Forward genetics reveals a conserved CNBHD-CNBHD interface that restrains EAG channel activation to regulate sleep.

TitleForward genetics reveals a conserved CNBHD-CNBHD interface that restrains EAG channel activation to regulate sleep.
Publication TypeJournal Article
Year of Publication2026
AuthorsHuang X, Kannan S, Robertson GA, Wang H
JournalPLoS Genet
Volume22
Issue10
Paginatione1012255
Date Published2026 Oct
ISSN1553-7404
KeywordsAnimals, Caenorhabditis elegans, Caenorhabditis elegans Proteins, Ether-A-Go-Go Potassium Channels, Gain of Function Mutation, Glycine, Humans, Ion Channel Gating, Neurons, Protein Domains, Sleep
Abstract

KCNH voltage-gated potassium channels regulate neuronal excitability, yet how their hallmark cyclic nucleotide-binding homology domains (CNBHDs) influence channel gating to regulate behavior remains unclear. Using an unbiased forward genetic screen in Caenorhabditis elegans, we identified a gain-of-function mutation in the EAG-subfamily KCNH channel EGL-2 that suppresses sleep. The mutation (G574E) alters a highly conserved glycine residue at the interface between CNBHDs of adjacent channel subunits. EGL-2 functions cell-autonomously in the central sleep-promoting neuron ALA. In vivo calcium imaging showed that the gain-of-function mutation suppresses sleep by inhibiting ALA neuronal activity, consistent with enhanced potassium channel activity. Genetic analysis demonstrated that the sleep-suppressing phenotype of G574E requires both an intact potassium selectivity filter and the intrinsic ligand-occupied CNBHD. A second substitution at the same glycine (G574R), which introduces a positively charged side chain in contrast to the negatively charged side chain in G574E, similarly suppresses sleep, indicating that perturbation of the CNBHD-CNBHD interface, rather than the specific amino acid change, underlies the phenotype. Moreover, mutations at the corresponding residue in the ERG-subfamily KCNH channels C. elegans UNC-103 and human hERG also produce gain-of-function effects, and electrophysiological analysis showed that hERG(G749R) shifts voltage-dependent channel activation to more negative potentials and accelerates activation kinetics. These findings identify EGL-2 as an important sleep regulator and uncover a conserved gating mechanism by which the intersubunit CNBHD-CNBHD interface restrains KCNH channel activation to regulate neuronal excitability and behavior.

DOI10.1371/journal.pgen.1012255
Alternate JournalPLoS Genet
PubMed ID42821616
PubMed Central IDPMC13660981
Grant ListP40 OD010440 / OD / NIH HHS / United States
R01 HL131403 / HL / NHLBI NIH HHS / United States
R01 NS081320 / NS / NINDS NIH HHS / United States
R35 GM150658 / GM / NIGMS NIH HHS / United States