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 assay conditions, protein purification methods, crystallisation and structure solution methods. The coordinates and structural factors for FTO in complex with 12, 16 and 21 have been deposited in the RCSB Protein Data Bank as PDB ID 4CXW, 4CXX and 4CXY. See DOI: 10.1039/c4sc02554g Click here for additional data file.
نویسندگان
چکیده
Department of Pharmacy, National Unive 117543, Singapore. E-mail: esther.woon@n 6516 2932 Institute of Molecular and Cell Biology, 61 B School of Biological Sciences, Nanyang Tec 637551, Singapore. E-mail: [email protected] † Electronic supplementary information including full synthesis procedure, T cell-based assay conditions, protein pur structure solution methods. The coordin complex with 12, 16 and 21 have been de as PDB ID 4CXW, 4CXX and 4CXY. See DO ‡ These authors contribute equally to this Cite this: Chem. Sci., 2015, 6, 112
منابع مشابه
A strategy based on nucleotide specificity leads to a subfamily-selective and cell-active inhibitor of N6-methyladenosine demethylase FTO.
The 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 t...
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Content General methods .............................................................................................................................................. S1 Apparatus ......................................................................................................................................................... S2 Abbreviations..................................................
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Departamento de Qúımica Orgánica, Lab Universidad de Santiago de Compostela, Compostela, Spain. E-mail: antonio.mourin Departamento de Fisioloǵıa–CIMUS, Unive 15706 Santiago de Compostela, Spain Department of Integrative Structural Biolo U964, 1, rue Laurent Fries, 67400 Illkirch, F Departmento de Qúımica Fundamental, Zapateira s/n, 15071 A Coruña, Spain † Accession number. The coordinates and ...
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School of Biological Sciences, University of CO4 3SQ, UK. E-mail: [email protected] Department of Chemistry and Biochemistry Oregon 97850, USA. E-mail: candrew@eou. Faculty of Science and Education Science, Iraq Medical Research Center, Hawler Medical Swiss Light Source, Paul Scherrer Institute, Manchester Institute of Biotechnology, 131 School of Chemistry, Bangor University, Ba Molecular Bio...
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عنوان ژورنال:
دوره 6 شماره
صفحات -
تاریخ انتشار 2015