Structural Basis for the Subversion of MAP Kinase Signaling by an Intrinsically Disordered Parasite Secreted Agonist

Structure. 2017 Jan 3;25(1):16-26. doi: 10.1016/j.str.2016.10.011. Epub 2016 Nov 23.

Abstract

The causative agent of toxoplasmosis, the intracellular parasite Toxoplasma gondii, delivers a protein, GRA24, into the cells it infects that interacts with the mitogen-activated protein (MAP) kinase p38α (MAPK14), leading to activation and nuclear translocation of the host kinase and a subsequent inflammatory response that controls the progress of the parasite. The purification of a recombinant complex of GRA24 and human p38α has allowed the molecular basis of this activation to be determined. GRA24 is shown to be intrinsically disordered, binding two kinases that act independently, and is the only factor required to bypass the canonical mitogen-activated protein kinase activation pathway. An adapted kinase interaction motif (KIM) forms a highly stable complex that competes with cytoplasmic regulatory partners. In addition, the recombinant complex forms a powerful in vitro tool to evaluate the specificity and effectiveness of p38α inhibitors that have advanced to clinical trials, as it provides a hitherto unavailable stable and highly active form of p38α.

Keywords: GRA24; MAPK p38; Toxoplasma effector; immunity; intrinsically disordered protein.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Binding Sites
  • Cell Nucleus / metabolism
  • Humans
  • Intrinsically Disordered Proteins / chemistry
  • Intrinsically Disordered Proteins / metabolism
  • MAP Kinase Signaling System
  • Mitogen-Activated Protein Kinase 14 / chemistry*
  • Mitogen-Activated Protein Kinase 14 / metabolism*
  • Models, Molecular
  • Protein Binding
  • Protein Conformation
  • Protein Domains
  • Protein Multimerization
  • Protozoan Proteins / chemistry*
  • Protozoan Proteins / metabolism*
  • Recombinant Proteins / chemistry
  • Recombinant Proteins / metabolism

Substances

  • GRA3 protein, Toxoplasma gondii
  • Intrinsically Disordered Proteins
  • Protozoan Proteins
  • Recombinant Proteins
  • Mitogen-Activated Protein Kinase 14