ArticleACS chemical biology2013
Calcium-dependent ligand binding and G-protein signaling of family B GPCR parathyroid hormone 1 receptor purified in nanodiscs.
Article in ACS chemical biology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 39 citations in OpenAlex.
- A novel mechanism for short-term post-tetanic plasticity in thalamocortical neurons.Brain research · 2025Article
- Design of an effective small expression tag to enhance GPCR production in E. coli-based cell-free and whole cell expression systems.Protein science : a publication of the Protein Society · 2023Article
- Accessible and Generalizable in Vitro Luminescence Assay for Detecting GPCR Activation.ACS measurement science au · 2023Article
- Proteolytic Cleavage of the Extracellular Domain Affects Signaling of Parathyroid Hormone 1 Receptor.Frontiers in endocrinology · 2022Article
- The Effects of Sodium Ions on Ligand Binding and Conformational States of G Protein-Coupled Receptors-Insights from Mass Spectrometry.Journal of the American Chemical Society · 2021Article
- Lipid nanoparticle technologies for the study of G protein-coupled receptors in lipid environments.Biophysical reviews · 2020Review
- Activation Microswitches in Adenosine Receptor ABiochemistry · 2020Article
- CaProceedings of the National Academy of Sciences of the United States of America · 2019Article
- GPCR drug discovery: integrating solution NMR data with crystal and cryo-EM structures.Nature reviews. Drug discovery · 2019Review
- Parathyroid Hormone Senses Extracellular Calcium To Modulate Endocrine Signaling upon Binding to the Family B GPCR Parathyroid Hormone 1 Receptor.ACS chemical biology · 2018Article
- Protein Sequence and Membrane Lipid Roles in the Activation Kinetics of Bovine and Human Rhodopsins.Biophysical journal · 2017Article
- Activation mechanism of a neuromodulator-gated pacemaker ionic current.Journal of neurophysiology · 2017Article
- Nanodiscs in Membrane Biochemistry and Biophysics.Chemical reviews · 2017Review
- In Situ Reconstitution of the Adenosine AJournal of the American Chemical Society · 2017Article
- Purification of family B G protein-coupled receptors using nanodiscs: Application to human glucagon-like peptide-1 receptor.PloS one · 2017Article
- Article
- Controlled Co-reconstitution of Multiple Membrane Proteins in Lipid Bilayer Nanodiscs Using DNA as a Scaffold.ACS chemical biology · 2015Article
- Tuning the Photocycle Kinetics of Bacteriorhodopsin in Lipid Nanodiscs.Biophysical journal · 2015Article
- G-protein coupled receptor solubilization and purification for biophysical analysis and functional studies, in the total absence of detergent.Bioscience reports · 2015Article
- Transmembrane signal transduction by peptide hormones via family B G protein-coupled receptors.Frontiers in pharmacology · 2015Review
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Authors and funding
8 authors at 2 institutions in 1 country.
Funding
Abstract
GPCRs mediate intracellular signaling upon external stimuli, making them ideal drug targets. However, little is known about their activation mechanisms due to the difficulty in purification. Here, we introduce a method to purify GPCRs in nanodiscs, which incorporates GPCRs into lipid bilayers immediately after membrane solubilization, followed by single-step purification. Using this approach, we purified a family B GPCR, parathyroid hormone 1 receptor (PTH1R), which regulates calcium and phosphate homeostasis and is a drug target for osteoporosis. We demonstrated that the purified PTH1R in nanodiscs can bind to PTH(1-34) and activate G protein. We also observed that Ca(2+) is a weak agonist of PTH1R, and Ca(2+) in millimolar concentration can switch PTH(1-34) from an inverse agonist to an agonist. Hence, our results show that nanodiscs are a viable vehicle for GPCR purification, enabling studies of GPCRs under precise experimental conditions without interference from other cellular or membrane components.
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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.