Dynamic metabolic control of an ion channel

Research output: Contribution to journalReview articleInvitedpeer-review

Contributors

  • Bertil Hille - , University of Washington (Author)
  • Eamonn Dickson - , University of Washington (Author)
  • Martin Kruse - , University of Washington (Author)
  • Bjoern Falkenburger - , University Hospital Aachen (Author)

Abstract

G-protein-coupled receptors mediate responses to external stimuli in various cell types. We are interested in the modulation of KCNQ2/3 potassium channels by the Gq-coupled M1 muscarinic (acetylcholine) receptor (M1R). Here, we describe development of a mathematical model that incorporates all known steps along the M1R signaling cascade and accurately reproduces the macroscopic behavior we observe when KCNQ2/3 currents are inhibited following M1R activation. Gq protein-coupled receptors of the plasma membrane activate phospholipase C (PLC) which cleaves the minor plasma membrane lipid phosphatidylinositol 4,5-bisphosphate (PI(4,5)P2) into the second messengers diacylgycerol and inositol 1,4,5-trisphosphate, leading to calcium release, protein kinase C (PKC) activation, and PI(4,5)P2 depletion. Combining optical and electrical techniques with knowledge of relative abundance of each signaling component has allowed us to develop a kinetic model and determine that (i) M1R activation and M1R/Gβ interaction are fast; (ii) Gαq/Gβ separation and Gαq/PLC interaction have intermediate time constants; (iii) the amount of activated PLC limits the rate of KCNQ2/3 suppression; (iv) weak PLC activation can elicit robust calcium signals without net PI(4,5)P2 depletion or KCNQ2/3 channel inhibition; and (v) depletion of PI(4,5)P2, and not calcium/CaM or PKC-mediated phosphorylation, closes KCNQ2/3 potassium channels, thereby increasing neuronal excitability.

Details

Original languageEnglish
Pages (from-to)219-47
Number of pages29
JournalProgress in Molecular Biology and Translational Science
Volume123
Publication statusPublished - 2014
Peer-reviewedYes
Externally publishedYes

External IDs

Scopus 84896738266
ORCID /0000-0002-2387-526X/work/176343370

Keywords

Keywords

  • Animals, GTP-Binding Proteins/metabolism, Humans, Ion Channel Gating, Ion Channels/metabolism, Models, Biological, Receptors, G-Protein-Coupled/metabolism, Type C Phospholipases/metabolism