A strategy based on nucleotide specificity leads to a subfamily-selective and cell-active inhibitor of N 6-methyladenosine demethylase FTO† †Electronic supplementary information (ESI) available: Experimental details, including full synthesis procedure, T m shift analyses, biochemical and cell-based
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Jackie Tan | Wanjin Hong | Eleanor Jing Yi Cheong | W. Hong | Joel D. W. Toh | J. Tan | Lingyi Sun | E. Woon | E. J. Y. Cheong | Joanne J. A. Low | Yong-Gui Gao | L.Z.M. Lau | Colin W. Q. Tang | Melissa J. H. Tan | Yun Chen | Joel D.W. Toh | Lingyi Sun | Lisa Z. M. Lau | Melissa Tan | Yun Chen | Yong-Gui Gao | Esther C. Y. Woon
[1] R. Klose,et al. Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases. , 2012, Journal of medicinal chemistry.
[2] Yi Zhang,et al. Active DNA demethylation: many roads lead to Rome , 2010, Nature Reviews Molecular Cell Biology.
[3] Arne Klungland,et al. ALKBH5 is a mammalian RNA demethylase that impacts RNA metabolism and mouse fertility. , 2013, Molecular cell.
[4] Yun-Gui Yang,et al. FTO and Obesity: Mechanisms of Association , 2014, Current Diabetes Reports.
[5] Michael A McDonough,et al. Structural basis for inhibition of the fat mass and obesity associated protein (FTO). , 2013, Journal of medicinal chemistry.
[6] Chengqi Yi,et al. Crystal structures of DNA/RNA repair enzymes AlkB and ABH2 bound to dsDNA , 2008, Nature.
[7] Qiang Wang,et al. Crystal structure of the FTO protein reveals basis for its substrate specificity , 2010, Nature.
[8] Chris P. Ponting,et al. The Obesity-Associated FTO Gene Encodes a 2-Oxoglutarate-Dependent Nucleic Acid Demethylase , 2007, Science.
[9] Yi Zhang,et al. TET enzymes, TDG and the dynamics of DNA demethylation , 2013, Nature.
[10] Christopher J. Schofield,et al. Oxygen sensing by HIF hydroxylases , 2004, Nature Reviews Molecular Cell Biology.
[11] Miao Yu,et al. A METTL3-METTL14 complex mediates mammalian nuclear RNA N6-adenosine methylation , 2013, Nature chemical biology.
[12] Yi Zhang,et al. JmjC-domain-containing proteins and histone demethylation , 2006, Nature Reviews Genetics.
[13] J. Essigmann,et al. Mutagenesis, genotoxicity, and repair of 1-methyladenine, 3-alkylcytosines, 1-methylguanine, and 3-methylthymine in alkB Escherichia coli. , 2004, Proceedings of the National Academy of Sciences of the United States of America.
[14] K. Tsujikawa,et al. Design and synthesis of prostate cancer antigen-1 (PCA-1/ALKBH3) inhibitors as anti-prostate cancer drugs. , 2014, Bioorganic & medicinal chemistry letters.
[15] J. Hunt,et al. Enzymological and structural studies of the mechanism of promiscuous substrate recognition by the oxidative DNA repair enzyme AlkB , 2009, Proceedings of the National Academy of Sciences.
[16] Michael A McDonough,et al. Dynamic combinatorial mass spectrometry leads to inhibitors of a 2-oxoglutarate-dependent nucleic acid demethylase. , 2012, Journal of medicinal chemistry.
[17] Chengqi Yi,et al. N6-Methyladenosine in Nuclear RNA is a Major Substrate of the Obesity-Associated FTO , 2011, Nature chemical biology.
[18] Samir Adhikari,et al. Mammalian WTAP is a regulatory subunit of the RNA N6-methyladenosine methyltransferase , 2014, Cell Research.
[19] Chengqi Yi,et al. Switching demethylation activities between AlkB family RNA/DNA demethylases through exchange of active-site residues. , 2014, Angewandte Chemie.
[20] T. Hollis,et al. Structural and Mutational Analysis of Escherichia coli AlkB Provides Insight into Substrate Specificity and DNA Damage Searching , 2010, PloS one.
[21] F. Niesen,et al. The use of differential scanning fluorimetry to detect ligand interactions that promote protein stability , 2007, Nature Protocols.
[22] Robert P. Hausinger,et al. Oxidative demethylation by Escherichia coli AlkB directly reverts DNA base damage , 2002, Nature.
[23] Yang Liu,et al. Crystal Structures of the Human RNA Demethylase Alkbh5 Reveal Basis for Substrate Recognition* , 2014, The Journal of Biological Chemistry.
[24] Cheng Luo,et al. Development of cell-active N6-methyladenosine RNA demethylase FTO inhibitor. , 2012, Journal of the American Chemical Society.
[25] Hiroshi Yamamoto,et al. Expression and sub-cellular localization of human ABH family molecules , 2007, Journal of cellular and molecular medicine.
[26] Michael A McDonough,et al. Dynamic combinatorial chemistry employing boronic acids/boronate esters leads to potent oxygenase inhibitors. , 2012, Angewandte Chemie.
[27] Chuan He,et al. Tet Proteins Can Convert 5-Methylcytosine to 5-Formylcytosine and 5-Carboxylcytosine , 2011, Science.
[28] Hwanho Choi,et al. Structure of human RNA N6-methyladenine demethylase ALKBH5 provides insights into its mechanisms of nucleic acid recognition and demethylation , 2014, Nucleic acids research.
[29] H. Yamamoto,et al. anti-tumor effect of AlkB homolog 3 knockdown in hormone- independent prostate cancer cells. , 2012, Current cancer drug targets.
[30] Julie A. Law,et al. Establishing, maintaining and modifying DNA methylation patterns in plants and animals , 2010, Nature Reviews Genetics.
[31] M. Dong,et al. ALKBH4-dependent demethylation of actin regulates actomyosin dynamics , 2013, Nature Communications.
[32] P. Weber,et al. Crystal structures of catalytic complexes of the oxidative DNA/RNA repair enzyme AlkB , 2006, Nature.
[33] T. Lindahl,et al. Demethylation of 3-Methylthymine in DNA by Bacterial and Human DNA Dioxygenases* , 2004, Journal of Biological Chemistry.
[34] G. J. Gabriel,et al. Synthesis of a FTO inhibitor with anticonvulsant activity. , 2014, ACS chemical neuroscience.
[35] F. Kirpekar,et al. ALKBH8-mediated formation of a novel diastereomeric pair of wobble nucleosides in mammalian tRNA. , 2011, Nature communications.
[36] U. Oppermann,et al. Linking of 2-oxoglutarate and substrate binding sites enables potent and highly selective inhibition of JmjC histone demethylases. , 2012, Angewandte Chemie.
[37] J. Tainer,et al. Human ABH3 structure and key residues for oxidative demethylation to reverse DNA/RNA damage , 2006, The EMBO journal.
[38] M. Jarvelin,et al. A Common Variant in the FTO Gene Is Associated with Body Mass Index and Predisposes to Childhood and Adult Obesity , 2007, Science.
[39] Gideon Rechavi,et al. Gene expression regulation mediated through reversible m6A RNA methylation , 2014, Nature Reviews Genetics.
[40] P. Ratcliffe,et al. Dual-action inhibitors of HIF prolyl hydroxylases that induce binding of a second iron ion. , 2013, Organic & biomolecular chemistry.
[41] A. Bjørk,et al. Repair deficient mice reveal mABH2 as the primary oxidative demethylase for repairing 1meA and 3meC lesions in DNA , 2006, The EMBO journal.