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Ordered phosphorylation of p42mapk by MAP kinase kinase

T A Haystead1, P Dent, J Wu

  • 1Department of Pharmacology, University of Virginia, Charlottesville 22908.

FEBS Letters
|July 13, 1992
PubMed

Insights

This study details the preparation of phosphorylated p42 mitogen-activated protein kinase (MAPK) for phosphatase assays. Tyr185 phosphorylation of p42MAPK precedes Thr183 phosphorylation, enhancing its affinity for MAP kinase kinase.

Area of Science:

  • Molecular Biology
  • Enzymology
  • Signal Transduction

Background:

  • p42 mitogen-activated protein kinase (MAPK) is a key signaling molecule.
  • The phosphorylation status of p42MAPK regulates its activity and interactions.
  • Understanding the sequential phosphorylation events is crucial for deciphering MAPK pathway function.

Purpose of the Study:

  • To describe the preparation of milligram quantities of [32P]p42MAPK phosphorylated at specific sites (Tyr185 or Tyr185/Thr183).
  • To investigate the substrate properties of differentially phosphorylated p42MAPK for protein phosphatases.
  • To elucidate the order and functional significance of Tyr185 and Thr183 phosphorylation in p42MAPK activation.

Main Methods:

  • Radiolabeling of p42MAPK with [32P]ATP.
  • Controlled phosphorylation of p42MAPK using limiting ATP conditions to favor Tyr185 phosphorylation.
  • Enzyme kinetic assays to determine the Michaelis constant (Km) for MAP kinase kinase (MAPKK) with different p42MAPK phosphorylation states.

Main Results:

  • Milligram amounts of [32P]p42MAPK, phosphorylated at Tyr185 or diphosphorylated at Tyr185/Thr183, were successfully prepared.
  • Tyr185-phosphorylated p42MAPK accumulated under conditions of limiting ATP, while Thr183 phosphorylation required further activation.
  • Tyr185-phosphorylated p42MAPK showed a significantly lower apparent Km (46.6 nM) for MAPKK compared to the dephospho form (476 nM), indicating a 10-fold increase in affinity.

Conclusions:

  • The phosphorylation of Tyr185 on p42MAPK precedes and is a prerequisite for Thr183 phosphorylation.
  • This sequential phosphorylation dramatically enhances the affinity of p42MAPK for its upstream activator, MAPKK.
  • The findings provide critical insights into the regulatory mechanism of MAPK pathway activation and substrate recruitment.

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