Matches in SemOpenAlex for { <https://semopenalex.org/work/W3213473981> ?p ?o ?g. }
- W3213473981 endingPage "16625" @default.
- W3213473981 startingPage "16609" @default.
- W3213473981 abstract "FTO catalyzes the Fe(II) and 2-oxoglutarate (2OG)-dependent modification of nucleic acids, including the demethylation of N6-methyladenosine (m6A) in mRNA. FTO is a proposed target for anti-cancer therapy. Using information from crystal structures of FTO in complex with 2OG and substrate mimics, we designed and synthesized two series of FTO inhibitors, which were characterized by turnover and binding assays, and by X-ray crystallography with FTO and the related bacterial enzyme AlkB. A potent inhibitor employing binding interactions spanning the FTO 2OG and substrate binding sites was identified. Selectivity over other clinically targeted 2OG oxygenases was demonstrated, including with respect to the hypoxia-inducible factor prolyl and asparaginyl hydroxylases (PHD2 and FIH) and selected JmjC histone demethylases (KDMs). The results illustrate how structure-based design can enable the identification of potent and selective 2OG oxygenase inhibitors and will be useful for the development of FTO inhibitors for use in vivo." @default.
- W3213473981 created "2021-11-22" @default.
- W3213473981 creator A5002485732 @default.
- W3213473981 creator A5003634348 @default.
- W3213473981 creator A5006328079 @default.
- W3213473981 creator A5027942208 @default.
- W3213473981 creator A5031864316 @default.
- W3213473981 creator A5032372602 @default.
- W3213473981 creator A5034271671 @default.
- W3213473981 creator A5034393288 @default.
- W3213473981 creator A5046490260 @default.
- W3213473981 creator A5050244686 @default.
- W3213473981 creator A5051872902 @default.
- W3213473981 creator A5052798526 @default.
- W3213473981 creator A5068579148 @default.
- W3213473981 creator A5074565235 @default.
- W3213473981 creator A5078342571 @default.
- W3213473981 creator A5080857661 @default.
- W3213473981 date "2021-11-11" @default.
- W3213473981 modified "2023-10-16" @default.
- W3213473981 title "Structure-Based Design of Selective Fat Mass and Obesity Associated Protein (FTO) Inhibitors" @default.
- W3213473981 cites W1539796472 @default.
- W3213473981 cites W1964028287 @default.
- W3213473981 cites W1976844911 @default.
- W3213473981 cites W1983652781 @default.
- W3213473981 cites W1986972735 @default.
- W3213473981 cites W1991838121 @default.
- W3213473981 cites W2006922696 @default.
- W3213473981 cites W2028335133 @default.
- W3213473981 cites W2028952070 @default.
- W3213473981 cites W2037989529 @default.
- W3213473981 cites W2038656195 @default.
- W3213473981 cites W2040842455 @default.
- W3213473981 cites W2071930821 @default.
- W3213473981 cites W2080178850 @default.
- W3213473981 cites W2082854050 @default.
- W3213473981 cites W2084588717 @default.
- W3213473981 cites W2097660065 @default.
- W3213473981 cites W2099694670 @default.
- W3213473981 cites W2105718456 @default.
- W3213473981 cites W2116571550 @default.
- W3213473981 cites W2122767064 @default.
- W3213473981 cites W2122969281 @default.
- W3213473981 cites W2124026197 @default.
- W3213473981 cites W2128120865 @default.
- W3213473981 cites W2138992920 @default.
- W3213473981 cites W2142612589 @default.
- W3213473981 cites W2143709841 @default.
- W3213473981 cites W2143857507 @default.
- W3213473981 cites W2163341755 @default.
- W3213473981 cites W2167133694 @default.
- W3213473981 cites W2169494000 @default.
- W3213473981 cites W2226253952 @default.
- W3213473981 cites W2276031634 @default.
- W3213473981 cites W2329246567 @default.
- W3213473981 cites W2483061037 @default.
- W3213473981 cites W2516749516 @default.
- W3213473981 cites W2563912688 @default.
- W3213473981 cites W2600862208 @default.
- W3213473981 cites W2756198750 @default.
- W3213473981 cites W2796769720 @default.
- W3213473981 cites W2902553069 @default.
- W3213473981 cites W2903992936 @default.
- W3213473981 cites W2912048746 @default.
- W3213473981 cites W2913752156 @default.
- W3213473981 cites W2931058147 @default.
- W3213473981 cites W2935701257 @default.
- W3213473981 cites W2936790196 @default.
- W3213473981 cites W2941333182 @default.
- W3213473981 cites W2973457155 @default.
- W3213473981 cites W2991036677 @default.
- W3213473981 cites W3090020170 @default.
- W3213473981 cites W3117936246 @default.
- W3213473981 cites W3118962566 @default.
- W3213473981 cites W3130391515 @default.
- W3213473981 cites W3152343159 @default.
- W3213473981 doi "https://doi.org/10.1021/acs.jmedchem.1c01204" @default.
- W3213473981 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/8631710" @default.
- W3213473981 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/34762429" @default.
- W3213473981 hasPublicationYear "2021" @default.
- W3213473981 type Work @default.
- W3213473981 sameAs 3213473981 @default.
- W3213473981 citedByCount "6" @default.
- W3213473981 countsByYear W32134739812022 @default.
- W3213473981 countsByYear W32134739812023 @default.
- W3213473981 crossrefType "journal-article" @default.
- W3213473981 hasAuthorship W3213473981A5002485732 @default.
- W3213473981 hasAuthorship W3213473981A5003634348 @default.
- W3213473981 hasAuthorship W3213473981A5006328079 @default.
- W3213473981 hasAuthorship W3213473981A5027942208 @default.
- W3213473981 hasAuthorship W3213473981A5031864316 @default.
- W3213473981 hasAuthorship W3213473981A5032372602 @default.
- W3213473981 hasAuthorship W3213473981A5034271671 @default.
- W3213473981 hasAuthorship W3213473981A5034393288 @default.
- W3213473981 hasAuthorship W3213473981A5046490260 @default.
- W3213473981 hasAuthorship W3213473981A5050244686 @default.
- W3213473981 hasAuthorship W3213473981A5051872902 @default.
- W3213473981 hasAuthorship W3213473981A5052798526 @default.