| 초록 |
We firstly proposed a new approach for studying receptor agonism and antagonism by combining the FET and GPCR roles in a dopamine receptor D1 (DRD1)-conjugated FET system, which is a suitable substitute for conventional cell-based receptor assays. DRD1, for the first time, was reconstituted and purified to mimic native binding pockets that have highly discriminative interaction toward 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 indicated the variation in the affinity between DRD1 and the agonists/antagonists: greater K value corresponds to a stronger DRD1 affinity in agonism, whereas a lower K value in antagonism indicates a stronger DA-blocking effect. |
