Phosphorylated Peptide Derived from the Myosin Phosphatase Target Subunit Is a Novel Inhibitor of Protein Phosphatase-1.

ABSTRACT: Identification of specific protein phosphatase-1 (PP1) inhibitors is of special importance regarding the study of its cellular functions and may have therapeutic values in diseases coupled to signaling processes. In this study, we prove that a phosphorylated peptide of the inhibitory region of myosin phosphatase (MP) target subunit (MYPT1), R⁶⁹⁰QSRRS(pT696)QGVTL⁷⁰¹ (P-Thr696-MYPT1^690-701), interacts with and inhibits the PP1 catalytic subunit (PP1c, IC₅₀ = 3.84 µM) and the MP holoenzyme (Flag-MYPT1-PP1c, IC₅₀ = 3.84 µM). Saturation transfer difference NMR measurements established binding of hydrophobic and basic regions of P-Thr696-MYPT1^690-701 to PP1c, suggesting interactions with the hydrophobic and acidic substrate bindin

SUBMITTER: Konya Z 

PROVIDER: S-EPMC10003451 | biostudies-literature | 2023 Mar

REPOSITORIES: biostudies-literature