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Table 2 small-molecule inhibitors of m6A regulators

From: Physio-pathological effects of N6-methyladenosine and its therapeutic implications in leukemia

Targeting Compounds Functions Reference
METTL3
inhibitor
Compound 1 and 2 Suppress m6A modification, exerts anti-tumor effects in AML models [148]
  STM2457 Suppress m6A modification, reduce AML growth and increase differentiation and apoptosis [128]
  UZH2 Suppress m6A modification in vitro [129]
  UZH1a Suppress m6A modification in vitro [127]
FTO
inhibitor
Rhein Competitively binds the FTO catalytic domain and disrupts FTO from binding m6A-modified RNAs. [133]
  Meclofenamic acid (MA) Competes with FTO binding for the m6A-containing RNA, increase m6A levels [134]
  MA2 Binds FTO active surface, induces m6A methylation, inhibits glioblastoma progression in mice [135]
  FB23-2 Reduces expression of c-Myc and CEBPA and promotes RARA and ASB2, represses leukemia cell proliferation, survival, and leukemia progression in mice [136]
  R-2HG Induces degradation of c-Myc and CEBPA, promotes leukemia cell apoptosis, and inhibits leukemia growth in mice. [108]
  CS1 and CS2 Attenuate LSC self-renewal, reprogram immune response by reducing LILRB4, sensitize leukemia cells to T-cell cytotoxicity, and show potent anti-leukemic efficacy in mouse models [136]
  acrylonitrile derivative 1a Binding FTO with chlorine atom, inhibits proliferation of leukemia cells [137]
  Saikosaponin D Inhibites AML cells proliferation, induce apoptosis and cell cycle arrest both in vitro and vivo, particularly in TKIs-resistant cells [138]
  let-7b-5p mimic Downregulate the expression of FTO and upregulate c-MYC level in AML line cells [139]
ALKBH5
inhibitor
Compound 1 and 2
Bioactive peptide
Reduces leukemia cell viability
inhibit AML cell proliferation and promote apoptosis in vitro, and reduce tumor growth in vivo
[143, 144]