In vitro expressed GPCR inserted in polymersome membranes for ligand-binding studies

Angew Chem Int Ed Engl. 2013 Jan 7;52(2):749-53. doi: 10.1002/anie.201204645. Epub 2012 Nov 19.

Abstract

The dopamine receptor D2 (DRD2), a G-protein coupled receptor is expressed into PBd(22)-PEO(13) and PMOXA(20)-PDMS(54)-PMOXA(20) block copolymer vesicles. 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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Drug Discovery
  • Humans
  • Ligands
  • Polymers / chemistry*
  • Polymers / metabolism*
  • Receptors, G-Protein-Coupled / chemistry*
  • Receptors, G-Protein-Coupled / metabolism*

Substances

  • Ligands
  • Polymers
  • Receptors, G-Protein-Coupled