Dual-specific Protein Phosphatase Inhibitors
Phosphorylation and dephosphorylation occur in various proteins as post-translational modifications of proteins. Phosphorylation and dephosphorylation are intricately regulated and contribute to the control of signaling and enzymatic activity.
Protein phosphatases are enzymes that dephosphorylate phosphorylated proteins. They are classified into tyrosine phosphatases and serine/threonine phosphatases according to their specificity for amino acid residues. Dual (double)-specific protein phosphatases that act on tyrosine/serine/threonine are also known.
RE12 and RE44 are selective inhibitors of the dual-specific protein phosphatases VHR and CDC25B.
RE12
Target of inhibition：Vaccinia H1-related Phosphatase (VHR)
VHR is a phosphatase that dephosphorylates ERK1/2 and JNK1/2 of the MAPK family. It is attracting attention for its involvement in cell cycle regulation or as a target for development of anticancer drugs.
RE44
Target of inhibition：Cell Division Cycle 25 B (CDC25B)、Cell Division Cycle 25 A (CDC25A)
CDC25B and CDC25A are involved in the acceleration of cell cycle progression and checkpoint regulation for DNA damage. Increased expression has been reported in various cancer cells.
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