IDH Mutation, Competitive Inhibition of FTO, and RNA Methylation

FTO Plays an Oncogenic Role in Acute Myeloid Leukemia as a N 6 -Methyladenosine RNA Demethylase

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Oncogenic Isocitrate Dehydrogenase Mutations: Mechanisms, Models, and Clinical Opportunities

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The AlkB family of Fe(II)/α-ketoglutarate-dependent dioxygenases: repairing nucleic acid alkylation damage and beyond

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D2HGDH regulates alpha-ketoglutarate levels and dioxygenase function by modulating IDH2

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Mutant <i>IDH</i> : A Targetable Driver of Leukemic Phenotypes Linking Metabolism, Epigenetics and Transcriptional Regulation

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Role of RNA modifications in cancer

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R-2HG Exhibits Anti-tumor Activity by Targeting FTO/m6A/MYC/CEBPA Signaling

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The roles of DNA, RNA and histone methylation in ageing and cancer

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N6-methyladenosine links RNA metabolism to cancer progression

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Metabolism, Activity, and Targeting of D- and L-2-Hydroxyglutarates

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The m6A demethylase FTO promotes the growth of lung cancer cells by regulating the m6A level of USP7 mRNA

Li, J., Han, Y., Zhang, H., Qian, Z., Jia, W., Gao, Y., Zheng, H., & Li, B. (2019) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2019.03.093 · Cited by 231 · see citing works

The cancer driver genes IDH1/2, JARID1C/ KDM5C, and UTX/ KDM6A: crosstalk between histone demethylation and hypoxic reprogramming in cancer metabolism

Chang, S., Yim, S., & Park, H. (2019) · Experimental &amp; Molecular Medicine · doi:10.1038/s12276-019-0230-6 · Cited by 228 · see citing works

Roles of RNA methylation by means of N6-methyladenosine (m6A) in human cancers

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Crosstalk between metabolic reprogramming and epigenetics in cancer: updates on mechanisms and therapeutic opportunities

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Discovery of RNA-binding proteins and characterization of their dynamic responses by enhanced RNA interactome capture

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RNA modification: mechanisms and therapeutic targets

Qiu, L., Qian, J., Li, Y., & Han, J. (2023) · Molecular Biomedicine · doi:10.1186/s43556-023-00139-x · Cited by 180 · see citing works

The Biology of m6A RNA Methylation in Normal and Malignant Hematopoiesis

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Oncogenic Activities of IDH1/2 Mutations: From Epigenetics to Cellular Signaling

Gagné, L. M., Boulay, K., Topisirović, I., Huot, M., & Mallette, F. A. (2017) · Trends in Cell Biology · doi:10.1016/j.tcb.2017.06.002 · Cited by 141 · see citing works

Methylation across the central dogma in health and diseases: new therapeutic strategies

Liu, R., Zhao, E., Yu, H., Yuan, C., Abbas, M. N., & Cui, H. (2023) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-023-01528-y · Cited by 147 · see citing works

Aberrant expression of enzymes regulating m6A mRNA methylation: implication in cancer

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Mitochondrial metabolism supports resistance to IDH mutant inhibitors in acute myeloid leukemia

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Downregulation of Fat Mass and Obesity Associated (FTO) Promotes the Progression of Intrahepatic Cholangiocarcinoma

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Epitranscriptomic influences on development and disease

Hsu, P. J., Shi, H., & He, C. (2017) · Genome biology · doi:10.1186/s13059-017-1336-6 · Cited by 113 · see citing works

The GDF11-FTO-PPARγ axis controls the shift of osteoporotic MSC fate to adipocyte and inhibits bone formation during osteoporosis

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RNA methylation and diseases: experimental results, databases, Web servers and computational models

Chen, X., Sun, Y., Liu, H., Zhang, L., Li, J., & Meng, J. (2017) · Briefings in Bioinformatics · doi:10.1093/bib/bbx142 · Cited by 90 · see citing works

The Emerging Role of Epitranscriptomics in Cancer: Focus on Urological Tumors

Lobo, J., Barros‐Silva, D., Henrique, R., & Jerónimo, C. (2018) · Genes · doi:10.3390/genes9110552 · Cited by 84 · see citing works

Phloroglucinol Treatment Induces Transgenerational Epigenetic Inherited Resistance Against Vibrio Infections and Thermal Stress in a Brine Shrimp (Artemia franciscana) Model

Roy, S., Kumar, V., Bossier, P., Norouzitallab, P., & Vanrompay, D. C. G. (2019) · Frontiers in Immunology · doi:10.3389/fimmu.2019.02745 · Cited by 71 · see citing works

Androgen receptor reverses the oncometabolite R-2-hydroxyglutarate-induced prostate cancer cell invasion via suppressing the circRNA-51217/miRNA-646/TGFβ1/p-Smad2/3 signaling

Xu, H., Sun, Y., You, B., Huang, C., Ye, D., & Chang, C. (2019) · Cancer Letters · doi:10.1016/j.canlet.2019.12.014 · Cited by 72 · see citing works

Stable Isotope Labeling Highlights Enhanced Fatty Acid and Lipid Metabolism in Human Acute Myeloid Leukemia

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Isocitrate dehydrogenase variants in cancer — Cellular consequences and therapeutic opportunities

Liu, S., Cadoux-Hudson, T. A. D., & Schofield, C. J. (2020) · Current Opinion in Chemical Biology · doi:10.1016/j.cbpa.2020.06.012 · Cited by 70 · see citing works

Regulatory role and mechanism of m6A RNA modification in human metabolic diseases

Zhang, Y., Chen, W., Zheng, X., Guo, Y., Cao, J., Zhang, Y., Wen, S., Gao, W., & Wu, Y. (2021) · Molecular Therapy — Oncolytics · doi:10.1016/j.omto.2021.05.003 · Cited by 57 · see citing works

Metabolic Control of m6A RNA Modification

Kim, J., & Lee, G. (2021) · Metabolites · doi:10.3390/metabo11020080 · Cited by 57 · see citing works

The roles of N6-methyladenosine methylation in the regulation of bone development, bone remodeling and osteoporosis

Li, Y., Li, M., & Zhao, B. (2022) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2022.108174 · Cited by 55 · see citing works

N 6 ‐methyladenosine (m 6 A) RNA modification in human cancer

Huo, F., Zhu, Z., & Pei, D. (2020) · Cell Proliferation · doi:10.1111/cpr.12921 · Cited by 51 · see citing works

Regulation of Gene Expression Associated With the N6-Methyladenosine (m6A) Enzyme System and Its Significance in Cancer

Tian, S., Lai, J., Yu, T., Li, Q., & Chen, Q. (2021) · Frontiers in Oncology · doi:10.3389/fonc.2020.623634 · Cited by 48 · see citing works

Towards a druggable epitranscriptome: Compounds that target RNA modifications in cancer

Berdasco, M., & Esteller, M. (2021) · British Journal of Pharmacology · doi:10.1111/bph.15604 · Cited by 43 · see citing works

Impact of DNA and RNA Methylation on Radiobiology and Cancer Progression

Chi, H., Tsai, C., Tsai, M.-M., & Lin, K. (2018) · International Journal of Molecular Sciences · doi:10.3390/ijms19020555 · Cited by 39 · see citing works

Insight into novel RNA-binding activities via large-scale analysis of lncRNA-bound proteome and IDH1-bound transcriptome

Liu, L., Li, T., Song, G., He, Q., Yin, Y., Lu, J. Y., Bi, X., Wang, K., Luo, S., Chen, Y., et al. (2019) · Nucleic Acids Research · doi:10.1093/nar/gkz032 · Cited by 34 · see citing works

Epitranscriptomics in Hematopoiesis and Hematologic Malignancies

Rosselló-Tortella, M., Ferrer, G., & Esteller, M. (2020) · Blood Cancer Discovery · doi:10.1158/2643-3249.bcd-20-0032 · Cited by 34 · see citing works

Regulation of PD-L1 expression is a novel facet of cyclic-AMP-mediated immunosuppression

Sasi, B. K., Ethiraj, P., Myers, J., Lin, A., Jiang, S., Qiu, Z., Holder, K. N., & Aguiar, R. C. T. (2020) · Leukemia · doi:10.1038/s41375-020-01105-0 · Cited by 32 · see citing works

m6A RNA Methylation in Systemic Autoimmune Diseases—A New Target for Epigenetic-Based Therapy?

Wardowska, A. (2021) · Pharmaceuticals · doi:10.3390/ph14030218 · Cited by 32 · see citing works

Methylation of RNA N6-methyladenosine in modulation of cytokine responses and tumorigenesis

Chang, G., Leu, J.-S., Ma, L., Xie, K., & Huang, S. (2018) · Cytokine · doi:10.1016/j.cyto.2018.06.018 · Cited by 29 · see citing works

MYC Regulation of D2HGDH and L2HGDH Influences the Epigenome and Epitranscriptome

Qiu, Z., Lin, A., Jiang, S., Elkashef, S. M., Myers, J., Srikantan, S., Sasi, B. K., Cao, J. Z., Godley, L. A., Rakheja, D., et al. (2020) · Cell chemical biology · doi:10.1016/j.chembiol.2020.02.002 · Cited by 30 · see citing works

Induction of transgenerational innate immune memory against Vibrio infections in a brine shrimp (Artemia franciscana) model

Roy, S., Baruah, K., Bossier, P., Vanrompay, D. C. G., & Norouzitallab, P. (2022) · Aquaculture · doi:10.1016/j.aquaculture.2022.738309 · Cited by 29 · see citing works

Advances in the role of m6A RNA modification in cancer metabolic reprogramming

Han, X., Wang, L., & Han, Q. (2020) · Cell & Bioscience · doi:10.1186/s13578-020-00479-z · Cited by 28 · see citing works

Metabolic Regulation of the Epitranscriptome

Thomas, J. M., Batista, P. J., & Meier, J. L. (2019) · ACS Chemical Biology · doi:10.1021/acschembio.8b00951 · Cited by 29 · see citing works

Epigenetic regulation of hematopoietic stem cell homeostasis

Jiang, P., Wang, H., Zheng, J., Han, Y., Huang, H., & Qian, P. (2019) · Blood Science · doi:10.1097/bs9.0000000000000018 · Cited by 27 · see citing works

MYC, mitochondrial metabolism and O-GlcNAcylation converge to modulate the activity and subcellular localization of DNA and RNA demethylases

Lin, A.-P., Qiu, Z., Ethiraj, P., Sasi, B., Jaafar, C., Rakheja, D., & Aguiar, R. C. T. (2022) · Leukemia · doi:10.1038/s41375-021-01489-7 · Cited by 25 · see citing works

Synergistic Targeting of the Regulatory and Catalytic Subunits of PI3Kδ in Mature B-cell Malignancies

Cooney, J. D., Lin, A., Jiang, D., Wang, L., Suhasini, A. N., Myers, J., Qiu, Z., Wölfler, A., Sill, H., & Aguiar, R. C. T. (2017) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-17-2218 · Cited by 25 · see citing works

Dynamic multilayered control of m 6 A RNA demethylase activity

Jaafar, C., & Aguiar, R. C. T. (2024) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.2317847121 · Cited by 21 · see citing works

Discovery of Novel RNA Demethylase FTO Inhibitors Featuring an Acylhydrazone Scaffold with Potent Antileukemia Activity

Liang, X., Huang, Y., Ren, H., Liu, Q., Chen, L., Zhao, J., Gao, X., Lu, J., Yang, C., & Liu, H. S. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.4c02076 · Cited by 20 · see citing works

Insights into the role of RNA m6A modification in the metabolic process and related diseases

Hu, H., Li, Z., Xie, X., Liao, Q., Hu, Y., Gong, C., Gao, N., Yang, H., Xiao, Y., & Chen, Y. (2023) · Genes & Diseases · doi:10.1016/j.gendis.2023.04.038 · Cited by 17 · see citing works

Abnormal changes in metabolites caused by m6A methylation modification: The leading factors that induce the formation of immunosuppressive tumor microenvironment and their promising potential for clinical application

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Deciphering the multifaceted roles and clinical implications of 2-hydroxyglutarate in cancer

Hao, J., Huang, Z., Zhang, S., Song, K., Wang, J., Gao, C., Fang, Z., & Zhang, N. (2024) · Pharmacological Research · doi:10.1016/j.phrs.2024.107437 · Cited by 15 · see citing works

Metabolic enzymes function as epigenetic modulators: A Trojan Horse for chromatin regulation and gene expression

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Multivariate Analysis of RNA Chemistry Marks Uncovers Epitranscriptomics-Based Biomarker Signature for Adult Diffuse Glioma Diagnostics

Relier, S., Amalric, A., Attina, A., Koumare, I. B., Rigau, V., Burel‐Vandenbos, F., Fontaine, D., Baroncini, M., Hugnot, J., Duffau, H., et al. (2022) · Analytical Chemistry · doi:10.1021/acs.analchem.2c01526 · Cited by 16 · see citing works

Cancer epitranscriptomics in a nutshell

Primac, I., Penning, A., & Fuks, F. (2022) · Current Opinion in Genetics & Development · doi:10.1016/j.gde.2022.101924 · Cited by 14 · see citing works

The Role of RNA m6A Modification in Cancer Glycolytic Reprogramming

Zhou, Y., Huang, T., Jiang, J., Li, Y., Huang, H., & Wu, S. (2022) · Current Gene Therapy · doi:10.2174/1566523222666220830150446 · Cited by 14 · see citing works

RNA modifications in hematological malignancies

Jin, Z., MacPherson, K., Liu, Z., & Vu, L. (2023) · International Journal of Hematology · doi:10.1007/s12185-023-03576-0 · Cited by 14 · see citing works

RNA Regulators in Leukemia and LymphomaPreprint

Prieto, C., & Kharas, M. G. (2019) · Cold Spring Harbor Perspectives in Medicine · doi:10.1101/cshperspect.a034967 · Cited by 13 · see citing works

The Regulation of m6A Modification in Glioblastoma: Functional Mechanisms and Therapeutic Approaches

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The curious case of IDH mutant acute myeloid leukaemia: biochemistry and therapeutic approaches

Gruber, E., & Kats, L. M. (2023) · Biochemical Society Transactions · doi:10.1042/bst20230017 · Cited by 11 · see citing works

m6A regulator-based methylation modification patterns and characterization of tumor microenvironment in acute myeloid leukemia

Xu, Z., Wen, X.-M., Zhang, Y.-C., Jin, Y., Ma, J., Gu, Y., Chen, X., Xia, P., Qian, W., Lin, J., et al. (2022) · Frontiers in Genetics · doi:10.3389/fgene.2022.948079 · Cited by 8 · see citing works

High expression of an intragenic long noncoding RNA misinterpreted as high FTO oncogene expression in NPM1 mutant acute myeloid leukemia

Arza-Apalategi, S., Heuts, B. M. H., Dooijes, M. T. M., Gilissen, D., van der Heijden, A., Jansen, J. H., Martens, J. H. A., & van der Reijden, B. A. (2023) · Leukemia · doi:10.1038/s41375-023-01844-w · Cited by 8 · see citing works

Oncogenic Mechanisms and Therapeutic Targeting of Metabolism in Leukemia and LymphomaPreprint

Stahl, M. F., Epstein-Peterson, Z. D., & Intlekofer, A. M. (2020) · Cold Spring Harbor Perspectives in Medicine · doi:10.1101/cshperspect.a035477 · Cited by 8 · see citing works

Intracellular Mis-Localization of Modified RNA Molecules and Non-Coding RNAs: Facts from Hematologic Malignancies

Symeonidis, A. S., Chroni, A., Dereki, I., Chartoumpekis, D. V., & Sgourou, A. (2025) · Current Issues in Molecular Biology · doi:10.3390/cimb47090758 · Cited by 5 · see citing works

Generation and characterization of the Eµ-Irf8 mouse model

Qiu, Z., Holder, K. N., Lin, A.-P., Myers, J., Jiang, S., Gorena, K. M., Kinney, M. C., & Aguiar, R. C. T. (2020) · Cancer Genetics · doi:10.1016/j.cancergen.2020.05.002 · Cited by 5 · see citing works

IDH1-dependent m6A methylation defines transcriptomic heterogeneity in gliomaPreprint

Batool, S. M., Lee, H., Muralidharan, K., Khan, S. M., Escobedo, A. K., Gashi, D., Faber, K., Ekanayake, E., Hsia, T., Al-Inaya, Y., et al. (2024) · medRxiv · doi:10.1101/2024.09.24.24314089 · Cited by 5 · see citing works

Enasidenib for the treatment of relapsed or refractory acute myeloid leukemia with an isocitrate dehydrogenase 2 mutation

Heiblig, M., Khalife‐Hachem, S., Willekens, C., Micol, J., Paci, A., Penard‐Lacronique, V., & de Botton, S. (2020) · Expert Review of Precision Medicine and Drug Development · doi:10.1080/23808993.2020.1831909 · Cited by 4 · see citing works

Evolution of Epigenome as the Blueprint for Carcinogenesis

Farooq, Z., Shah, A. T., Tauseef, M., Rather, R. A., & Anwar, M. (2021) · Biochemistry · doi:10.5772/intechopen.97379 · Cited by 4 · see citing works

Epigenetic and epitranscriptomic regulation of cardiac metabolism in aging and disease

Liu, J., Yang, M., & Zhou, B. (2025) · The Journal of Cardiovascular Aging · doi:10.20517/jca.2025.06 · Cited by 3 · see citing works

FTO Regulates Apoptosis in CPB2-Treated IPEC-J2 Cells by Targeting Caspase 3 Apoptotic Protein

Yang, J., Zhang, J., Gao, X., Luo, R., Xie, K., Wang, W., Li, J., Yang, Q., Huang, X., Yan, Z., et al. (2022) · Animals · doi:10.3390/ani12131644 · Cited by 4 · see citing works

Modulation of DNA/RNA Methylation Signaling Mediating Metabolic Homeostasis in Cancer

Choubey, P., Kaur, H., & Bansal, K. (2022) · Sub-cellular biochemistry/Subcellular biochemistry · doi:10.1007/978-3-031-07634-3_7 · Cited by 3 · see citing works

FTO in Lung Cancer: Its Progression and Therapeutic Potential

Chen, X., & Chen, G. (2024) · Combinatorial Chemistry & High Throughput Screening · doi:10.2174/0113862073281598240227072839 · Cited by 3 · see citing works

Ivosidenib for the treatment of relapsed or refractory acute myeloid leukemia with an IDH1 mutation

Pasquier, F., Chahine, C., Marzac, C., & de Botton, S. (2020) · Expert Review of Precision Medicine and Drug Development · doi:10.1080/23808993.2020.1792286 · Cited by 3 · see citing works

Metabolic regulation in urological tumors: Interplay with epigenetics and epitranscriptomics

Miranda‐Gonçalves, V., Guimarães‐Teixeira, C., Henrique, R., & Jerónimo, C. (2021) · Elsevier eBooks · doi:10.1016/b978-0-323-85652-2.00019-1 · Cited by 2 · see citing works

α-Ketoglutarate promotes amino acid depletion and suppresses B-cell lymphoma growth and development

Jaafar, C., Ethiraj, P., Qiu, Z., Lin, A., Ferrari, P. S. S. M., & Aguiar, R. C. T. (2025) · Blood · doi:10.1182/blood.2024028069 · Cited by 2 · see citing works

Emerging Roles of Epigenetic Regulators in Maintaining Hematopoietic Stem Cell Homeostasis

Wang, H., Han, Y., & Qian, P. (2023) · Advances in experimental medicine and biology · doi:10.1007/978-981-99-7471-9_3 · Cited by 2 · see citing works

Resolving challenges in detection and quantification of D-2-hydroxyglutarate and L-2-hydroxyglutarate via LC/MS

Dowdy, T., & Larion, M. (2026) · Methods · doi:10.1016/j.ymeth.2026.08.005 · Cited by 1 · see citing works

Biochemical and Genetic Markers in Neurological Trauma and Tumors: Review Article

Ashraf, O., Saleem, T. H., Elsadek, B., Hamdan, A. R. K., & Hassan, M. H. (2022) · Asian Journal of Biochemistry Genetics and Molecular Biology · doi:10.9734/ajbgmb/2022/v11i230260

Étude multi-omics des mutations des isocitrates déshydrogénases dans les leucémies aiguës myéloïdes

Hucteau, A. (2023) · theses.fr (ABES) · doi:10.70675/2ddbfecfzaa70z4d57z87cbzbcc9f3c01cc6

An intelligent DNAzyme theranostic probe for in situ FTO bioimaging and real-time therapeutic efficacy evaluation in living cells

Liu, H., Yu, S., Feng, R., Chen, J., Xie, G., Wu, X., Zhang, T., He, J., Wu, Y., & Tang, K. (2026) · The Analyst · doi:10.1039/d6an00400h

BindingDB Entry 50023655: Discovery of Novel RNA Demethylase FTO Inhibitors Featuring an Acylhydrazone Scaffold with Potent Antileukemia Activity.

BindingDB (2026) · UC San Diego · doi:10.7270/q2mp5860

D-2-HG Inhibits IDH1mut Glioma Growth via FTO Inhibition and Resultant m6A Hypermethylation

Pianka, S. T., Li, T., Prins, T. J., Eldred, B. S. C., Kevan, B. M., Liang, H., Rinonos, S. Z., Kornblum, H. I., Nathanson, D. A., Pellegrini, M. A., et al. (2024) · Cancer Research Communications · doi:10.1158/2767-9764.crc-23-0271 · Cited by 24 · see citing works

Effective Novel Fto Inhibitors Show Potent Anti-Cancer Efficacy and Suppress Drug Resistance

Su, R. J., Dong, L., Li, Y., Han, L., Gao, M., Wunderlich, M., Deng, X., Li, H., Gao, L., Li, C., et al. (2019) · Blood · doi:10.1182/blood-2019-124535 · Cited by 13 · see citing works

Fto Plays an Oncogenic Role in Acute Myeloid Leukemia As a N6-Methyladenosine RNA Demethylase

Su, R. J., Li, Z., Weng, H., Weng, X., Zuo, Z., Li, C., Huang, H., Hu, C., Qin, X., Tang, L., et al. (2016) · Blood · doi:10.1182/blood.v128.22.2706.2706 · Cited by 20 · see citing works

RNA Modification in Cancer

Chen, J. (2020) · The FASEB Journal · doi:10.1096/fasebj.2020.34.s1.00188

High expression of an intragenic long noncoding RNA misinterpreted as high FTO oncogene expression in NPM1 mutant acute myeloid leukemia

Arza-Apalategi, S., Heuts, B. M. H., Dooijes, M. T. M., Gilissen, D., van der Heijden, A., Jansen, J. H., Martens, J. H. A., & van der Reijden, B. A. (2023) · Leukemia · doi:10.1038/s41375-023-01844-w · Cited by 8 · see citing works