Fig. 1.
Gonadotropin releasing hormone (GnRH) receptor (GnRHR) pharmacoperone assay principle. The mutant GnRHR is retained in the lumen of untreated cells. Addition of pharmacoperone rescues GnRHR, and the receptors are trafficked to the plasma membrane. GnRHR on the plasma membrane is now responsive to agonism by GnRH, which is quantitated using Fluo-2 detection reagents (box). The level of functional GnRHR (mutant) is proportional to the magnitude of Gq modulated signaling, IP3 induction, and subsequent Ca2+ released and detected in the cells via Fluo2 using the FLIPR Tetra reader as illustrated via the kinetic traces shown in the lower inset diagram.