Fig. 5: Select mGlu2 PAMs mediate their effects on cis-activation of the mGlu2 protomer and have no effect on mGlu4 protomer activation within mGlu2/4 heterodimers.
From: Elucidating the molecular logic of a metabotropic glutamate receptor heterodimer
a Structures of the mGlu2 PAMs BINA and LY487379. b, c CODA-RET measurements with the mGlu2/4 heterodimer mutant described in Fig. 3d legend showing DCG IV-concentration-response curves in the absence (DMSO vehicle) or presence of 50 µM (b) BINA and (c) LY487379. d, e CODA-RET measurements with the mGlu2/4 heterodimer mutant described in Fig. 3g legend showing DCG IV-concentration-response curves in the absence (DMSO vehicle) or presence of 50 µM (d) BINA and (e) LY487379. For all plots, symbols represent the mean drug-induced BRET, error bars represent ± SEM, and the exact number of ‘n’ independent experiments and technical replicates are reported in Supplementary Table 1. Source data are provided as a Source Data file.
