Calmodulin regulates Ca2+-sensing receptor-mediated Ca2+ signaling and its cell surface expression

J Biol Chem. 2010 Nov 12;285(46):35919-31. doi: 10.1074/jbc.M110.147918. Epub 2010 Sep 8.

Abstract

The Ca(2+)-sensing receptor (CaSR) is a member of family C of the GPCRs responsible for sensing extracellular Ca(2+) ([Ca(2+)](o)) levels, maintaining extracellular Ca(2+) homeostasis, and transducing Ca(2+) signaling from the extracellular milieu to the intracellular environment. In the present study, we have demonstrated a Ca(2+)-dependent, stoichiometric interaction between CaM and a CaM-binding domain (CaMBD) located within the C terminus of CaSR (residues 871-898). Our studies suggest a wrapping around 1-14-like mode of interaction that involves global conformational changes in both lobes of CaM with concomitant formation of a helical structure in the CaMBD. More importantly, the Ca(2+)-dependent association between CaM and the C terminus of CaSR is critical for maintaining proper responsiveness of intracellular Ca(2+) responses to changes in extracellular Ca(2+) and regulating cell surface expression of the receptor.

Publication types

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

MeSH terms

  • Algorithms
  • Amino Acid Sequence
  • Binding Sites / genetics
  • Calcium / metabolism*
  • Calcium Signaling
  • Calmodulin / metabolism*
  • Cell Membrane / metabolism*
  • Circular Dichroism
  • Flow Cytometry
  • HEK293 Cells
  • Humans
  • Immunoprecipitation
  • Intracellular Space / metabolism
  • Kinetics
  • Molecular Sequence Data
  • Mutation
  • Protein Binding
  • Receptors, Calcium-Sensing / genetics
  • Receptors, Calcium-Sensing / metabolism*
  • Sequence Homology, Amino Acid

Substances

  • Calmodulin
  • Receptors, Calcium-Sensing
  • Calcium