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Table 3 Tumor-targeted drug therapy based on m6A methylation

From: Crosstalk among m6A RNA methylation, hypoxia and metabolic reprogramming in TME: from immunosuppressive microenvironment to clinical application

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]