Dynamic metabolic control of an ion channel
Research output: Contribution to journal › Review article › Invited › peer-review
Contributors
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 language | English |
|---|---|
| Pages (from-to) | 219-47 |
| Number of pages | 29 |
| Journal | Progress in Molecular Biology and Translational Science |
| Volume | 123 |
| Publication status | Published - 2014 |
| Peer-reviewed | Yes |
| Externally published | Yes |
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