Extended Data Fig. 8: The role of pocket 4 in TAAR1.
From: Ligand recognition and G-protein coupling of trace amine receptor TAAR1
a-h, Structural representations of the polar interaction network of the residues at position 2.61, 2.64, 3.32 and 7.43, for the hTAAR1 with SEP-363856 (a), T1AM (b), (S)-AMPH (c), RO-6889450 (d), fenoldopam (g) and A77636 (h), or mTAAR1 with SEP-363856 (e), T1AM (f), respectively. The estimated hydrogen bonds are represented with red dash lines. i, Representative curve for effects of the S802.61A, R832.64A and H993.28A mutations in hTAAR1 on ligands (fenoldopam, A77636, T1AM, SEP-363856) induced Gs signalling using CAMYEL assay. Data are presented as mean ± SEM of three independent experiments performed in triplicate. WT, wild type. j, Representative curve for effects of the S802.61A, R832.64A and H993.28A mutations in hTAAR1 on ligands (fenoldopam, A77636, T1AM, SEP-363856) binding using FlAsH-BRET assay. Data are presented as mean ± SEM of three independent experiments performed in triplicate.
