Bimodal antagonism of PKA signalling by ARHGAP36

Nat Commun. 2016 Oct 7:7:12963. doi: 10.1038/ncomms12963.

Abstract

Protein kinase A is a key mediator of cAMP signalling downstream of G-protein-coupled receptors, a signalling pathway conserved in all eukaryotes. cAMP binding to the regulatory subunits (PKAR) relieves their inhibition of the catalytic subunits (PKAC). Here we report that ARHGAP36 combines two distinct inhibitory mechanisms to antagonise PKA signalling. First, it blocks PKAC activity via a pseudosubstrate motif, akin to the mechanism employed by the protein kinase inhibitor proteins. Second, it targets PKAC for rapid ubiquitin-mediated lysosomal degradation, a pathway usually reserved for transmembrane receptors. ARHGAP36 thus dampens the sensitivity of cells to cAMP. We show that PKA inhibition by ARHGAP36 promotes derepression of the Hedgehog signalling pathway, thereby providing a simple rationale for the upregulation of ARHGAP36 in medulloblastoma. Our work reveals a new layer of PKA regulation that may play an important role in development and disease.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 3T3 Cells
  • Animals
  • Carcinogenesis / pathology
  • Catalytic Domain / physiology
  • Cell Line, Tumor
  • Cerebellar Neoplasms / pathology
  • Cyclic AMP / metabolism*
  • Cyclic AMP-Dependent Protein Kinases / antagonists & inhibitors*
  • Cyclic AMP-Dependent Protein Kinases / metabolism*
  • Dogs
  • GTPase-Activating Proteins / metabolism*
  • HEK293 Cells
  • Hedgehog Proteins / metabolism*
  • Humans
  • Madin Darby Canine Kidney Cells
  • Medulloblastoma / pathology*
  • Mice
  • Protein Binding / physiology
  • Protein Kinase Inhibitors / metabolism
  • Proteolysis
  • RNA Interference
  • RNA, Small Interfering / genetics
  • Signal Transduction / physiology
  • Ubiquitination / physiology

Substances

  • ARHGAP36 protein, human
  • GTPase-Activating Proteins
  • Hedgehog Proteins
  • Protein Kinase Inhibitors
  • RNA, Small Interfering
  • rho GTPase-activating protein
  • Cyclic AMP
  • Cyclic AMP-Dependent Protein Kinases