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In vitro expressed GPCR inserted in polymersome membranes for ligand-binding studies
Sylvia May1, Mirjam Andreasson-Ochsner, Zhikang Fu
1Patterning and Fabrication, Institute of Materials Research and Engineering, Agency for Science, Technology and Research, Singapore, Singapore.
Angewandte Chemie (International Ed. in English)
|November 20, 2012
Summary
Dopamine receptor D2 (DRD2) was successfully integrated into block copolymer vesicles. This novel platform demonstrates dopamine replacement, showing promise for future drug screening applications.
Area of Science:
- Biochemistry
- Materials Science
- Pharmacology
Background:
- The dopamine receptor D2 (DRD2) is a crucial G-protein coupled receptor involved in various neurological processes.
- Block copolymer vesicles offer a versatile platform for biomimetic applications.
Purpose of the Study:
- To investigate the expression and functional integrity of DRD2 within block copolymer vesicles.
- To evaluate the potential of these polymersomes as a platform for drug screening.
Main Methods:
- DRD2 was expressed in PBd(22)-PEO(13) and PMOXA(20)-PDMS(54)-PMOXA(20) block copolymer vesicles.
- Antibody- and ligand-binding assays were employed to confirm the receptor's conformational integrity.
- Dopamine replacement assays were conducted on surface-immobilized polymersomes.
Main Results:
- Successful expression of functional DRD2 within the block copolymer vesicles was confirmed.
- The conformational integrity of the expressed DRD2 was validated through binding assays.
- Demonstration of dopamine replacement on surface-immobilized polymersomes.
Conclusions:
- Block copolymer vesicles can successfully incorporate and maintain the functional integrity of DRD2.
- Surface-immobilized polymersomes displaying DRD2 represent a promising platform for drug screening and development.
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