Journal
FRONTIERS IN PHARMACOLOGY
Volume 6, Issue -, Pages -Publisher
FRONTIERS MEDIA SA
DOI: 10.3389/fphar.2015.00066
Keywords
G protein-coupled receptor (GPCR); expression; purification; protein engineering; isotope labeling
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Funding
- Marie Curie Intra-European Fellowship [PIEF-GA-2010-274497]
- UBS Promedica foundation Fellowship [GHDE KXQ7-DZZ]
- Swiss National Science Foundation grants Sinergia [141898, 133810, 31-135754]
- NCCR Structural Biology and NCCR Molecular Systems Engineering
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Structural studies of G protein-coupled receptors (GPCRs) gave insights into molecular mechanisms of their action and contributed significantly to molecular pharmacology. This is primarily due to technical advances in protein engineering, production and crystallization of these important receptor targets. On the other hand, NMR spectroscopy of GPCRs, which can provide information about their dynamics, still remains challenging due to difficulties in preparation of isotopically labeled receptors and their low long-term stabilities. In this review, we discuss methods used for expression and purification of GPCRs for crystallographic and NMR studies. We also summarize protein engineering methods that played a crucial role in obtaining GPCR crystal structures.
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