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PIP2 stabilises active states of GPCRs and enhances the selectivity

Abstract:

G protein-coupled receptors (GPCRs) are involved in many physiological processes and are therefore key drug targets 1. Despite detailed structural information however the effects of lipids on the receptors themselves, or on their downstream coupling to G proteins, are ill defined. Here we use native mass spectrometry to identify endogenous lipids bound to three class A GPCRs. We demonstrate preferential binding of phosphatidylinositol 4,5 bisphosphate (PIP2) over related lipids and confirm ho...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1038/s41586-018-0325-6

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Institution:
University of Oxford
Division:
MPLS Division
Department:
Chemistry; Physical & Theoretical Chem
More by this author
Institution:
University of Oxford
Division:
MPLS Division
Department:
Chemistry; Physical & Theoretical Chem
More by this author
Institution:
University of Oxford
Division:
MPLS Division
Department:
Chemistry; Physical & Theoretical Chem
More by this author
Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
Biochemistry
More by this author
Institution:
University of Oxford
Division:
Medical Sciences Division
Department:
Biochemistry
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Publisher:
Nature Publishing Group Publisher's website
Journal:
Nature Journal website
Volume:
559
Pages:
423–427
Publication date:
2018-07-11
Acceptance date:
2018-06-20
DOI:
EISSN:
1476-4687
ISSN:
0028-0836
Pubs id:
pubs:858720
URN:
uri:2786d7cb-eb6c-4862-975c-d68c56b7f282
UUID:
uuid:2786d7cb-eb6c-4862-975c-d68c56b7f282
Local pid:
pubs:858720

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