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Updated: Jun 25, 2026

Assessing Cellular Target Engagement by SHP2 (PTPN11) Phosphatase Inhibitors
Published on: July 17, 2020
The N-terminal domain influences the structure and property of protein phosphatase 1
Xiu-Jie Xie1, Wei Huang, Cheng-Zhe Xue
1Department of Biochemistry and Molecular Biology, Beijing Normal University, Beijing Key Laboratory, Beijing 100875, People's Republic of China.
Abstract:
The protein phosphatase 1 has conserved cores in PPP gene family flanked by non-conserved N-terminal domains. PP1 with residues 1-8 deleted or substituted by residues 1-42 of calcineurin catalytic subunit were designated PP1-(9-330) and CNA(1-42)-PP1(9-330), respectively. When compared with PP1, PP1-(9-330) had higher and CNA(1-42)-PP1(9-330) had lower activity with three kinds of substrates; PP1-(9-330) has higher and CNA(1-42)-PP1(9-330) has lower sensitivity to okadaic acid. These results imply that the N-terminal residues influence the activity and sensitivity to inhibitors of PP1. PP1-(9-330), PP1, and CNA(1-42)-PP1(9-330) displayed increasing K (m) and decreasing V (max) with three kinds of substrates, which suggest that the N-terminal residues are connected with the substrates affinity and catalytic efficiency of PP1. PP1-(9-330) has higher and CNA(1-42)-PP1(9-330) has lower fluorescence intensity than PP1, and the emission wavelength maximum was blue-shifted from PP1 to PP1-(9-330) and red-shifted from PP1 to CNA(1-42)-PP1(9-330). Our findings provide evidence that the N-terminal domain is an important region influencing the structure and properties of PP1.
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