Extended Data Fig. 9: Gq protein and arrestin signaling of NTSR1 potentiated by NTS and SBI-553. | Nature

Extended Data Fig. 9: Gq protein and arrestin signaling of NTSR1 potentiated by NTS and SBI-553.

From: GPCR activation and GRK2 assembly by a biased intracellular agonist

Extended Data Fig. 9

NTS is a balanced agonist, which binds to orthosteric site and promotes NTSR1 to mediate both G protein and arrestin signaling. SBI-553 is an arresin-biased allosteric modulator, which binds to the intracellular site and promotes GRK2 binding and arrestin signaling, but blocks Gq protein binding and signaling (red circled star). ++ marks indicate membrane binding.

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