9f5o: Difference between revisions
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==CryoEM structure of open sTeLIC in detergent, with 4-Bromoamphetamine== | |||
<StructureSection load='9f5o' size='340' side='right'caption='[[9f5o]], [[Resolution|resolution]] 4.16Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[9f5o]] is a 5 chain structure with sequence from [https://en.wikipedia.org/wiki/Endosymbiont_of_Tevnia_jerichonana_(vent_Tica) Endosymbiont of Tevnia jerichonana (vent Tica)]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=9F5O OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=9F5O FirstGlance]. <br> | |||
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">Electron Microscopy, [[Resolution|Resolution]] 4.16Å</td></tr> | |||
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=9f5o FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=9f5o OCA], [https://pdbe.org/9f5o PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=9f5o RCSB], [https://www.ebi.ac.uk/pdbsum/9f5o PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=9f5o ProSAT]</span></td></tr> | |||
</table> | |||
== Function == | |||
[https://www.uniprot.org/uniprot/G2FID1_9GAMM G2FID1_9GAMM] | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
BACKGROUND AND PURPOSE: Allosteric modulation of pentameric ligand-gated ion channels (pLGICs) are critical for the action of neurotransmitters and many psychoactive drugs. However, details of their modulatory mechanisms remain unclear, especially beyond the orthosteric neurotransmitter-binding sites. The recently reported prokaryotic symbiont of Tevnia jerichonana ligand-gated ion channel (sTeLIC), a pH-gated homologue of eukaryotic receptors in the pLGIC family, is thought to be modulated by aromatic compounds via a relatively uncharacterised modulatory site in the extracellular vestibule. EXPERIMENTAL APPROACH: We have characterised the effects of psychostimulant derivatives on sTeLIC using two-electrode voltage-clamp electrophysiology in the presence and absence of engineered mutations, and determined X-ray and cryo-EM structures of the channel in both closed and open states. KEY RESULTS: We have shown that sTeLIC is sensitive to potentiation by several amphiphilic compounds, which preferentially bind to a vestibular pocket in the contracted open-state extracellular domain. CONCLUSIONS AND IMPLICATIONS: This work provides a detailed structure-function mechanism for allosteric potentiation via a noncanonical ligand site, with potential conservation of the eukaryotic pentameric ligand-gated ion channels. | |||
Vestibular modulation by stimulant derivatives in a pentameric ligand-gated ion channel.,Karlsson E, Anden O, Fan C, Fourati Z, Haouz A, Zhuang Y, Howard RJ, Delarue M, Lindahl E Br J Pharmacol. 2025 Mar 11. doi: 10.1111/bph.70011. PMID:40065647<ref>PMID:40065647</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
[[Category: | </div> | ||
[[Category: Anden | <div class="pdbe-citations 9f5o" style="background-color:#fffaf0;"></div> | ||
[[Category: Howard | == References == | ||
[[Category: Lindahl | <references/> | ||
__TOC__ | |||
</StructureSection> | |||
[[Category: Large Structures]] | |||
[[Category: Anden O]] | |||
[[Category: Howard RJ]] | |||
[[Category: Lindahl E]] | |||
Latest revision as of 21:46, 26 March 2025
CryoEM structure of open sTeLIC in detergent, with 4-Bromoamphetamine
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