Fig. 3: Comparison between inactive and active BLT1 structures.
From: Structural basis of leukotriene B4 receptor 1 activation
a An overall comparison of LTB4-bound (cyan), MK-D-046-bound (brown) and BIIL260-bound (magenta) BLT1. A 5.7 Å outward displacement (dash arrow) of TM6 was measured by the Cα of R2216.35. b A detailed comparison of polar interaction between the LTB4-bound and the MK-D-046-bound receptor (PDB:7k15). c A detailed comparison of polar interaction between the LTB4-bound and the BIIL260-bound receptor (PDB:5×33). d The displacements of key residues that block the entry of water or ion molecules into the lower part of ligand binding pocket upon agonist LTB4 binding. e A SRE reporter assay of key mutants that lock receptor in the inactive conformation. LTB4, 300 nM; data are presented as mean values ± SD; n = 3 independent samples; n.s. no significant; *p < 0.05; **p < 0.01; ***p < 0.001. The exact p value for S104K, S277K, S104K/S277K are 0.0001, 0.0007, 0.0001, respectively. T-test, two tailed, sample equal variance.
