Sci. STKE, 25 May 2004
Regulation of GABA Receptor Activity by Neurosteroids and Phosphorylation
*Corresponding author. E-mail: email@example.com
These two animations show two models for how neurosteroids and protein kinases regulate the flow of chloride ions (Cl–) through ionotropic gamma-aminobutyric acid (GABA) receptors. The difference between the two models is the sequence of the phosphorylation and neurosteroid-binding events. In the first model, binding of the neurosteroid allopregnanolone (ALLO) occurs first and allows a protein kinase C (PKC) phosphorylation site to become accessible. Phosphorylation of the channel increases flux through the channel. In the second model, phosphorylation by PKC occurs first and allows the neurosteroid (ALLO) to bind and increase flux through the channel. In both animations, PKC activity is stimulated by heterotrimeric G proteins, which can be activated by G protein-coupled receptors (GPCRs). This provides a mechanism for cross talk between ion channels and GPCRs. The animations are animated gifs that have two parts: (i) a diagrammatic representation of the sequence of events at the channel in the membrane and (ii) a representative current trace of data obtained using electrophysiological techniques. These animations would be useful in teaching how allosteric modulators (neurosteroids) and covalent modulators (kinases) can work together as regulators of protein activity.
Animation 1. Neurosteroid Binding Exposes a Phosphorylation Site (Model A). This animation shows one model for how neurosteroids may increase Cl– flux through a GABA
Animation 2. Phosphorylation Exposes a Neurosteroid Binding Site (Model B). This animation shows an alternative model for how neurosteroids and PKC may increase Cl– flux through GABA
Learning Resource Type: Animation
Context: Undergraduate upper division, graduate, professional (degree program)
Intended Users: Teacher, learner
Intended Educational Use: Teach, learn
Discipline: Cell biology, molecular biology, neurobiology
Keywords: Signal transduction, channel, GABAergic, electrophysiology
Size: 165 kb (animation 1), 195 kb (animation 2)
Limits for Use
Rights: This material may be downloaded, printed, linked to, and/or redistributed without modification for noncommercial, course-teaching purposes only, provided credit to STKE is included by listing the citation for the teaching resource.
Citation: J. Tasker, Regulation of GABA receptor activity by neurosteroids and phosphorylation. Sci. STKE 2004, tr4 (2004).
Science Signaling. ISSN 1937-9145 (online), 1945-0877 (print). Pre-2008: Science's STKE. ISSN 1525-8882