Solution- and solid-state NMR studies of GPCRs and their ligands.

G protein-coupled receptors (GPCRs) represent one of the major targets of new drugs on the market given their roles as key membrane receptors in many cellular signalling pathways. Structure-based drug design has potential to be the most reliable method for novel drug discovery. Unfortunately, GPCR-l...

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Main Authors: Tapaneeyakorn, S, Goddard, A, Oates, J, Willis, C, Watts, A
Formato: Journal article
Idioma:English
Publicado: 2011
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author Tapaneeyakorn, S
Goddard, A
Oates, J
Willis, C
Watts, A
author_facet Tapaneeyakorn, S
Goddard, A
Oates, J
Willis, C
Watts, A
author_sort Tapaneeyakorn, S
collection OXFORD
description G protein-coupled receptors (GPCRs) represent one of the major targets of new drugs on the market given their roles as key membrane receptors in many cellular signalling pathways. Structure-based drug design has potential to be the most reliable method for novel drug discovery. Unfortunately, GPCR-ligand crystallisation for X-ray diffraction studies is very difficult to achieve. However, solution- and solid-state NMR approaches have been developed and have provided new insights, particularly focussing on the study of protein-ligand interactions which are vital for drug discovery. This review provides an introduction for new investigators of GPCRs/ligand interactions using NMR spectroscopy. The guidelines for choosing a system for efficient isotope labelling of GPCRs and their ligands for NMR studies will be presented, along with an overview of the different sample environments suitable for generation of high resolution structural information from NMR spectra.
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spelling oxford-uuid:c95c46e0-d6ca-455f-b75c-e76d29677bd62022-03-27T06:58:37ZSolution- and solid-state NMR studies of GPCRs and their ligands.Journal articlehttp://purl.org/coar/resource_type/c_dcae04bcuuid:c95c46e0-d6ca-455f-b75c-e76d29677bd6EnglishSymplectic Elements at Oxford2011Tapaneeyakorn, SGoddard, AOates, JWillis, CWatts, AG protein-coupled receptors (GPCRs) represent one of the major targets of new drugs on the market given their roles as key membrane receptors in many cellular signalling pathways. Structure-based drug design has potential to be the most reliable method for novel drug discovery. Unfortunately, GPCR-ligand crystallisation for X-ray diffraction studies is very difficult to achieve. However, solution- and solid-state NMR approaches have been developed and have provided new insights, particularly focussing on the study of protein-ligand interactions which are vital for drug discovery. This review provides an introduction for new investigators of GPCRs/ligand interactions using NMR spectroscopy. The guidelines for choosing a system for efficient isotope labelling of GPCRs and their ligands for NMR studies will be presented, along with an overview of the different sample environments suitable for generation of high resolution structural information from NMR spectra.
spellingShingle Tapaneeyakorn, S
Goddard, A
Oates, J
Willis, C
Watts, A
Solution- and solid-state NMR studies of GPCRs and their ligands.
title Solution- and solid-state NMR studies of GPCRs and their ligands.
title_full Solution- and solid-state NMR studies of GPCRs and their ligands.
title_fullStr Solution- and solid-state NMR studies of GPCRs and their ligands.
title_full_unstemmed Solution- and solid-state NMR studies of GPCRs and their ligands.
title_short Solution- and solid-state NMR studies of GPCRs and their ligands.
title_sort solution and solid state nmr studies of gpcrs and their ligands
work_keys_str_mv AT tapaneeyakorns solutionandsolidstatenmrstudiesofgpcrsandtheirligands
AT goddarda solutionandsolidstatenmrstudiesofgpcrsandtheirligands
AT oatesj solutionandsolidstatenmrstudiesofgpcrsandtheirligands
AT willisc solutionandsolidstatenmrstudiesofgpcrsandtheirligands
AT wattsa solutionandsolidstatenmrstudiesofgpcrsandtheirligands