Table 2.
Small molecule inhibitor of IGF2BPs
| IGF2BPs | Inhibitors | Cancer types | Target site | Effect | Ref |
|---|---|---|---|---|---|
| IGF2BP1 | BTYNB | Melanoma, Ovarian cancer | Unknown | Disrupting the interaction between | 117, 118 |
| IGF2BP1 and target mRNAs | |||||
| 7773 | Lung cancer | A hydrophobic surface at the | Reducing the level of mRNA targets | 119 | |
| boundary of KH3 and KH4 domain | |||||
| Cucurbitacin B | HCC | The Cys253 site in the KH1-2 domain | A pharmacological allosteric effect to inhibit | 73 | |
| recognition of target mRNAs | |||||
| C646 | Intrahepatic | H3K27ac in the promoter of IGF2BP1 | Decreasing the IGF2BP1 mRNA and protein | 45 | |
| cholangiocarcinoma | expression | ||||
| IGF2BP2 | Ten compounds, | CRC, Liver cancer | RRM1 and KH3-4 (Compounds | Reducing tumor cell proliferation | 120 |
| belonging to the | from benzamidobenzoic acid class), | ||||
| benzamidobenzoic acid class | Unknown (Compounds from | ||||
| and ureidothiophene class | ureidothiophene class) | ||||
| JX5 | Leukemia | KH3-4 domain | Suppressing the cancer progression without | 121 | |
| influencing the IGF2BP2 mRNA levels | |||||
| CWI1-2 | Leukemia | The hydrophobic pocket within | Decreasing downstream RNA and protein levels of | 122 | |
| the KH4 domain | IGF2BP2 to exert anti-tumor efficacy | ||||
| IGF2BP3 | JQ1 and I-BET151 | Leukemia, | Unknown | Decreasing levels of IGF2BP3 and its mRNA | 27, 123 |
| Ewing Sarcoma | targets to hinder tumor growth | ||||
| Berberine | CRC | Unknown | Down-regulating IGF2BP3 at the protein level to | 105, 124 | |
| inhibit CRC growth | |||||
| Isoliquiritigenin | Non-small cell lung cancer | Unknown | Reducing IGF2BP3 at the mRNA and protein level | 125 | |
| to inhibit lung cancer progression | |||||
| RIG | Lung adenocarcinoma | Unknown | Reducing IGF2BP3 expression and tumor growth | 57 |