Fig. 5: Different efficacies of orthosteric ligands on mGlu2 ECD rearrangement. | Nature Communications

Fig. 5: Different efficacies of orthosteric ligands on mGlu2 ECD rearrangement.

From: Allosteric modulators enhance agonist efficacy by increasing the residence time of a GPCR in the active state

Fig. 5

a–h FRET distributions were obtained in the presence of partial agonists LCCG-I (a) and DCG-IV (b) or full synthetic agonist LY379268 (g) alone or in the presence of BINA (c, d, h respectively) or Gi (e and f, respectively). i Comparison of the fraction of the active state (LF/(LF+HF)) in response to different orthosteric and allosteric ligands. n = 3 independent biological replicates examined over 3 independent experiments for each condition. The scatter plot shows data together with the mean± SD. Statistical differences were determined using a one-way ANOVA with Sidak multiple comparisons test and are given as: pLY35/Glu = 0.0068 (**), pGlu/LY37 = 0.0006 (***), pDCG-IV+BINA/Glu+BINA = 0.0028 (**), pGlu+BINA/LY37+BINA = 0.61 (ns). j Comparison of the fraction of all states in response to different orthosteric and allosteric ligands. Data represent the stacked means ± SD from 3 independent biological replicates for each state with error bars centered around the mean for the VLF, LF, HF, and VHF from top to bottom, respectively. Source data of panels a–j are provided as a source data file.

Back to article page