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. 2022 Jul 6;15:84. doi: 10.1186/s13045-022-01304-5

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]