The DOI matches its Crossref record; 15 of the 15 references it cites were found in a registry or an index.
Small-Molecule Targeting of Oncogenic FTO Demethylase in Acute Myeloid Leukemia
Open accessAbstract
Summary FTO, a mRNA N6-methyladenosine (m6A) demethylase, was reported to promote leukemogenesis. Using structure-based rational design, we have developed two promising FTO inhibitors, namely FB23 and FB23-2, which directly bind to FTO and selectively inhibit FTO’s m6A demethylase activity. Mimicking FTO depletion, FB23-2 dramatically suppresses proliferation and promotes the differentiation/apoptosis of human acute myeloid leukemia (AML) cell line cells and primary blast AML cells in vitro. Moreover, FB23-2 significantly inhibits the progression of human AML cell lines and primary cells in xenotransplanted mice. Collectively, our data suggest that FTO is a druggable target and that targeting FTO by small-molecule inhibitors holds potential to treat AML.
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N6-methyladenosine-dependent regulation of messenger RNA stability
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Comprehensive Analysis of mRNA Methylation Reveals Enrichment in 3′ UTRs and near Stop Codons
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N6-Methyladenosine in nuclear RNA is a major substrate of the obesity-associated FTO
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ALKBH5 Is a Mammalian RNA Demethylase that Impacts RNA Metabolism and Mouse Fertility
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Self-citationN6-methyladenosine Modulates Messenger RNA Translation Efficiency
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Recognition of RNA N6-methyladenosine by IGF2BP proteins enhances mRNA stability and translation
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Self-citationNuclear m6A Reader YTHDC1 Regulates mRNA Splicing
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Cited by
The role of m6A modification in the biological functions and diseases
Jiang, X., Liu, B., Nie, Z., Duan, L., Xiong, Q., Jin, Z., Yang, C., & Chen, Y. (2021) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-020-00450-x · Cited by 2,335
Self-citationRole of RNA modifications in cancer
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The role of m6A RNA methylation in cancer metabolism
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Xiong, J., He, J., Zhu, J., Pan, J., Liao, W., Ye, H., Wang, H., Song, Y., Du, Y., Cui, B., et al. (2022) · Molecular Cell · doi:10.1016/j.molcel.2022.02.033 · Cited by 804
m 6 A RNA methylation: from mechanisms to therapeutic potential
He, P. C., & He, C. (2021) · The EMBO Journal · doi:10.15252/embj.2020105977 · Cited by 786
Metadata
- Authors
- Huang, Y., Su, R., Sheng, Y., Dong, L., Dong, Z., Xu, H., Ni, T., Zhang, Z. S., Zhang, T., Li, C., Han, L., Zhu, Z., Lian, F., Wei, J., Deng, Q., Wang, Y., Wunderlich, M., Gao, Z., Pan, G., Zhong, D., Zhou, H., Zhang, N., Gan, J., Jiang, H., Mulloy, J. C., Qian, Z., Chen, J., & Yang, C.-G.
- Venue
- Cancer Cell
- Publisher
- Elsevier BV
- Published
- 2019-04
- Volume
- 35
- Issue
- 4
- Pages
- 677-691.e10
- ISSN
- 1535-6108 (ISSN-L)
- OpenAlex
- W2936790196
- Cited by
- 877
- References
- 15
- FWCI
- 55.60
- Type
- journal article
- Language
- en
- Open access
- bronze
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- Huang, Y., Su, R., Sheng, Y., Dong, L., Dong, Z., Xu, H., Ni, T., Zhang, Z. S., Zhang, T., Li, C., Han, L., Zhu, Z., Lian, F., Wei, J., Deng, Q., Wang, Y., Wunderlich, M., Gao, Z., Pan, G., . . . Yang, C.-G. (2019). Small-Molecule Targeting of Oncogenic FTO Demethylase in Acute Myeloid Leukemia. Cancer Cell. https://doi.org/10.1016/j.ccell.2019.03.006
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
