ArticleBiochemistry2011
Direct measurement of thermal stability of expressed CCR5 and stabilization by small molecule ligands.
Article in Biochemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
20 citing papers in PubMed, 43 citations in OpenAlex.
- Bioorthogonal Tethering Enhances Drug Fragment Affinity for G Protein-Coupled Receptors in Live Cells.Journal of the American Chemical Society · 2023Article
- Genetic code expansion to enable site-specific bioorthogonal labeling of functional G protein-coupled receptors in live cells.Protein science : a publication of the Protein Society · 2023Article
- FRET sensors reveal the retinal entry pathway in the G protein-coupled receptor rhodopsin.iScience · 2022Article
- Epitope Binning of Novel Monoclonal Anti F1 and Anti LcrV Antibodies and Their Application in a Simple, Short, HTRF Test for Clinical Plague Detection.Pathogens (Basel, Switzerland) · 2021Article
- Cryo-EM structure of an activated GPCR-G protein complex in lipid nanodiscs.Nature structural & molecular biology · 2021Article
- QTY code designed thermostable and water-soluble chimeric chemokine receptors with tunable ligand affinity.Proceedings of the National Academy of Sciences of the United States of America · 2019Article
- High-Affinity Binding of Chemokine Analogs that Display Ligand Bias at the HIV-1 Coreceptor CCR5.Biophysical journal · 2019Article
- Article
- Real time monitoring of membrane GPCR reconstitution by plasmon waveguide resonance: on the role of lipids.Scientific reports · 2016Article
- Cell-free translation and purification of Arabidopsis thaliana regulator of G signaling 1 protein.Protein expression and purification · 2016Article
- Micelle-Enhanced Bioorthogonal Labeling of Genetically Encoded Azido Groups on the Lipid-Embedded Surface of a GPCR.Chembiochem : a European journal of chemical biology · 2015Article
- Multiplex detection of functional G protein-coupled receptors harboring site-specifically modified unnatural amino acids.Biochemistry · 2015Article
- Stabilization of G protein-coupled receptors by point mutations.Frontiers in pharmacology · 2015Review
- Bioorthogonal fluorescent labeling of functional G-protein-coupled receptors.Chembiochem : a European journal of chemical biology · 2014Article
- Rapid homogenous time-resolved fluorescence (HTRF) immunoassay for anthrax detection.Journal of fluorescence · 2014Article
- Calcium-dependent ligand binding and G-protein signaling of family B GPCR parathyroid hormone 1 receptor purified in nanodiscs.ACS chemical biology · 2013Article
- Nanodiscs as a new tool to examine lipid-protein interactions.Methods in molecular biology (Clifton, N.J.) · 2013Review
- Homogeneous time-resolved fluorescence assay to probe folded G protein-coupled receptors.Methods in enzymology · 2013Article
- Modulation of the interaction between neurotensin receptor NTS1 and Gq protein by lipid.Journal of molecular biology · 2012Article
- Escaping the flatlands: new approaches for studying the dynamic assembly and activation of GPCR signaling complexes.Trends in pharmacological sciences · 2011Review
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
The inherent instability of heptahelical G protein-coupled receptors (GPCRs) during purification and reconstitution is a primary impediment to biophysical studies and to obtaining high-resolution crystal structures. New approaches to stabilizing receptors during purification and screening reconstitution procedures are needed. Here we report the development of a novel homogeneous time-resolved fluorescence assay (HTRF) to quantify properly folded CC-chemokine receptor 5 (CCR5). The assay permits high-throughput thermal stability measurements of femtomole quantities of CCR5 in detergent and in engineered nanoscale apolipoprotein-bound bilayer (NABB) particles. We show that recombinantly expressed CCR5 can be incorporated into NABB particles in high yield, resulting in greater thermal stability compared with that of CCR5 in a detergent solution. We also demonstrate that binding of CCR5 to the HIV-1 cellular entry inhibitors maraviroc, AD101, CMPD 167, and vicriviroc dramatically increases receptor stability. The HTRF assay technology reported here is applicable to other membrane proteins and could greatly facilitate structural studies of GPCRs.
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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.