DNA methyltransferase inhibitors are widely used in preclinical and clinical studies, but poor pharmacokinetics and low efficacy in solid tumors limit their therapeutic use. A new study reports the development and characterization of a specific, non-covalent DNA methyltransferase inhibitor with more-durable DNA hypomethylation and lower toxicity than that of nucleoside analogs.
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References
Jones, P. A. & Liang, G. Nat. Rev. Genet. 10, 805–811 (2009).
Roulois, D. et al. Cell 162, 961–973 (2015).
Chiappinelli, K. B. et al. Cell 162, 974–986 (2015).
Pappalardi, M. B. et al. Nat. Cancer https://doi.org/10.1038/s43018-021-00249-x (2021).
Egger, G., Liang, G., Aparicio, A. & Jones, P. A. Nature 429, 457–463 (2004).
Mehdipour, P., Murphy, T. & De Carvalho, D. D. Pharmacol. Ther. 205, 107416 (2020).
Mehdipour, P. et al. Nature 588, 169–173 (2020).
Loo Yau, H. et al. Mol. Cell 81, 1469–1483.e8 (2021).
Fresquet, V. et al. Cancer Discov. 11, 1268–1285 (2021).
Derissen, E. J. B., Beijnen, J. H. & Schellens, J. H. M. Oncologist 18, 619–624 (2013).
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D.D.D.C. received research funds from Pfizer and Nektar Therapeutics, and is co-founder and chief scientific officer at Adela.
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Mehdipour, P., Chen, R. & De Carvalho, D.D. The next generation of DNMT inhibitors. Nat Cancer 2, 1000–1001 (2021). https://doi.org/10.1038/s43018-021-00271-z
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DOI: https://doi.org/10.1038/s43018-021-00271-z
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