SEC62 | [281] |
miR-186 | METTL3 | HCC | miR-186 targets METTL3 and inhibits value-added invasion of HCC through the Wnt/β-catenin signaling pathway | [282] |
Cisplatin | METTL3 | Seminoma | Enhanced stability of TFAP2C mRNA may promote survival of cisplatin-loaded spermatocytoma cells through upregulation of DNA repair-related genes | [334] |
Oxaliplatin | METTL3 | Colorectal cancer | Depletion of Sec62 sensitizes tumor cells to chemotherapeutic agents by inhibiting Wnt/β-catenin signaling | [335] |
Everolimus | METTL3 | Gastric cancer | Inhibition of AKT/mTOR pathway to enhance drug sensitivity in tumor cells | [336] |
Anti‑PD‑1 | METTL3 | Melanoma | Inhibition of NF-κB and STAT3 via suppressing the ERK pathway, thereby slowing tumor growth | [150] |
STM2457 | METTL3 | Leukemia | STM2457 inhibits growth and differentiation and increases apoptosis of cancer cells by targeting METTL3 | [337] |
Imidazobenzoxazin-5-thione MV1035 | ALKBH5 | Glioblastoma | MV1035 reduces tumor migration and invasion by inhibiting ALKBH5 | [338] |
CS1/CS2 | FTO | Leukemia | Inhibits expression of immune checkpoint genes (in particular, LILRB4) and significantly attenuates leukemic stem cell/initiating cell self-renewal and reprogramming immune responses through targeting FTO | [190] |
Tyrosine kinase inhibitors | FTO | Leukemia | FTO-dependent m6A demethylation enhances mRNA stability of proliferation/survival transcripts containing m6A, leading to increased protein synthesis | [339] |
Triptonide | IGF2BP1 | Nasopharyngeal carcinoma | Inhibits tumor growth by disrupting the lncRNA THOR-IGF2BP1 signaling pathway | [340] |
Berberine | IGF2BP3 | Colorectal cancer | Blocks tumor proliferation by downregulating IGF2BP3, inducing a G0/G1 phase block | [341] |
JQ1 | IGF2BP3 | Ewing sarcoma | Inhibits tumor growth by reducing IGF2BP3 expression | [342] |
BTYNB | IGF2BP1 | Melanoma | Suppresses IGF2BP1 protein expression and retards ovarian cancer growth by impairing interactions between IGF2BP1 and c-MYC or E2F1 mRNA | [273] |
Benzamidobenzoic acid/ureidothiophene | IGF2BP2 | Colorectal/HCC | Delays tumor progression through targeted inhibition of IGF2BP2 | [343] |
Chidamide | METTL3/WTAP | Lung cancer | Downregulates c-MET expression by suppressing its mRNA m6A methylation, leading to a subsequent c-MET-/HGF-dependent increase in crizotinib sensitivity of tumor cells | [344] |