Article
Discovery of a novel series of inhibitors of lymphoid tyrosine phosphatase with activity in human T cells.
Journal of medicinal chemistry - 24 Mar 2011
Stanford Stephanie M, Krishnamurthy Divya, Falk Matthew D, Messina Rossella, Debnath Bikash, Li Sheng, Liu Tong, Kazemi Roza, Dahl Russell, He Yantao, Yu Xiao, Chan Andrew C, Zhang Zhong-Yin, Barrios Amy M, Woods Virgil L, Neamati Nouri, Bottini Nunzio
Abstract excerpt
The lymphoid tyrosine phosphatase LYP, encoded by the PTPN22 gene, is a critical regulator of signaling in T cells and recently emerged as a candidate target for therapy of autoimmune diseases. Here, by library screening, we identified a series of noncompetitive inhibitors of LYP that showed activity in primary T cells. Kinetic analysis confirmed that binding of the compounds to the phosphatase is nonmutually...
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