Featured
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Article |
GABAA receptor signalling mechanisms revealed by structural pharmacology
Cryo-electron microscopy structures are reported in which the full-length human α1β3γ2L GABAA receptor in lipid nanodiscs is bound to the channel-blocker picrotoxin, the competitive antagonist bicuculline, the agonist GABA, and the benzodiazepines alprazolam and diazepam.
- Simonas Masiulis
- , Rooma Desai
- & A. Radu Aricescu
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Letter |
Cryo-EM structure of the human α1β3γ2 GABAA receptor in a lipid bilayer
A high-resolution cryo-electron microscopy structure is reported for the full-length human α1β3γ2L GABAA receptor, functionally reconstituted in lipid nanodiscs.
- Duncan Laverty
- , Rooma Desai
- & A. Radu Aricescu
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Letter |
Cryo-EM reveals two distinct serotonin-bound conformations of full-length 5-HT3A receptor
Cryo-electron microscopy structures of the serotonin-bound 5-HT3A serotonin receptor show the receptor populating two distinct states, characterized by twisting in the extracellular and transmembrane domains relative to the apo state, which creates pathways for ion permeation.
- Sandip Basak
- , Yvonne Gicheru
- & Sudha Chakrapani
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Article |
Structure of a human synaptic GABAA receptor
The cryo-electron microscopy structure of the type A GABA receptor bound to GABA and the benzodiazepine site antagonist flumazenil reveals structural mechanisms that underlie intersubunit interactions and ligand selectivity of the receptor.
- Shaotong Zhu
- , Colleen M. Noviello
- & Ryan E. Hibbs
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Letter |
X-ray structure of the human α4β2 nicotinic receptor
Nicotinic acetylcholine receptors are ligand-gated ion channels that mediate fast chemical neurotransmission; here, the first X-ray crystal structure of a nicotinic receptor is reported, revealing how nicotine stabilizes the receptor in a non-conducting, desensitized conformation.
- Claudio L. Morales-Perez
- , Colleen M. Noviello
- & Ryan E. Hibbs
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Article |
Gating of the TrkH ion channel by its associated RCK protein TrkA
Here it is shown that ion flux through the TrkH–TrkA complex is upregulated by ATP and downregulated by ADP; solving the X-ray crystal structures of the tetrameric TrkA ring in the absence and presence of TrkH suggests a mechanism by which ATP-induced conformational changes in TrkA augment the activity of TrkH.
- Yu Cao
- , Yaping Pan
- & Ming Zhou
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Letter |
X-ray structures of general anaesthetics bound to a pentameric ligand-gated ion channel
The mechanism of action of general anaesthetics is poorly understood, although there is some evidence that their principal protein targets are pentameric ligand-gated ion channels (pLGICs). Here, the X-ray crystal structures of propofol and desflurane bound to a bacterial homologue of the pLGIC family are solved. The structures reveal a common binding site for these two anaesthetics in the upper part of the transmembrane domain of each protomer.
- Hugues Nury
- , Catherine Van Renterghem
- & Pierre-Jean Corringer
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News & Views |
Astrocytes as aide-mémoires
Memory formation is known to occur at the level of synaptic contacts between neurons. It therefore comes as a surprise that another type of brain cell, the astrocyte, is also involved in establishing memory.
- Mirko Santello
- & Andrea Volterra