TRPV1 structures in nanodiscs reveal mechanisms of ligand and lipid action
TRPV1 structures in nanodiscs reveal mechanisms of ligand and lipid action
When integral membrane proteins are visualized in detergents or other artificial systems, an important layer of information is lost regarding lipid interactions and their effects on protein structure. This is especially relevant to proteins for which lipids have both structural and regulatory roles. Here we demonstrate the power of combining electron cryo-microscopy with lipid nanodisc technology to ascertain the structure of the rat TRPV1 ion channel in a native bilayer environment. Using this approach, we determined the locations of annular and regulatory lipids and showed that specific phospholipid interactions enhance binding of a spider toxin to TRPV1 through formation of a tripartite complex. Furthermore, phosphatidylinositol lipids occupy the binding site for capsaicin and other vanilloid ligands, suggesting a mechanism whereby chemical or thermal stimuli elicit channel activation by promoting the release of bioactive lipids from a critical allosteric regulatory site.
- University of California System United States
- Howard Hughes Medical Institute United States
- Howard Hughes Medical Institute University of Washington United States
- UNIVERSITY OF CALIFORNIA, SAN FRANCISCO
- University of California, San Francisco United States
Cryoelectron Microscopy, Lipid Bilayers, Molecular Sequence Data, Temperature, Membrane Proteins, Spider Venoms, TRPV Cation Channels, Ligands, Article, Nanostructures, Rats, Phosphatidylinositol Phosphates, Animals, Amino Acid Sequence, Capsaicin, Allosteric Site, Phospholipids
Cryoelectron Microscopy, Lipid Bilayers, Molecular Sequence Data, Temperature, Membrane Proteins, Spider Venoms, TRPV Cation Channels, Ligands, Article, Nanostructures, Rats, Phosphatidylinositol Phosphates, Animals, Amino Acid Sequence, Capsaicin, Allosteric Site, Phospholipids
11 Research products, page 1 of 2
- 2016IsSupplementTo
- 2016IsRelatedTo
- 2016IsSupplementTo
- 2016IsRelatedTo
- 2016IsSupplementTo
- 2016IsRelatedTo
- 2018IsRelatedTo
- IsSupplementTo
- IsSupplementTo
- 2017IsRelatedTo
chevron_left - 1
- 2
chevron_right
citations This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).745 popularity This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.Top 0.1% influence This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).Top 1% impulse This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.Top 0.01%
