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Dopamine receptor D1 agonism and antagonism using a field-effect transistor assay

Title
Dopamine receptor D1 agonism and antagonism using a field-effect transistor assay
Author
이승환
Keywords
dopamine; dopamine receptor D1; agonists-antagonists; agonism-antagonism; field-effect transistor; nanohybrids; equilibrium constants
Issue Date
2017-06
Publisher
AMER CHEMICAL SOC
Citation
ACS NANO, v. 11, no. 6, page. 5950-5959
Abstract
The field-effect transistor (FET) has been used in the development of diagnostic tools for several decades, leading to high-performance biosensors. Therefore, the FET platform can provide the foundation for the next generation of analytical methods. A major role of G-protein-coupled receptors (GPCRs) is in the transfer of external signals into the cell and promoting human body functions; thus, their principle application is in the screening of new drugs. The research community uses efficient systems to screen potential GPCR drugs; nevertheless, the need to develop GPCR-conjugated analytical devices remains for next-generation new drug screening. In this study, we proposed an approach for studying receptor agonism and antagonism by combining the roles of FETs and GPCRs in a dopamine receptor D1 (DRD1)-conjugated FET system, which is a suitable substitute for conventional cell-based receptor assays. DRD1 was reconstituted and purified to mimic native binding pockets that have highly discriminative interactions with DRD1 agonists/antagonists. The real-time responses from the DRD1-nanohybrid FET were highly sensitive and selective for dopamine agonists/antagonists, and their maximal response levels were clearly different depending on their DRD1 affinities. Moreover, the equilibrium constants (K) were estimated by fitting the response levels. Each K value indicates the variation in the affinity between DRD1 and the agonists/antagonists; a greater K value corresponds to a stronger DRD1 affinity in agonism, whereas a lower K value in antagonism indicates a stronger dopamine-blocking effect.
URI
https://pubs.acs.org/doi/10.1021/acsnano.7b01722https://repository.hanyang.ac.kr/handle/20.500.11754/114366
ISSN
1936-0851; 1936-086X
DOI
10.1021/acsnano.7b01722
Appears in Collections:
GRADUATE SCHOOL[S](대학원) > BIONANOTECHNOLOGY(바이오나노학과) > Articles
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