Dopamine Receptor D1 Agonism and Antagonism Using a Field-Effect Transistor Assay
- Authors
- Park, Seon Joo; Yang, Heehong; Lee, Seung Hwan; Song, Hyun Seok; Park, Chul Soon; Bae, Joonwon; Kwon, Oh Seok; Park, Tai Hyun; Jang, Jyongsik
- Issue Date
- Jun-2017
- Publisher
- AMER CHEMICAL SOC
- Keywords
- dopamine; dopamine receptor D1; agonists-antagonists; agonism-antagonism; field-effect transistor; nanohybrids; equilibrium constants
- Citation
- ACS NANO, v.11, no.6, pp.5950 - 5959
- Indexed
- SCIE
SCOPUS
- Journal Title
- ACS NANO
- Volume
- 11
- Number
- 6
- Start Page
- 5950
- End Page
- 5959
- URI
- https://scholarworks.bwise.kr/erica/handle/2021.sw.erica/9587
- DOI
- 10.1021/acsnano.7b01722
- ISSN
- 1936-0851
- 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.
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