Cited by 229Neuroscience and Neuropharmacology ResearchAnesthesia and Sedative AgentsNicotinic Acetylcholine Receptors Study

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A propofol binding site on mammalian GABAA receptors identified by photolabeling

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Yip, Grace M S, Chen, Zi-Wei, Edge, Christopher J, Smith, Edward H, Dickinson, Robert, Hohenester, Erhard, Townsend, R Reid, Fuchs, Karoline, Sieghart, Werner, Evers, Alex S, Franks, Nicholas P·2013·Nature Chemical Biology

DOI 10.1038/nchembio.1340PMC PMC3951778

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Abstract

Propofol is the most important intravenous general anesthetic in current clinical use. It acts by potentiating GABAA (γ-aminobutyric acid type A) receptors, but where it binds to this receptor is not known and has been a matter of some debate. We synthesized a new propofol analog photolabeling reagent whose biological activity is very similar to that of propofol. We confirmed that this reagent labeled known propofol binding sites in human serum albumin that have been identified using X-ray crystallography. Using a combination of protiated and deuterated versions of the reagent to label mammalian receptors in intact membranes, we identified a new binding site for propofol in GABAA receptors consisting of both β3 homopentamers and α1β3 heteropentamers. The binding site is located within the β subunit at the interface between the transmembrane domains and the extracellular domain and lies close to known determinants of anesthetic sensitivity in the transmembrane segments TM1 and TM2.

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Authors: Yip, G. M. S., Chen, Z.-W., Edge, C. J., Smith, E. H., Dickinson, R., Hohenester, E., Townsend, R. R., Fuchs, K., Sieghart, W., Evers, A. S., & Franks, N. P.
Affiliations: Imperial College London (GB)
Washington University in St. Louis (US)
Royal Berkshire Hospital (GB)
Medical University of Vienna (AT)
Corresponding author: Evers, Alex S
Franks, Nicholas P
ORCID: Chen, Zi-Wei
Smith, Edward H
Dickinson, Robert
Hohenester, Erhard
Townsend, R Reid
Sieghart, Werner
Evers, Alex S
Franks, Nicholas P
Venue: Nature Chemical Biology
Publisher: Springer Science and Business Media LLC
Published: 2013-09-22
Volume: 9
Issue: 11
Pages: 715-720
ISSN: 1552-4450 (ISSN-L)
1552-4469
DOI: 10.1038/nchembio.1340
PMC: PMC3951778
OpenAlex: W1972473633
Cited by: 226
References: 40
Citations by year: 2026: 7 · 2025: 6 · 2024: 9 · 2023: 7 · 2022: 12 · 2021: 19 · 2020: 19 · 2019: 21 · 2018: 30 · 2017: 20 · 2016: 31 · 2015: 18 · 2014: 22 · 2013: 5
FWCI: 12.43
Type: journal article
Language: en
Open access: green
europepmc.org
Licence: www.springer.com/tdm (tdm)
Locations: Nature Chemical Biology (publishedVersion)
PubMed (publishedVersion)
Europe PMC (PubMed Central) (acceptedVersion)
PubMed Central (acceptedVersion)
Spiral (Imperial College London) (submittedVersion)
Funders: National Institutes of Health (5p41rr000954-34)
National Institute of General Medical Sciences (P01GM047969, P01GM47969, P41GM103422)
National Center for Research Resources (P41-RR000954, UL1RR024992)
Topics: Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
Health Sciences › Medicine › Anesthesiology and Pain Medicine › Anesthesia and Sedative Agents
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Nicotinic Acetylcholine Receptors Study
Keywords: propofol, GABAA receptor, anesthetic binding sites, beta subunit, transmembrane domain, extracellular domain, anesthetic sensitivity, general anesthetics, human serum albumin
MeSH terms: Binding Sites, Humans, Models, Molecular, Receptors, GABA-A, Serum Albumin, Structure-Activity Relationship, Molecular Structure, Propofol, Photoaffinity Labels

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A propofol binding site on mammalian GABAA receptors identified by photolabeling

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