Fig. 1: Lack of G-protein activation upon stimulation of CXCR7.
From: Molecular insights into intrinsic transducer-coupling bias in the CXCR4-CXCR7 system
a CXCL12, a CXC type chemokine, is a common agonist for both, CXCR4 and CXCR7 (created with BioRender.com). b NanoBiT-based assay for CXCL12-induced dissociation of heterotrimeric G-proteins for CXCR4 and CXCR7 (mean ± SEM; n = 4-5 independent experiments; i.e., for Gi1 dissociation: Mock, n = 4; CXCR4, n = 5; CXCR7, n = 4; for Gi2 and Gi3 dissociation: n = 5; for Go dissociation: Mock, n = 4; CXCR4, n = 5; CXCR7, n = 5; for Gs, Gq, G12, and G13 dissociation: n = 4; normalized with luminescence signal under unstimulated condition taken as 1). Mock represents empty vector transfected cells as a negative control. c VUF11207 is a small molecule agonist for CXCR7 but its efficacy for CXCR4, if any, is not known (created with BioRender.com). d NanoBiT-based assay for VUF11207-induced dissociation of heterotrimeric G-proteins for CXCR4 and CXCR7 (mean ± SEM; n = 3 independent experiments; normalized with luminescence signal under unstimulated condition taken as 1). e Agonist-induced decrease in forskolin-induced cAMP level measured using the GloSensor assay for the indicated receptor-ligand combinations as a readout of Gαi-activation (mean ± SEM; n = 4; normalized with the signal at minimal ligand dose for CXCL12-CXCR4 combination as 100%). f Agonist-induced increase in cAMP level measured using the GloSensor assay for the indicated receptor-ligand combinations as a readout of Gαs-activation (mean ± SEM; n = 3; normalized with maximal signal for V2R as 100%). V2R (vasopressin receptor subtype 2) is used as a positive control. g Agonist-induced increase in Ca++ level measured using the GCaMP sensor for the indicated receptor-ligand combinations as a readout of Gαq-activation (mean ± SEM; n = 4; normalized with maximal signal for serotonin as 100%). 5-HT2C receptor is used as a positive control. Source data are provided as a source data file.
