GPCR Biology

G-Protein Coupled Receptors (GPCRs) are one of the largest receptor families in the genome and are essential for the healthy function of nearly every organ in the body. GPCRs are also important targets for therapeutic drugs. Increase your understanding of drug effects and GPCR biology with bright fluorescent assays in living cells.

With our GPCR Assays in Living Cells, you can:

Detect kinetic Gs, Gi, and Gq mediated responses in living cells
Combine multiple assays in the same cell population
Express sensors and run assays in disease relevant cell types
Detect fluorescence on imaging systems or automated plate readers (Z’>0.8)
Quantify agonist bias
De-orphanize receptors

Detecting Gs

Detect Gs mediated cAMP fluctuations with the cADDis cAMP assay.

→ BMG CLARIOstar® Application Note for Gs

Detecting Gi

Our cADDis cAMP sensor can be also used to detect Gi mediated responses.

→ Request Gi Assay Paper

Detecting Gq

Detect Gq mediated responses using R-GECO Ca²⁺, DAG, and PIP₂ assays.

→ BMG CLARIOstar® Application Note for Gq

Detecting β-Arrestin

Fluorescent beta-arrestin assays to detect arrestin recruitment at specific GPCRs.

→ Choose your receptor

Measuring GPCR Signaling Kinetics

See the Assay Guidance Manual chapter from NIH NCATS:

Biosensor Assays for Measuring the Kinetics of G-Protein and Arrestin-Mediated Signaling in Live Cells

Express GPCRs with BacMam

We have a growing catalog of GPCRs packaged in a modified Baculovirus vector, BacMam. BacMam transduction is a low-cost, effective method to express GPCRs in your cells of interest, including in primary and iPSC derived cells. See low cell-to-cell variability in expression, get consistent results from experiment to experiment, and titrate expression to your desired level. For more information and a current list of available receptors please see our GPCRs page.

Continuous Multiplex Measurements

Red fluorescent DAG sensor multiplexed with cADDis, a green fluorescent cAMP sensor, indicates Gs & Gq signaling via a calcitonin receptor.

Combine our red and green sensors in the same cells to measure multiple analytes simultaneously. Simply add both sensors to the transduction mix. Measure two signals, examine ligand bias, deorphanize GPCRs, and look for off-target GPCR activation.

Assays in Primary Cultures or iPSCs

Detect GPCR mediated responses in cells relevant to your disease, drug target, or biology of interest. Our BacMam-packaged sensors have been used in neurons, cardiomyoctes, islets, and many more primary and iPSC derived cells! Alternate promoters or viral vectors are available by request. The BacMam Transducible Cells page lists some publications showing disease-relevant cells transduced with BacMam. Pictured, at right, are the cADDis cAMP Assay in primary striatal neurons and the Red GECO calcium assay in nCardia’s Cor.4u cardiomyocytes.

Simple Protocol

We strive to create simple protocols with minimal liquid handling. Cell lysis, IBMX, enzymes, and co-factors are not necessary for these assays. Add our sensors to your cells, incubate, add drug, and measure fluorescent changes.