Mechanism of RNA modification N6-methyladenosine in human cancer

Table 5 Partial regulators or inhibitors of m6A modifications may provide the potential therapeutic strategies in cancer treatment

Drug	Role	Target	Selective	Biological function	Cancer	Effect/ Mechanism on cancer	Refs
MA /MA2	Inhibitor	FTO	Yes	Stabilize FTO binding for the m6A-containing nucleic acid	GBM	Inhibit GSC growth and self-renewal	[49]
FB23/FB23–2	Inhibitor	FTO	Yes	Directly bind to FTO and inhibit m6A demethylase activity	AML	Suppress proliferation and promote the differentiation/apoptosis	[148]
Rhein	Inhibitor	FTO	No	Binding FTO catalytic domain against ssRNA substrate	AML BC	Prevent or override tyrosine kinase inhibitor resistance Decrease tumor growth	[149] [94]
R-2HG	Inhibitor	FTO	No	Suppress FTO activity and elevate m6A RNA modification	AML	Inhibit proliferation/survival of FTO-high cancer cells	[45]
MO-I-500	Inhibitor	FTO	Yes	Purify FTO demethylase catalyzing demethylation	BC	Inhibit survival of BC cells via decreasing FTO and IRX3 proteins	[150]
SPI1	Regulator	METTL14	No	Negatively regulate METTL14 expression	AML	Inhibit differentiation via targeting MYB and MYC	[42]
CA4	Regulator	WTAP	No	Interact with WTAP and induce WTAP protein degradation	CRC	Inhibits CRC development through WTAP–WT1–TBL1 axis	[73]

GBM glioblastoma; AML acute myeloid leukemia; BC breast cancer; CRC colorectal cancer

ISSN: 1476-4598