From: Targeting RNA N6-methyladenosine to synergize with immune checkpoint therapy
Targeting | Compounds | Role | Functions | References |
---|---|---|---|---|
METTL3-METTL14-WTAP complex | Asp295 | Activator | Promotes mRNA m6A modification | [159] |
METTL3-METTL14-WTAP complex | Phe534 | Activator | Promotes mRNA m6A modification | [159] |
METTL3-METTL14-WTAP complex | Arg536 | Activator | Promotes mRNA m6A modification | [159] |
METTL3-METTL14-WTAP complex | Asn539 | Activator | Promotes mRNA m6A modification | [159] |
METTL3 | molecule 1 | Inhibitor | Reduces the abundance of mRNA targeted by METTL3 and suppresses the proliferation of leukemia cell | [146] |
METTL3 | molecule 2 | Inhibitor | Reduces the abundance of mRNA targeted by METTL3 and suppresses the proliferation of leukemia cell | [146] |
METTL3 | STM2457 | Inhibitor | Shows antitumor capacity against leukemia in vitro and in vivo | [160] |
FTO | R-2HG | Inhibitor | Downregulates the expression of oncogene c-Myc and CEBPA, and increases the expression of antioncogene RARA and ASB2 expression; represses AML cell proliferation/viability | [144] |
FTO | MO-I-50 | Inhibitor | Suppresses the survival or colony forming ability of cancer cells in triple-negative inflammatory breast cancer cell lines | [153] |
FTO | Rhein | Inhibitor | Competitively binds with the FTO catalytic domain and suppresses FTO function | [154] |
FTO | CHTB | Inhibitor | Suppresses FTO function by binding with FTO between an antiparallel sheet and the extended C-terminal of the long loop of FTO | [155] |
FTO | N-CDPCB | Inhibitor | Suppresses FTO function by binding with FTO between an antiparallel b-sheet and the L1 loop of FTO | [156] |
FTO | Meclofenamic acid (MA) | Inhibitor | Specially integrates with the active surface of FTO to inhibit the activity of FTO and increase m6A abundance | |
FTO | FB23 | Inhibitor | Downregulates the expression of oncogene c-Myc and CEBPA, and increases the expression of anti-oncogene RARA and ASB2 expression | [149] |
FTO | FB23-2 | Inhibitor | Downregulates the expression of oncogene c-Myc and CEBPA, and increases the expression of anti-oncogene RARA and ASB2 expression | [149] |
FTO | CS1 | Inhibitor | Directly binds to the enzymatic reaction center of FTO, interfere with its binding with target mRNA; reprograms the immune response, conquers immune escape by suppressing the expression of immune checkpoint gene LILRB4, and sensitizes leukemia cells to cytotoxic T cells | [101] |
FTO | CS2 | Inhibitor | Directly binds to the enzymatic reaction center of FTO, interfere its binding to target mRNA; reprograms the immune response, conquers immune escape by suppressing the expression of immune checkpoint gene LILRB4, and sensitizes leukemia cells to cytotoxic T cells | [101] |
FTO | Entacapone | Inhibitor | Suppresses the function of FTO by directly binding with FTO at its cofactor and substrate binding sites | [150] |
ALKBH5 | ALK-04 | Inhibitor | Functions synergistically with PD-1 inhibitor to inhibit melanoma | [105] |
ALKBH5 | MV1035 | Inhibitor | Shows a favorable antitumor potency in GBM | [157] |
ALKBH5 | 2-[(1-hydroxy-2-oxo-2- phenylethyl)sulfanyl]acetic acid | Inhibitor | Suppresses the proliferation of leukemia | [158] |
ALKBH5 | 4-[(furan-2-yl)methyl]amino-1,2-diazinane-3,6-dione, | Inhibitor | suppresses the proliferation of leukemia | [158] |
IGF2BP1 | BTYNB | Inhibitor | Suppresses the proliferation of melanoma and ovarian cancer cells by downregulating the expression of targeted mRNAs |