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TitleStructure and dynamics of differential ligand binding in the human ρ-type GABA receptor.
Journal, issue, pagesNeuron, Vol. 111, Issue 21, Page 3450-33464.e5, Year 2023
Publish dateNov 1, 2023
AuthorsJohn Cowgill / Chen Fan / Nandan Haloi / Victor Tobiasson / Yuxuan Zhuang / Rebecca J Howard / Erik Lindahl /
PubMed AbstractThe neurotransmitter γ-aminobutyric acid (GABA) drives critical inhibitory processes in and beyond the nervous system, partly via ionotropic type-A receptors (GABARs). Pharmacological properties of ...The neurotransmitter γ-aminobutyric acid (GABA) drives critical inhibitory processes in and beyond the nervous system, partly via ionotropic type-A receptors (GABARs). Pharmacological properties of ρ-type GABARs are particularly distinctive, yet the structural basis for their specialization remains unclear. Here, we present cryo-EM structures of a lipid-embedded human ρ1 GABAR, including a partial intracellular domain, under apo, inhibited, and desensitized conditions. An apparent resting state, determined first in the absence of modulators, was recapitulated with the specific inhibitor (1,2,5,6-tetrahydropyridin-4-yl)methylphosphinic acid and blocker picrotoxin and provided a rationale for bicuculline insensitivity. Comparative structures, mutant recordings, and molecular simulations with and without GABA further explained the sensitized but slower activation of ρ1 relative to canonical subtypes. Combining GABA with picrotoxin also captured an apparent uncoupled intermediate state. This work reveals structural mechanisms of gating and modulation with applications to ρ-specific pharmaceutical design and to our biophysical understanding of ligand-gated ion channels.
External linksNeuron / PubMed:37659407
MethodsEM (single particle)
Resolution2.2 - 3.36 Å
Structure data

17045

8op9

EMDB-17045, PDB-8op9:
CryoEM structure of human rho1 GABAA receptor in complex with GABA
Method: EM (single particle) / Resolution: 3.36 Å

17106

8oq6

EMDB-17106, PDB-8oq6:
CryoEM structure of human rho1 GABAA receptor apo state
Method: EM (single particle) / Resolution: 3.21 Å

17107

8oq7

EMDB-17107, PDB-8oq7:
CryoEM structure of human rho1 GABAA receptor in complex with inhibitor TPMPA
Method: EM (single particle) / Resolution: 2.2 Å

17108

8oq8

EMDB-17108, PDB-8oq8:
CryoEM structure of human rho1 GABAA receptor in complex with pore blocker picrotoxin
Method: EM (single particle) / Resolution: 2.9 Å

17110

8oqa

EMDB-17110, PDB-8oqa:
CryoEM structure of human rho1 GABAA receptor in complex with GABA and picrotoxin
Method: EM (single particle) / Resolution: 2.9 Å

Chemicals

ChemComp-ABU:
GAMMA-AMINO-BUTANOIC ACID / neurotransmitter, inhibitor*YM / Γ-Aminobutyric acid

ChemComp-NAG:
2-acetamido-2-deoxy-beta-D-glucopyranose / N-Acetylglucosamine

ChemComp-HEX:
HEXANE / Hexane

ChemComp-CL:
Unknown entry / Chloride

ChemComp-HOH:
WATER / Water

ChemComp-OCT:
N-OCTANE / Octane

ChemComp-D10:
DECANE / Decane

ChemComp-7P9:
[(2R)-2-heptanoyloxy-3-phosphonooxy-propyl] nonanoate

ChemComp-VZA:
methyl(1,2,3,6-tetrahydropyridin-4-yl)phosphinic acid

ChemComp-D12:
DODECANE / Dodecane

ChemComp-RI5:
(1aR,2aR,3S,6R,6aS,8aS,8bR,9R)-2a-hydroxy-8b-methyl-9-(prop-1-en-2-yl)hexahydro-3,6-methano-1,5,7-trioxacyclopenta[ij]c / toxin*YM / Picrotoxin

Source
  • homo sapiens (human)
KeywordsMEMBRANE PROTEIN / GABAA receptor / rho1

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