化学
蛋白质酪氨酸磷酸酶
伊萨丁
原癌基因酪氨酸蛋白激酶Src
奥西多尔
生物化学
磷酸酶
蛋白磷酸酶2
酪氨酸
脚手架
计算生物学
立体化学
酶
磷酸化
医学
生物
生物医学工程
催化作用
有机化学
作者
Harshani R. Lawrence,Roberta Pireddu,Liwei Chen,Yunting Luo,Shen Shu Sung,Ann Marie Szymanski,M.L. Richard Yip,Wayne C. Guida,Saı̈d M. Sebti,Jie Wu,Nicholas J. Lawrence
摘要
Screening of the NCI diversity set of compounds has led to the identification of 5 (NSC-117199), which inhibits the protein tyrosine phosphatase (PTP) Shp2 with an IC50 of 47 microM. A focused library incorporating an isatin scaffold was designed and evaluated for inhibition of Shp2 and Shp1 PTP activities. Several compounds were identified that selectively inhibit Shp2 over Shp1 and PTP1B with low to submicromolar activity. A model for the binding of the active compounds is proposed.
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