Plasma membrane targeting is essential for Rem-mediated Ca2+ channel inhibition

J Biol Chem. 2007 Sep 28;282(39):28431-28440. doi: 10.1074/jbc.M706176200. Epub 2007 Aug 7.

Abstract

The small GTPase Rem is a potent negative regulator of high voltage-activated Ca(2+) channels and a known interacting partner for Ca(2+) channel accessory beta subunits. The mechanism for Rem-mediated channel inhibition remains controversial, although it has been proposed that Ca(V)beta association is required. Previous work has shown that a C-terminal truncation of Rem (Rem-(1-265)) displays reduced in vivo binding to membrane-localized beta 2a and lacks channel regulatory function. In this paper, we describe a role for the Rem C terminus in plasma membrane localization through association with phosphatidylinositol lipids. Moreover, Rem-(1-265) can associate with beta 2a in vitro and beta 1b in vivo, suggesting that the C terminus does not directly participate in Ca(V)beta association. Despite demonstrated beta 1b binding, Rem-(1-265) was not capable of regulating a Ca(V)1.2-beta 1b channel complex, indicating that beta subunit binding is not sufficient for channel regulation. However, fusion of the CAAX domain from K-Ras4B or H-Ras to the Rem-(1-265) C terminus restored membrane localization and Ca(2+) channel regulation, suggesting that beta binding and membrane localization are independent events required for channel inhibition.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Calcium Channels, L-Type / genetics
  • Calcium Channels, L-Type / metabolism*
  • Cell Line
  • Cell Membrane / genetics
  • Cell Membrane / metabolism*
  • Humans
  • Mice
  • Monomeric GTP-Binding Proteins / genetics
  • Monomeric GTP-Binding Proteins / metabolism*
  • Phosphatidylinositols / metabolism*
  • Protein Binding / genetics
  • Protein Structure, Tertiary / genetics
  • Protein Subunits / genetics
  • Protein Subunits / metabolism
  • Proto-Oncogene Proteins p21(ras) / genetics
  • Proto-Oncogene Proteins p21(ras) / metabolism
  • Recombinant Fusion Proteins / genetics
  • Recombinant Fusion Proteins / metabolism
  • ras Proteins / genetics
  • ras Proteins / metabolism

Substances

  • Calcium Channels, L-Type
  • KRAS protein, human
  • L-type calcium channel alpha(1C)
  • Phosphatidylinositols
  • Protein Subunits
  • Recombinant Fusion Proteins
  • Rem protein, mouse
  • Monomeric GTP-Binding Proteins
  • Proto-Oncogene Proteins p21(ras)
  • ras Proteins