Figure The coupling of Stachel-activated GPR56 and disease associated
mutations of the receptor with Gα12.
The effect of BFPP mutations on
Gα13coupling
GPR56 or BFPP mutants of the receptor were co-expressed with
Gα13 and GRK-based Gβδ biosensors to assess the effect
of each mutation on the Gα13 protein coupling, upon
receptor activation with the Stachel peptide. For this, HEK293
cells were treated with the 1mM P7 Stachel peptide and
Gα13 coupling and heterotrimeric G protein activation
was measured as nanoBRET. Under the biosensor conditions reported in
this work, all BFPP mutants showed disrupted Gα13coupling while the most severe was observed for GPR56R38W.