2005
DOI: 10.1073/pnas.0507599102
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Pore conformations and gating mechanism of a Cys-loop receptor

Abstract: ion channel ͉ membrane protein ͉ structure ͉ acetylcholine

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Cited by 68 publications
(89 citation statements)
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“…The up and outward motion of the N terminus of the M2 helix widens the channel pore, leading to channel opening. This type of tilting motion is precisely what is implicated by recent experimental data for channel opening (11,12).…”
Section: Structural Validation Of the Lbd-toxin Complex By Mutation Ementioning
confidence: 66%
See 1 more Smart Citation
“…The up and outward motion of the N terminus of the M2 helix widens the channel pore, leading to channel opening. This type of tilting motion is precisely what is implicated by recent experimental data for channel opening (11,12).…”
Section: Structural Validation Of the Lbd-toxin Complex By Mutation Ementioning
confidence: 66%
“…allostery ͉ spontaneous opening ͉ ligand-gated ion channel ͉ ligand binding N icotinic AChRs (nAChRs) are a well studied prototype for ligand-gated ion channels (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15)(16)(17)(18)(19). nAChRs are pentamers consisting of either homo or hetero subunits.…”
mentioning
confidence: 99%
“…Paas and colleagues probed the conformation of the ion pore with a histidine scan measuring state-dependent Zn 2+ -channel interactions in a chimeric α7-5HT 3A receptor [68] . With their experiments they propose a constriction at the intracellular end of the ion pore in the resting state, similar to the conformation concluded by Wilson and Karlin, which was described as an 'inverted teepee'.…”
Section: Location Of the Gate And Opening Movementsmentioning
confidence: 99%
“…These considerations imply that the outer part of M2 should be an informative place to investigate the structural basis of receptor activation, as the movements in this region should not reflect either those occurring at the ligand binding site or the activation gate. Thus, in this study we probe conformational changes at the 19Ј and 22Ј residues, near the external end of M2.Current models of Cys loop receptor activation consider only structural changes associated with transitions from the resting closed state to the agonist-induced open state (5,6,12,13). Relatively little attention has been given to the possibility that different agonists and pharmacological modulators may promote different structural conformations in the pore region.…”
mentioning
confidence: 99%
“…Current models of Cys loop receptor activation consider only structural changes associated with transitions from the resting closed state to the agonist-induced open state (5,6,12,13). Relatively little attention has been given to the possibility that different agonists and pharmacological modulators may promote different structural conformations in the pore region.…”
mentioning
confidence: 99%