A novel phosphoprotein inhibitor of protein type-1 phosphatase holoenzymes

Biochemistry. 1999 Dec 21;38(51):16952-7. doi: 10.1021/bi992030o.

Abstract

Control of protein phosphatases is now understood to depend on binding to a variety of regulatory or targeting subunits to form holoenzymes with restricted localization and substrate specificity. In addition, the catalytic subunits of both type-1 and type-2 phosphatases bind specific inhibitor proteins. Here, we report discovery of a new inhibitor protein called PHI-1 that is specific for type-1 protein phosphatase (PP1). Recombinant tagged PHI-1 was phosphorylated by protein kinase C at two sites, one a Ser and one a Thr; phosphorylation enhanced inhibitory potency 50-fold. Mutation of Thr57 to Ala gave a protein phosphorylated only on Ser, without change in inhibitory activity, indicating that phosphorylation of Thr57 was required for full activity. Immunoblotting showed that PHI-1 was expressed in most animal tissues and several cell lines, and a second larger protein called PHI-2 was present in different muscles, especially cardiac muscle. Unlike any other known inhibitor, PHI-1 inhibited the myosin- and glycogen-associated holoenzyme versions of PP1 as well as the monomeric catalytic subunit of PP1. Discovery of PHI-1 and PHI-2 opens new possibilities for regulation of PP1 via phosphorylation-dependent signaling pathways.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / isolation & purification
  • Holoenzymes / chemistry
  • Humans
  • Intracellular Signaling Peptides and Proteins
  • Mice
  • Muscle Proteins / chemistry
  • Muscle Proteins / genetics
  • Phosphoprotein Phosphatases / antagonists & inhibitors*
  • Phosphoproteins / biosynthesis
  • Phosphoproteins / chemistry*
  • Phosphoproteins / isolation & purification
  • Protein Biosynthesis
  • Protein Phosphatase 1
  • Proteins / chemistry*
  • Proteins / genetics
  • Proteins / isolation & purification
  • Rats
  • Recombinant Fusion Proteins / biosynthesis
  • Recombinant Fusion Proteins / isolation & purification
  • Sequence Homology, Amino Acid
  • Swine

Substances

  • Enzyme Inhibitors
  • Holoenzymes
  • Intracellular Signaling Peptides and Proteins
  • Muscle Proteins
  • PPP1R14A protein, human
  • Phosphoproteins
  • Ppp1r14a protein, mouse
  • Ppp1r14a protein, rat
  • Ppp1r14b protein, mouse
  • Proteins
  • Recombinant Fusion Proteins
  • phosphoprotein phosphatase inhibitor 1
  • Phosphoprotein Phosphatases
  • Protein Phosphatase 1