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

Satita Tapaneeyakorn, Alan D. Goddard, Joanne Oates, Christine L. Willis, Anthony Watts*

*Corresponding author for this work

Research output: Contribution to journalReview article

Abstract

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.

Original languageEnglish
Pages (from-to)1462-1475
Number of pages14
JournalBBA -Biomembranes
Volume1808
Issue number6
Early online date15 Oct 2010
DOIs
Publication statusPublished - Jun 2011

Fingerprint

G-Protein-Coupled Receptors
Nuclear magnetic resonance
Ligands
Drug Discovery
Cell signaling
Isotope Labeling
Drug Design
Crystallization
X-Ray Diffraction
Isotopes
Pharmaceutical Preparations
Labeling
Nuclear magnetic resonance spectroscopy
Magnetic Resonance Spectroscopy
Research Personnel
Guidelines
Membranes
X ray diffraction
Proteins

Keywords

  • expression system
  • GPCR
  • protein-ligand interaction
  • sample environment
  • solid-state NMR
  • solution-state NMR

Cite this

Tapaneeyakorn, Satita ; Goddard, Alan D. ; Oates, Joanne ; Willis, Christine L. ; Watts, Anthony. / Solution- and solid-state NMR studies of GPCRs and their ligands. In: BBA -Biomembranes. 2011 ; Vol. 1808, No. 6. pp. 1462-1475.
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Tapaneeyakorn, S, Goddard, AD, Oates, J, Willis, CL & Watts, A 2011, 'Solution- and solid-state NMR studies of GPCRs and their ligands', BBA -Biomembranes, vol. 1808, no. 6, pp. 1462-1475. https://doi.org/10.1016/j.bbamem.2010.10.003

Solution- and solid-state NMR studies of GPCRs and their ligands. / Tapaneeyakorn, Satita; Goddard, Alan D.; Oates, Joanne; Willis, Christine L.; Watts, Anthony.

In: BBA -Biomembranes, Vol. 1808, No. 6, 06.2011, p. 1462-1475.

Research output: Contribution to journalReview article

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