[HTML][HTML] Structure and dynamics of GPCRs in lipid membranes: physical principles and experimental approaches

AJY Jones, F Gabriel, A Tandale, D Nietlispach - Molecules, 2020 - mdpi.com
Over the past decade, the vast amount of information generated through structural and
biophysical studies of GPCRs has provided unprecedented mechanistic insight into the …

The role of NMR spectroscopy in mapping the conformational landscape of GPCRs

MJ Bostock, AS Solt, D Nietlispach - Current opinion in structural biology, 2019 - Elsevier
Highlights•Using multiple labelling strategies, NMR spectroscopy provides insights into the
dynamic nature of several class A GPCRs.•Receptors populate a range of states that are in …

Uncovering the intimate relationship between lipids, cholesterol and GPCR activation

J Oates, A Watts - Current opinion in structural biology, 2011 - Elsevier
The membrane bilayer has a significant influence over the proteins embedded within it. G
protein-coupled receptors (GPCRs) form a large group of membrane proteins with a vast …

Emerging structural biology of lipid G protein‐coupled receptors

M Audet, RC Stevens - Protein Science, 2019 - Wiley Online Library
The first crystal structure of a G protein‐coupled receptor (GPCR) was that of the bovine
rhodopsin, solved in 2000, and is a light receptor within retina rode cells that enables vision …

Function-related conformational dynamics of G protein–coupled receptors revealed by NMR

T Ueda, Y Kofuku, J Okude, S Imai, Y Shiraishi… - Biophysical …, 2019 - Springer
G protein–coupled receptors (GPCRs) function as receptors for various neurotransmitters,
hormones, cytokines, and metabolites. GPCR ligands impart differing degrees of signaling in …

How the dynamic properties and functional mechanisms of GPCRs are modulated by their coupling to the membrane environment

S Mondal, G Khelashvili, N Johner… - G Protein-Coupled …, 2014 - Springer
Experimental observations of the dependence of function and organization of G protein-
coupled receptors (GPCRs) on their lipid environment have stimulated new quantitative …

Allosteric binding sites at the receptor–lipid bilayer interface: novel targets for GPCR drug discovery

Y Wang, Z Yu, W Xiao, S Lu, J Zhang - Drug discovery today, 2021 - Elsevier
Highlights•Allosteric GPCR drug discovery is gaining increasing attention.•Lipid bilayer
plays a unique role in the allosteric sites of GPCRs.•The role of lipid bilayer in allosteric sites …

Molecular modeling and simulation of membrane lipid-mediated effects on GPCRs

SK Sadiq, R Guixa-Gonzalez, E Dainese… - Current Medicinal …, 2013 - ingentaconnect.com
Functioning of G protein-coupled receptors (GPCRs) is tightly linked to the membrane
environment, but a molecular level understanding of the modulation of GPCR by membrane …

[HTML][HTML] Recent advances in structure, function, and pharmacology of class A lipid GPCRs: opportunities and challenges for drug discovery

RNV Krishna Deepak, RK Verma, YD Hartono… - Pharmaceuticals, 2021 - mdpi.com
Great progress has been made over the past decade in understanding the structural,
functional, and pharmacological diversity of lipid GPCRs. From the first determination of the …

GPCRs: Lipid‐dependent membrane receptors that act as drug targets

A Chattopadhyay - Advances in Biology, 2014 - Wiley Online Library
G protein‐coupled receptors (GPCRs) are the largest class of molecules involved in signal
transduction across cell membranes and represent major targets in the development of …