Thyroid-stimulating hormone/cAMP and glycogen synthase kinase 3beta elicit opposing effects on Rap1GAP stability

J Biol Chem. 2004 Feb 13;279(7):5501-7. doi: 10.1074/jbc.M305824200. Epub 2003 Dec 2.

Abstract

Beyond regulating Rap activity, little is known regarding the regulation and function of the Rap GTPase-activating protein Rap1GAP. Tuberin and E6TP1 protein levels are tightly regulated through ubiquitin-mediated proteolysis. A role for these RapGAPs, along with SPA-1, as tumor suppressors has been demonstrated. Whether Rap1GAP performs a similar role was investigated. We now report that Rap1GAP protein levels are dynamically regulated in thyroid-stimulating hormone (TSH)-dependent thyroid cells. Upon TSH withdrawal, Rap1GAP undergoes a net increase in phosphorylation followed by proteasome-mediated degradation. Sequence analysis identified two putative destruction boxes in the Rap1GAP C-terminal domain. Glycogen synthase kinase 3beta (GSK3beta) phosphorylated Rap1GAP immunoprecipitated from thyroid cells, and GSK3beta inhibitors prevented phosphorylation and degradation of endogenous Rap1GAP. Co-expression of GSK3beta and Rap1GAP in human embryonic kidney 293 cells stimulated proteasome-dependent Rap1GAP turnover. Mutational analysis established a role for serine 525 in the regulation of Rap1GAP stability. Overexpression of Rap1GAP in thyroid cells impaired TSH/cAMP-stimulated p70S6 kinase activity and cell proliferation. These data are the first to show that Rap1GAP protein levels are tightly regulated and are the first to support a role for Rap1GAP as a tumor suppressor.

Publication types

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

MeSH terms

  • Animals
  • Blotting, Western
  • Bromodeoxyuridine / pharmacology
  • Cell Division
  • Cell Line
  • Cyclic AMP / metabolism*
  • Cysteine Endopeptidases / metabolism
  • DNA Mutational Analysis
  • Dose-Response Relationship, Drug
  • GTPase-Activating Proteins / metabolism
  • Glycogen Synthase Kinase 3 / metabolism*
  • Glycogen Synthase Kinase 3 beta
  • Humans
  • Multienzyme Complexes / antagonists & inhibitors
  • Multienzyme Complexes / metabolism
  • Mutagenesis, Site-Directed
  • Mutation
  • Phosphorylation
  • Precipitin Tests
  • Proteasome Endopeptidase Complex
  • Protein Structure, Tertiary
  • Rats
  • Rats, Wistar
  • Repressor Proteins / metabolism
  • Ribosomal Protein S6 Kinases, 70-kDa / metabolism
  • Thyroid Gland / metabolism
  • Thyrotropin / metabolism*
  • Time Factors
  • Transfection
  • Tuberous Sclerosis Complex 2 Protein
  • Tumor Suppressor Proteins
  • rap1 GTP-Binding Proteins / metabolism*

Substances

  • E6-target protein 1
  • GTPase-Activating Proteins
  • Multienzyme Complexes
  • Repressor Proteins
  • TSC2 protein, human
  • Tuberous Sclerosis Complex 2 Protein
  • Tumor Suppressor Proteins
  • Thyrotropin
  • Cyclic AMP
  • GSK3B protein, human
  • Glycogen Synthase Kinase 3 beta
  • Gsk3b protein, rat
  • Ribosomal Protein S6 Kinases, 70-kDa
  • Glycogen Synthase Kinase 3
  • Cysteine Endopeptidases
  • Proteasome Endopeptidase Complex
  • rap1 GTP-Binding Proteins
  • Bromodeoxyuridine