Several structural domains contribute to the regulation of N-type calcium channel inactivation by the beta 3 subunit

J Biol Chem. 2004 Jan 30;279(5):3793-800. doi: 10.1074/jbc.M308991200. Epub 2003 Nov 5.

Abstract

Calcium channel beta subunits are essential regulatory elements of the gating properties of high voltage-activated calcium channels. Co-expression with beta(3) subunits typically accelerates inactivation, whereas co-expression with beta(4) subunits results in a slowly inactivating phenotype. Here, we have examined the molecular basis of the differential effect of these two subunits on the inactivation characteristics of Ca(v)2.2 + alpha(2)-delta(1) N-type calcium channels by creating a series of 22 chimeric beta subunits that are based on various combinations of variable and conserved regions of the parent beta subunit isoforms. Our data show that replacement of the N terminus region of beta(4) with a corresponding 14-amino acid stretch of beta(3) sequence accelerates the inactivation kinetics to levels seen with wild type beta(3). A similar kinetic speeding is observed by a concomitant substitution of the second conserved and variable regions, but not when these regions are substituted individually, suggesting that 1) the second variable and conserved regions cooperatively regulate N-type calcium channel inactivation and 2) that there are two redundant mechanisms that allow the beta(3) subunit to accelerate N-type channel inactivation. In contrast with previous reports in Ca(v)2.1 calcium channels, deletion of the C-terminal region of Ca(v)2.2 did not alter the regulation of the channel by wild type and chimeric beta subunits. Hence, the molecular underpinnings of beta subunit regulation of voltage-gated calcium channels appear to vary with calcium channel subtype.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Calcium / metabolism
  • Calcium Channels / chemistry
  • Calcium Channels, N-Type / chemistry*
  • Calcium Channels, N-Type / physiology*
  • Cell Line
  • Electrophysiology
  • Gene Deletion
  • Humans
  • Kinetics
  • Molecular Sequence Data
  • Phenotype
  • Precipitin Tests
  • Protein Conformation
  • Protein Structure, Secondary
  • Protein Structure, Tertiary
  • Rats
  • Sequence Homology, Amino Acid
  • Transfection

Substances

  • Calcium Channels
  • Calcium Channels, N-Type
  • Calcium