ArticleMethods (San Diego, Calif.)2011
GPCR stabilization using the bicelle-like architecture of mixed sterol-detergent micelles.
Article in Methods (San Diego, Calif.), 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 50 papers.
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Who cites it
50 citing papers in PubMed, 95 citations in OpenAlex.
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- The Conformational Equilibria of a Human GPCR Compared between Lipid Vesicles and Aqueous Solutions by IntegrativeJournal of the American Chemical Society · 2025Article
- ABC transporter activity is affected by the size of lipid nanodiscs.FEBS letters · 2025Article
- Article
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- Overview of Membrane Protein Sample Preparation for Single-Particle Cryo-Electron Microscopy Analysis.International journal of molecular sciences · 2023Review
- Quantitative analysis of sterol-modulated monomer-dimer equilibrium of the βProceedings of the National Academy of Sciences of the United States of America · 2023Article
- Detergents and alternatives in cryo-EM studies of membrane proteins.Acta biochimica et biophysica Sinica · 2022Review
- Allosteric modulators enhance agonist efficacy by increasing the residence time of a GPCR in the active state.Nature communications · 2021Article
- Catalytically Cleavable Detergent for Membrane Protein Studies.ACS omega · 2021Article
- Detergent-free purification and reconstitution of functional human serotonin transporter (SERT) using diisobutylene maleic acid (DIBMA) copolymer.Biochimica et biophysica acta. Biomembranes · 2021Article
- Refolding and characterization of two G protein-coupled receptors purified from E. coli inclusion bodies.PloS one · 2021Article
- Structure and Dynamics of GPCRs in Lipid Membranes: Physical Principles and Experimental Approaches.Molecules (Basel, Switzerland) · 2020Review
- Thermostability of a recombinant G protein-coupled receptor expressed at high level in mammalian cell culture.Scientific reports · 2020Article
- Interfacial Binding Sites for Cholesterol on Kir, Kv, KBiophysical journal · 2020Article
- Crystal structure of the human oxytocin receptor.Science advances · 2020Article
- Interfacial Binding Sites for Cholesterol on TRP Ion Channels.Biophysical journal · 2019Article
- Chemical tools for membrane protein structural biology.Current opinion in structural biology · 2019Review
- Application of antihelix antibodies in protein structure determination.Proceedings of the National Academy of Sciences of the United States of America · 2019Article
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
The biophysical characterization of purified membrane proteins typically requires detergent mediated extraction from native lipid membrane environments. In the case of human G protein-coupled receptors (GPCRs), this process has been complicated by their conformational heterogeneity and the general lack of understanding the composition and interactions within the diverse human cellular membrane environment. Several successful GPCR structure determination efforts have shown that the addition of cholesterol analogs is often critical for maintaining protein stability. We have identified sterols that substantially increase the stability of the NOP receptor (ORL-1), a member of the opioid GPCR family, in a mixed micelle environment. Using dynamic light scattering and small-angle X-ray scattering, we have determined that the most thermal stabilizing sterol, cholesteryl hemisuccinate, induces the formation of a bicelle-like micelle architecture when mixed with dodecyl maltoside detergent. Together with mutagenesis studies and recent GPCR structures, our results provide indications that stabilization is attained through a combination of specific sterol binding to GPCRs and modulation of micelle morphology.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.