Fig. 5: Activation mechanism of CysLT2R.
From: Molecular insights into ago-allosteric modulation at cysteinyl leukotriene receptor 2
Conformational differences of important residues and motifs in CysLT2R activation, including residues in ICL2 (a), TM5 and TM6 (b) and NPxxY motif in TM7 (c). The steric clash between inactive CysLT2R and Gq protein is indicated by blue stars. The movement from inactive state to active state is highlighted with red arrows. d Effects of mutations in key residues involved in CysLT2R activation by LTC4. The pEC50 and Emax values are provided in Supplementary Table 2. Data from three independent experiments are presented as the mean ± s.e.m. (n = 3). Source data are provided in the Source Data file. e Distinct activation propagation paths by ceramide and CysLTs. The orthosteric and allosteric propagation paths are shown by pink and green arrows, respectively. The conformational changes of key residues and the outward movement of TM6 are highlighted with red arrows.
