GPCR drug discovery: integrating solution NMR data with crystal and cryo-EM structures

GPCR drug discovery: integrating solution NMR data with crystal and cryo-EM structures

GPCR drug discovery: integrating solution NMR data with crystal and cryo-EM structures, Published online: 09 November 2018; doi:10.1038/nrd.2018.180

Determination of the crystal structures of more than 50 human G protein-coupled receptors (GPCRs) during the past decade has provided a platform for structure-based drug design for this key target class, which is being augmented with cryo-electron microscopy (cryo-EM) structures and nuclear magnetic resonance (NMR) spectroscopy studies of dynamic features. This Review describes the application of NMR techniques to GPCRs and projects where crystal and/or cryo-EM structures have been complemented with NMR studies and discusses the impact of this integrative approach on GPCR biology and drug discovery.

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