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Structure paper

TitleStructural basis for domain coupling in heteromeric glycine receptors revealed by an atypical allosteric agonist.
Journal, issue, pagesSci Adv, Vol. 12, Issue 7, Page eaeb2036, Year 2026
Publish dateFeb 13, 2026
AuthorsEric Gibbs / Bjarne Feddersen / Kayla J Kindig / David Seiferth / Philip C Biggin / Sudha Chakrapani /
PubMed AbstractGlycine receptors (GlyRs), pentameric ligand-gated ion channels (pLGICs), mediate sensory and motor functions. GlyR functional states are well characterized; however, structural details of ...Glycine receptors (GlyRs), pentameric ligand-gated ion channels (pLGICs), mediate sensory and motor functions. GlyR functional states are well characterized; however, structural details of transitions between states remain undefined. Here, we determined cryo-electron microscopy structures of GlyRα1β (with gephyrin E-domain) at varying concentrations of ivermectin, a transmembrane domain (TMD) allosteric agonist, and at saturating concentrations of strychnine, a competitive antagonist at the extracellular domain (ECD). Electrophysiology shows that ivermectin activates GlyR even with strychnine present. Structures with both ligands reveal intermediate states featuring a desensitized TMD and an ECD between closed and desensitized conformations, providing insights into domain cooperativity and ligand efficacy. Molecular dynamics simulations show how ivermectin affects strychnine dynamics. These data support a model where ivermectin activates GlyRs through a concerted and near-symmetric TMD mechanism, whereas allosteric ECD motions are graded and spatially heterogeneous. These findings reveal unanticipated features of GlyR gating and establish principles of allosteric modulation applicable to pLGICs.
External linksSci Adv / PubMed:41686897 / PubMed Central
MethodsEM (single particle)
Resolution2.86 - 2.89 Å
Structure data

71705

9pkw

EMDB-71705, PDB-9pkw:
Alpha1/Beta Heteromeric Glycine receptor in the presence of 0.200 mM strychnine and 200 nM ivermectin
Method: EM (single particle) / Resolution: 2.86 Å

71706

9pkx

EMDB-71706, PDB-9pkx:
Alpha1/Beta Heteromeric Glycine receptor in the presence of 0.200 mM strychnine and 500 nM ivermectin
Method: EM (single particle) / Resolution: 2.86 Å

71707

9pky

EMDB-71707, PDB-9pky:
Alpha1/Beta Heteromeric Glycine receptor in the presence of 0.200 mM strychnine and 2000 nM ivermectin
Method: EM (single particle) / Resolution: 2.89 Å

71708

9pkz

EMDB-71708, PDB-9pkz:
Alpha1/Beta Heteromeric Glycine receptor in the presence of 0.200 mM strychnine and 0.02 mM ivermectin
Method: EM (single particle) / Resolution: 2.89 Å

Chemicals

ChemComp-SY9:
STRYCHNINE

ChemComp-NAG:
2-acetamido-2-deoxy-beta-D-glucopyranose

ChemComp-IVM:
(2aE,4E,5'S,6S,6'R,7S,8E,11R,13R,15S,17aR,20R,20aR,20bS)-6'-[(2S)-butan-2-yl]-20,20b-dihydroxy-5',6,8,19-tetramethyl-17

Source
  • danio rerio (zebrafish)
KeywordsTRANSPORT PROTEIN / Ion Channel / Pentameric / Glycine / Receptor

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