In Vitro Expressed GPCR Inserted in Polymersome Membranes for Ligand-Binding Studies

In Vitro Expressed GPCR Inserted in Polymersome Membranes for Ligand-Binding Studies

The dopamine receptor D2 (DRD2), a G‐protein coupled receptor is expressed into PBd22‐PEO13 and PMOXA20‐PDMS54‐PMOXA20 block copolymer vesicles (see scheme). The conformational integrity of the receptor is confirmed by antibody‐ and ligand‐binding assays. Replacement of bound dopamine is demonstrate...

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Veröffentlicht in:Angewandte Chemie International Edition 2013-01, Vol.52 (2), p.749-753
Hauptverfasser: May, Sylvia, Andreasson-Ochsner, Mirjam, Fu, Zhikang, Low , Ying Xiu, Tan, Darren, de Hoog, Hans-Peter M., Ritz, Sandra, Nallani, Madhavan, Sinner, Eva-Kathrin
Format: Artikel
Sprache:eng
Schlagworte:
biosensors
Block copolymers
Dopamine
Drug Discovery
Humans
Integrity
Joining
Ligands
Platforms
polymers
Polymers - chemistry
Polymers - metabolism
protein expression
Receptors
Receptors, G-Protein-Coupled - chemistry
Receptors, G-Protein-Coupled - metabolism
Screening
Vesicles
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Zusammenfassung:The dopamine receptor D2 (DRD2), a G‐protein coupled receptor is expressed into PBd22‐PEO13 and PMOXA20‐PDMS54‐PMOXA20 block copolymer vesicles (see scheme). The conformational integrity of the receptor is confirmed by antibody‐ and ligand‐binding assays. Replacement of bound dopamine is demonstrated on surface‐immobilized polymersomes, thus making this a promising platform for drug screening.
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.201204645