Investigating the molecular mechanisms through which <scp>FTY</scp>720‐<scp>P</scp> causes persistent <scp>S1P₁</scp> receptor internalization

Abstract

FTY720-P and S1P activation of the S1P1R results in receptor internalization as a consequence of an efficient recruitment of β-arrestin. The combination of slow off-rate, efficacious β-arrestin recruitment and metabolic stability all contribute to FTY720-P's ability to promote prolonged S1P1R internalization and may be critical factors in its efficacy in the clinic.