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

Abstract:

:Over recent years, nuclear magnetic resonance (NMR) spectroscopy has developed into a powerful mechanistic tool for the investigation of G protein-coupled receptors (GPCRs). NMR provides insights which underpin the dynamic nature of these important receptors and reveals experimental evidence for a complex conformational energy landscape that is explored during receptor activation resulting in signalling. NMR studies have highlighted both the dynamic properties of different receptor states as well as the exchange pathways and intermediates formed during activation, extending the static view of GPCRs obtained from other techniques. NMR studies can be undertaken in realistic membrane-like phospholipid environments and an ever-increasing choice of labelling strategies provides comprehensive, receptor-wide information. Combined with other structural methods, NMR is contributing to our understanding of allosteric signal propagation and the interaction of GPCRs with intracellular binding partners (IBP), crucial to explaining cellular signalling.

journal_name

Curr Opin Struct Biol

authors

Bostock MJ,Solt AS,Nietlispach D

doi

10.1016/j.sbi.2019.03.030

subject

Has Abstract

pub_date

2019-08-01 00:00:00

pages

145-156

eissn

0959-440X

issn

1879-033X

pii

S0959-440X(19)30028-4

journal_volume

57

pub_type

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