Multiple structural elements contribute to voltage-dependent facilitation of neuronal alpha 1C (CaV1.2) L-type calcium channels

Neuropharmacology. 2001 Jun;40(8):1050-7. doi: 10.1016/s0028-3908(01)00025-9.

Abstract

Voltage- and frequency-dependent facilitation of calcium channel activity has been implicated in a number of key physiological processes. Various mechanisms have been proposed to mediate these regulations, including a switch between channel gating modes, voltage-dependent phosphorylation, and a voltage-dependent deinhibition of G-protein block. Studying such modulation on recombinant Ca channels expressed in oocytes, we previously reported that alpha(1C) L-type calcium channel contrast with non-L type Ca channels by its ability to exhibit facilitation by pre-depolarization (Voltage-dependent facilitation of a neuronal alpha(IC) L-type calcium channel, E. Bourinet et al., EMBO Journal, 1994; 13, 5032-5039). To further analyze this effect, we have investigated the molecular determinants which mediate the differences in voltage-dependent facilitation between "facilitable" alpha(1C) and "non facilitable" alpha(1E) calcium channels. We used a series of chimeras which combine the four transmembrane domains of the two channels. Results show that the four domains of alpha(1C) contribute to facilitation, with domain I being most critical. This domain is required but not sufficient alone to generate facilitation. The minimal requirement to observe the effect is the presence of domain I plus one of the three others. We conclude that similarly to activation gating, voltage-dependent facilitation of alpha(1C) is a complex process which involves multiple structural elements were domains I and III play the major role.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Calcium Channel Agonists / pharmacology
  • Calcium Channels / chemistry
  • Calcium Channels / physiology*
  • Calcium Channels, L-Type / chemistry
  • Calcium Channels, L-Type / physiology*
  • Calcium Channels, R-Type
  • Cation Transport Proteins*
  • Humans
  • Ion Channel Gating
  • Membrane Potentials / physiology
  • Neurons / drug effects
  • Neurons / physiology
  • Oocytes / physiology
  • Patch-Clamp Techniques
  • Pyrroles / pharmacology
  • Structure-Activity Relationship
  • Xenopus

Substances

  • CACNA1E protein, human
  • Calcium Channel Agonists
  • Calcium Channels
  • Calcium Channels, L-Type
  • Calcium Channels, R-Type
  • Cation Transport Proteins
  • L-type calcium channel alpha(1C)
  • Pyrroles
  • FPL 64176