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Activation of Engineered Protein Tyrosine Phosphatases with the Biarsenical Compound AsCy3-EDT2
ChemBioChem ( IF 2.6 ) Pub Date : 2017-08-23 05:15:59 , DOI: 10.1002/cbic.201700253
Wai Cheung Chan 1 , Gregory S. Knowlton 1 , Anthony C. Bishop 1
Affiliation  

Turn it up: Cysteine point mutations on the WPD loop generated protein tyrosine phosphatase (PTP) mutants that could be target-specifically activated with the small molecule AsCy3. Given the strict conservation of the WPD loop across the classical PTP family, this strategy for direct chemical control over enzyme activity could be applicable to a range of signaling proteins.

中文翻译:

用双砷化合物AsCy3-EDT2激活工程蛋白酪氨酸磷酸酶。

事实证明:WPD回路上的半胱氨酸点突变产生了蛋白质酪氨酸磷酸酶(PTP)突变体,该突变体可以被小分子AsCy3特异性靶向激活。鉴于经典PTP系列中WPD环的严格保护,这种对酶活性进行直接化学控制的策略可能适用于一系列信号蛋白。
更新日期:2017-08-23
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