Please use this identifier to cite or link to this item: https://hdl.handle.net/10356/79355
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dc.contributor.authorToh, Joel D. W.en
dc.contributor.authorSun, Lingyien
dc.contributor.authorLau, Lisa Z. M.en
dc.contributor.authorTan, Jackieen
dc.contributor.authorLow, Joanne J. A.en
dc.contributor.authorTang, Colin W. Q.en
dc.contributor.authorCheong, Eleanor J. Y.en
dc.contributor.authorTan, Melissa J. H.en
dc.contributor.authorChen, Yunen
dc.contributor.authorHong, Wanjinen
dc.contributor.authorGao, Yong-Guien
dc.contributor.authorWoon, Esther C. Y.en
dc.date.accessioned2015-02-26T06:39:08Zen
dc.date.accessioned2019-12-06T13:23:17Z-
dc.date.available2015-02-26T06:39:08Zen
dc.date.available2019-12-06T13:23:17Z-
dc.date.copyright2015en
dc.date.issued2015en
dc.identifier.citationToh, J. D. W., Sun, L., Lau, L. Z. M., Tan, J., Low, J. J. A., Tang, C. W. Q., et al. (2015). A strategy based on nucleotide specificity leads to a subfamily-selective and cell-active inhibitor of N6-methyladenosine demethylase FTO. Chemical science, 6, 112-122.en
dc.identifier.urihttps://hdl.handle.net/10356/79355-
dc.description.abstractThe AlkB family of nucleic acid demethylases are of intense biological and medical interest because of their roles in nucleic acid repair and epigenetic modification. However their functional and molecular mechanisms are unclear, hence, there is strong interest in developing selective inhibitors for them. Here we report the identification of key residues within the nucleotide-binding sites of the AlkB subfamilies that likely determine their substrate specificity. We further provide proof of principle that a strategy exploiting these inherent structural differences can enable selective and potent inhibition of the AlkB subfamilies. This is demonstrated by the first report of a subfamily-selective and cell-active FTO inhibitor 12. The distinct selectivity of 12 for FTO against other AlkB subfamilies and 2OG oxygenases shall be of considerable interest with regards to its potential use as a functional probe. The strategy outlined here is likely applicable to other AlkB subfamilies, and, more widely, to other 2OG oxygenases.en
dc.format.extent12 p.en
dc.language.isoenen
dc.relation.ispartofseriesChemical scienceen
dc.rights© 2015 Royal Society of Chemistry. This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.en
dc.subjectDRNTU::Science::Biological sciencesen
dc.titleA strategy based on nucleotide specificity leads to a subfamily-selective and cell-active inhibitor of N6-methyladenosine demethylase FTOen
dc.typeJournal Articleen
dc.contributor.schoolSchool of Biological Sciencesen
dc.identifier.doi10.1039/C4SC02554Gen
dc.description.versionPublished versionen
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item.grantfulltextopen-
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