GPCR Assay Kits: Streamline Your GPCR Research

Illuminate cellular signaling with our GPCR Assay Kits:

Uncover subtle changes in cellular signaling pathways through quantification of GPCR activity

Enable confident decision-making with robust and reliable results

GPCR Assays2 (3)

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Unveiling the Significance of GPCRs: Key Players in Cellular Signaling and Therapeutic Potential

GPCRs, short for G-protein coupled receptors, are a vital class of cell surface receptors involved in various physiological processes. These receptors transmit extracellular signals to the intracellular environment, influencing cellular behavior and regulation of important functions.

GPCRs are incredibly diverse and exist in abundance throughout the human body. They play crucial roles in the molecular sensing of hormones, neurotransmitters, and light, making them vital to sensory processes such as vision, olfaction, and taste.

The basic structure of GPCRs consists of seven transmembrane helices embedded in the cellular membrane. When a ligand binds to the receptor, it triggers a series of events leading to the activation of intracellular signaling pathways. These pathways, often mediated by G-proteins, can impact gene expression, enzyme activity, ion channel conductance, and other cellular responses.

Understanding GPCRs is crucial for drug development, as they are targets for a significant proportion of medications on the market today. Exploring the intricacies of these receptors continues to be an exciting area of research, offering promising avenues for novel therapeutic interventions.

Frequently Asked Questions

INDIGO’s assays are not binding assays. They are cell-based trans-activation assays, and the principal application is in the screening of test samples to quantify any functional activity, either agonist or antagonist, that the compounds may exert against the nuclear receptors. INDIGO reporter systems utilize firefly luciferase reporter gene technology, and while there is a binding taking place, our assays do not measure it. Instead, the luciferase light response is measured which correlates to the activation status of the receptor (either activation or inhibition). Quantifying changes in luciferase expression in the treated reporter cells provides a sensitive surrogate measure of the changes in receptor activity. It will tell the scientist the significance (strength) of the interaction by the level of light emitted. In addition, cell-based assays are more sensitive and able to detect smaller levels of activation.

INDIGO’s nuclear receptor assays utilize proprietary human and non-human mammalian cells engineered to provide constitutive, high-level expression of the designated receptor. Specific cell type information for each assay is proprietary and available only through consultation with INDIGO’s technical team following a screening service or assay kit purchase.

Reporter cells included in INIDIGO’s steroid hormone nuclear assay kits (ERα, ERβ, AR, PGR, MR, GR) express the native, full-length receptors. INDIGO’s other nuclear receptor assays, however, include reporter cells that express hybrid nuclear receptors. In these cases, the respective receptor’s native N-terminal sequence comprising the DNA Binding Domain (DBD) has been replaced with sequence encoding the yeast Gal4-DBD. All other native NR functional/structural domains (ligand binding domain, hinge region, and various activation domains) are present in these hybrid receptors. These reporter cells also contain the firefly luciferase reporter gene functionally linked to the upstream genetic response element for Gal4. Consequently, once a bioactive compound associates with the ligand binding domain of the hybrid receptor, only the luciferase reporter gene is induced. Ligand-activation of the hybrid receptor will not induce collateral expression of target genes that are otherwise regulated by the native nuclear receptor.

View our list of reference compounds. We do utilize commercially available reference agonists for our assays, and this reference agonist is included in each assay kit. We do use reference antagonists where a reference is known and commercially available. Some of our antagonist assays do not have reference antagonists available.

Each kit includes luciferase reporter cells, an assay plate, all required reagents (optimized culture media, positive-control agonist, and detection reagent), and a detailed Technical Manual. A luminometer is required for Relative Light Unit (RLU) measurements.

INDIGO’s kits are intended for research purposes only, and not for diagnostic or therapeutic use in humans.

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