Structure and Dynamics of GPCRs in Lipid Membranes: Physical Principles and Experimental Approaches

Over the past decade, the vast amount of information generated through structural and biophysical studies of GPCRs has provided unprecedented mechanistic insight into the complex signalling behaviour of these receptors. With this recent information surge, it has also become increasingly apparent tha...

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2020-10, Vol.25 (20), p.4729
Main Authors: Jones, Andrew J Y, Gabriel, Florian, Tandale, Aditi, Nietlispach, Daniel
Format: Article
Language:English
Subjects:
Allosteric properties
Biomimetics
GPCR
Humans
Hydrocarbons
Lipid bilayers
Lipid Bilayers - chemistry
Lipid membranes
Lipids
Magnetic Resonance Spectroscopy
Membrane Lipids - chemistry
membrane mimetics
Membranes
Molecular Structure
NMR
Physical Phenomena
Receptor mechanisms
Receptors, G-Protein-Coupled - chemistry
Receptors, G-Protein-Coupled - ultrastructure
Review
Signal Transduction
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Summary:Over the past decade, the vast amount of information generated through structural and biophysical studies of GPCRs has provided unprecedented mechanistic insight into the complex signalling behaviour of these receptors. With this recent information surge, it has also become increasingly apparent that in order to reproduce the various effects that lipids and membranes exert on the biological function for these allosteric receptors, in vitro studies of GPCRs need to be conducted under conditions that adequately approximate the native lipid bilayer environment. In the first part of this review, we assess some of the more general effects that a membrane environment exerts on lipid bilayer-embedded proteins such as GPCRs. This is then followed by the consideration of more specific effects, including stoichiometric interactions with specific lipid subtypes. In the final section, we survey a range of different membrane mimetics that are currently used for in vitro studies, with a focus on NMR applications.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules25204729