2009
DOI: 10.1038/aps.2009.51
|View full text |Cite
|
Sign up to set email alerts
|

Allosteric activation mechanism of the cys-loop receptors

Abstract: Binding of a neurotransmitter to its ionotropic receptor opens a distantly located ion channel, a process termed allosteric activation. Here we review recent advances in the molecular mechanism by which the cys-loop receptors are activated with emphasis on the best studied nicotinic acetylcholine receptors (nAChRs). With a combination of affinity labeling, mutagenesis, electrophysiology, kinetic modeling, electron microscopy (EM), and crystal structure analysis, the allosteric activation mechanism is emerging.… Show more

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...
1
1
1
1

Citation Types

2
25
0

Year Published

2011
2011
2023
2023

Publication Types

Select...
7
1

Relationship

0
8

Authors

Journals

citations
Cited by 25 publications
(27 citation statements)
references
References 73 publications
2
25
0
Order By: Relevance
“…Previous studies have demonstrated that several interactions between pairs of oppositely charged residues exist throughout this signaling pathway and that these interactions mediate the channel gating information flow (16,17). However, the results presented here imply that proper residue interaction also affects surface expression.…”
Section: Mutations Of Charged Residues In the Transition Zone Blockmentioning
confidence: 47%
See 1 more Smart Citation
“…Previous studies have demonstrated that several interactions between pairs of oppositely charged residues exist throughout this signaling pathway and that these interactions mediate the channel gating information flow (16,17). However, the results presented here imply that proper residue interaction also affects surface expression.…”
Section: Mutations Of Charged Residues In the Transition Zone Blockmentioning
confidence: 47%
“…A large body of studies has demonstrated that networks of energetic interactions between residues, especially between charged residues, exist throughout the transition zone (16,17). These residue interactions have been shown to be essential for the transmission of agonist-induced conformational changes to the channel gate.…”
mentioning
confidence: 99%
“…Serotonin is observed to dock into a more polar region than the setron compounds which is as expected given their greater degree of lipophilicity. A strong site of interaction correlates well with the position of the aromatic ring and alkyl chain of docked [6]-gingerol).…”
Section: Serotonin Binding Site Resultsmentioning
confidence: 75%
“…[5] The cationic 5-HT3 receptor belongs to the CYS loop superfamily of ligand-gated ion channels (LGICs) along with nicotinic acetylcholine receptors (nAchR) and anionic g-aminobutyric acid receptor (GABAA and GABAC) and glycine receptor. [6] The function of 5-HT3 receptors is intricately fine-tuned by the binding of other molecules and ions in and adjacent to the channel, either extracellularly or within the membrane region. For example, all CYS-loop receptors are allosterically regulated by zinc ions binding at multiple locations.…”
Section: Introductionmentioning
confidence: 99%
“…Irrespective of their location, the main function of neurotransmitter-gated ion channels is to rapidly transmit the binding "signal" to the ion channel, opening the gate and permitting ion flux (Lester et al 2004;Bartos et al 2009;Cederholm et al 2009;Chang et al 2009;Miller and Smart 2010). Our understanding as to how the receptor's underlying molecular machinery is structurally and functionally configured to achieve this rapid response is constantly evolving.…”
Section: Anchoring Cys-loop Receptors: Receptor-associated Molecules mentioning
confidence: 99%