Illustration from Scientific Research

P2Y 1 -R constitutive activity depends on receptor expression level. Increasing P2Y 1 -R expression switched the receptor equilibrium from an inactive R conformation to an active R* conformation, thereby promoting a constitutive activation of Gq protein signaling as well as constitutive recruitment of beta-arrestin 2, and precluding ADP-induced signaling. By contrast, decreasing P2Y 1 -R expression had an opposite effect, balancing the receptor equilibrium towards an inactive R state responding to agonist stimulation

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