A Fluorescence Polarization Biophysical Assay for the Naegleria DNA Hydroxylase Tet1.
A Fluorescence Polarization Biophysical Assay for the Naegleria DNA Hydroxylase Tet1.
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DOI：
10.1021/acsmedchemlett.5b00366
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发表时间：
2016-02-11
影响因子：
4.2
通讯作者：
Wang, Xiang
中科院分区：
文献类型：
--
作者：
Marholz, Laura J.;Wang, Wei;Zheng, Yu;Wang, Xiang
关键词：
The discovery of the 5-methylcytosine (5mC) oxidation by the ten–eleven translocation (Tet) protein family was an important advancement in our understanding of DNA-modified epigenetics. Potent inhibitors of these proteins are greatly desired for both the understanding of the functions of these enzymes and to serve as eventual therapeutic leads. So far, the discovery of such small molecules with high affinity has been quite limited. Original tools to screen for activity are greatly needed in order to accelerate this process. Here we present a novel fluorescent probe, and the results of a fluorescence polarization-based binding assay for Naegleria Tet1, a homologue to mammalian Tet. A fluorescence polarization-based competition assay was also established and applied to the rapid and quantitative measurement of the binding affinity of the cofactor αKG and several known Tet1 inhibitors.
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影响因子：
16
作者：
Piccolo, Francesco M.;Bagci, Hakan;Brown, Karen E.;Landeira, David;Soza-Ried, Jorge;Feytout, Amelie;Mooijman, Dylan;Hajkova, Petra;Leitch, Harry G.;Tada, Takashi;Kriaucionis, Skirmantas;Dawlaty, Meelad M.;Jaenisch, Rudolf;Merkenschlager, Matthias;Fisher, Amanda G.
通讯作者：
Fisher, Amanda G.
影响因子：
50.3
作者：
Xu W;Yang H;Liu Y;Yang Y;Wang P;Kim SH;Ito S;Yang C;Wang P;Xiao MT;Liu LX;Jiang WQ;Liu J;Zhang JY;Wang B;Frye S;Zhang Y;Xu YH;Lei QY;Guan KL;Zhao SM;Xiong Y
通讯作者：
Xiong Y
影响因子：
62.1
作者：
Lu X;Zhao BS;He C
通讯作者：
He C
影响因子：
12.3
作者：
Scourzic L;Mouly E;Bernard OA
通讯作者：
Bernard OA
DOI：
10.1016/j.tig.2014.07.005
发表时间：
2014-10
期刊：
Trends in genetics : TIG
影响因子：
--
作者：
Huang Y;Rao A
通讯作者：
Rao A