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Table 3 Inhibitors of m6A regulators in cancer treatment

From: Targeting RNA N6-methyladenosine modification: a precise weapon in overcoming tumor immune escape

Drugs

Regulator

Cancer

Function

Structure

Refs.

Rhein

FTO

BC

Suppresses tumor growth of BC in vivo.

[183, 184]

Augments antiproliferative effects of atezolizumab based on BC regression.

[185]

MA2

FTO

glioblastoma

Inhibits GSCs growth and self-renewal in vitro, and tumor growth in vivo.

[137, 186]

Enhances the effect of the chemotherapy drug

temozolomide on suppressing proliferation of glioma cells.

[187]

MO-I-500

FTO

BC

Inhibits the survival and/or colony formation of a triple-negative inflammatory BC cell line.

[188,189,190]

FB23-2

FTO

AML

Suppresses proliferation and promotes the differentiation/apoptosis of AML cells and in vitro, and inhibits tumor growth in vivo.

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[191]

R-2HG

FTO

AML

Inhibits cell growth, promotes cell cycle arrest and apoptosis of leukemia cells.

[192]

CS1

FTO

AML, BC, PC, and glioblastoma

Suppresses CSC maintenance and immune evasion of AML.

[39]

CS2

BTYNB

IGF2BP1

LC, OC

Inhibits proliferation and anchorage-independent growth of IGF2BP1-positive cancer cells. Blocks tumor cells’ growth and spread in xenograft tumors. Synergizes with palbociclib at low concentrations of both compounds.

[193, 194]

STM2457

METTL3

AML

Inhibits AML cells growth and promotes differentiation and apoptosis in vitro, and disrupts engraftment and prolonged survival in vivo.

[195]

  1. Abbreviations: AML acute myeloid leukemia, BC breast cancer, CSC cancer stem cell, GSC glioblastoma stem cell, LC lung cancer, MA meclofenamic acid, OC ovarian cancer, PC pancreatic cancer, R-2HG R-2-hydroxyglutarate