GPR55, GPR75, MRGPRB2, and other orphan or understudied 7-Transmembrane (7TM) receptors represent the "frontier" of novel drug discovery. They play crucial roles in key physiological and pathological processes such as neurobiology, metabolism, and immunity, offering vast untapped therapeutic potential.
Figure 1. Dose Response of Doxycycline in Inducible GPR75 β-Arrestin CHO-K1(C1)
Doxycycline induced a dose-dependent receptor expression response with EC50 = 0.028 μM. The data confirms the inducible system works well, suitable for GPR75 target pharmacological research and compound screening.
Figure 2. Inhibition of Doxycycline (60 nM) induced β-Arrestin Recruitment by β-Arrestin inhibitor in Inducible GPR75 β-Arrestin CHO(C1)
In Inducible GPR75 β-Arrestin CHO-K1 (C1) cells, β-arrestin inhibitor Oridonin dose-dependently inhibits β-arrestin recruitment induced by 60 nM Doxycycline, with IC50 = 5.56 μM. The data confirms the cell line can be used for antagonist and inhibitor screening targeting GPR75.
