Nuclear Receptor (NR) Assays and Functional Profiling Services

CD Biosynsis offers comprehensive Nuclear Receptor (NR) Assays essential for drug discovery targeting metabolic disorders, inflammation, cancer, and reproductive health. Nuclear Receptors are ligand-activated transcription factors that regulate gene expression upon binding to steroids, hormones, and xenobiotics. Our platform provides quantitative measurement of ligand binding affinity, co-regulator recruitment, and transcriptional activity (agonism/antagonism). We utilize robust, high-throughput technologies including FRET/TR-FRET (ligand binding, co-activator assays), High-Content Imaging (translocation), and Luciferase Reporter Gene Assays (RGAs). Researchers can select and combine individual NR targets and functional modules to build a custom profiling panel, enabling precise characterization of compound efficacy and mechanism of action for both endocrine and orphan receptors.

Get a Quote

Functional Mapping of Ligand-Activated Transcription Factors

Nuclear Receptors (NRs) modulate gene expression by undergoing conformational changes upon ligand binding, leading to the recruitment or dissociation of co-activator and co-repressor proteins. This makes both the ligand binding domain (LBD) and the co-regulator interaction surface attractive targets. Our services are designed to address this complexity by offering modules for both direct binding and functional consequences. We offer selectable panels allowing clients to focus on specific NR families, such as profiling compounds against steroid receptors (e.g., ER, GR) or metabolic regulators (e.g., PPARs, LXRs). This targeted and comprehensive analysis provides the precise data needed to understand compound mechanism of action (MoA) and predict in vivo effects, distinguishing between full agonists, partial agonists, and antagonists.

Nuclear Receptor Assay Service Workflow

A staged process for characterizing NR ligand activity and binding.

Target Selection and Reagent Prep

Ligand Binding and Co-Regulator Assays

Cell-Based Functional Analysis (RGA)

Data Interpretation and Reporting

Panel Customization: Finalize the list of NR targets and select the corresponding LBD domain and RGA cell lines.

Quality Control: Validate purified LBD protein functionality and reporter cell line response to known agonists/antagonists.

Binding Assay: Determine the binding constant (Kd) using the selected method (e.g., TR-FRET, Saturation Binding).

Co-Regulator Profiling: Measure the compound's effect on co-activator peptide recruitment to the LBD (IC50/EC50).

RGA Screening: Treat reporter cell lines with test compounds across a concentration range to measure transcriptional agonism/antagonism.

MoA Confirmation: Differentiate full, partial, and inverse agonists based on concentration-response curves and maximal activity.

Selectivity Index: Compare potency (EC50) across a panel of related NR targets (e.g., PPARs vs. LXR).
Mechanistic Correlation: Compare in vitro LBD affinity (Kd) with cellular potency (RGA EC50).
Reporting: Deliver raw data, dose-response curves, calculated Kd, EC50/IC50 values, and full technical protocols.

Comprehensive Functional and Binding Analysis

Dual-Mode Profiling

Simultaneous measurement of direct ligand binding and functional transcriptional output (RGA) for MoA clarity.

Co-Regulator Interaction

FRET/TR-FRET assays to quantify the recruitment of key co-activator peptides (SRC-1, TIF2) upon ligand binding.

Extensive NR Target Library

Validated assays for all major Class I (Steroid) and Class II (Metabolic) Receptors, including Orphan NRs.

Agonist/Antagonist Differentiation

Accurate identification and quantification of full agonists, partial agonists, and pure antagonists.

Client Testimonials on Nuclear Receptor Assays

"The combination of the PPARg RGA and the co-regulator recruitment assay definitively proved our compound was a novel partial agonist, reducing the risk of side effects."

Dr. Emily Carter, Metabolic Disease Research

"The TR-FRET binding assay for the Glucocorticoid Receptor provided a highly accurate Kd, which was essential for calibrating the cellular potency of our antagonists."

Mr. David Rodriguez, Assay Development Lead

"Their full selectivity panel against all major steroid receptors quickly identified our compound's specificity for the Androgen Receptor, accelerating our oncology program."

Ms. Sophia Chen, Translational Biology Manager

FAQs about Nuclear Receptor Assays

Still have questions?

What are the key functional domains of a Nuclear Receptor?

The key domains are the DNA-binding domain (DBD) which binds to hormone response elements (HREs), and the Ligand-Binding Domain (LBD) which binds ligands and recruits co-regulators.

What is the difference between an in vitro binding assay and a Reporter Gene Assay (RGA)?

The in vitro binding assay (e.g., TR-FRET) measures the direct physical binding affinity (Kd) of the ligand to the purified LBD. The RGA measures the functional consequence of binding (transcriptional agonism/antagonism) in a living cell (EC50/IC50).

What is a partial agonist in the context of NRs?

A partial agonist is a ligand that, even at saturating concentrations, activates the receptor to a maximal response that is less than that achieved by the full agonist. This often correlates with a unique co-regulator recruitment profile.

What is the role of Orphan Nuclear Receptors?

Orphan NRs are receptors whose endogenous ligands have not yet been definitively identified. They are attractive drug targets because they often regulate critical metabolic or developmental pathways, and their function can be modulated by synthetic ligands.

How much does Metabolic Engineering services cost?

The cost of Metabolic Engineering services depends on the project scope, complexity of the target compound, the host organism chosen, and the required yield optimization. We provide customized quotes after a detailed discussion of your specific research objectives.

Do your engineered strains meet regulatory standards?

We adhere to high quality control standards in all strain construction and optimization processes. While we do not handle final regulatory approval, our detailed documentation and compliance with best laboratory practices ensure your engineered strains are prepared for necessary regulatory filings (e.g., GRAS, FDA).

What to look for when selecting the best gene editing service?

We provide various gene editing services such as CRISPR-sgRNA library generation, stable transformation cell line generation, gene knockout cell line generation, and gene point mutation cell line generation. Users are free to select the type of service that suits their research.

Does gene editing allow customisability?

Yes, we offer very customised gene editing solutions such as AAV vector capsid directed evolution, mRNA vector gene delivery, library creation, promoter evolution and screening, etc.

What is the process for keeping data private and confidential?

We adhere to the data privacy policy completely, and all customer data and experimental data are kept confidential.

Nuclear Receptor (NR) Assays and Functional Profiling Services

Functional Mapping of Ligand-Activated Transcription Factors

Customizable Nuclear Receptor Targets and Functional Modules

Selectable Steroid and Endocrine Receptors

Choose Key Endocrine NR Targets for Profiling

Selectable Metabolic and Orphan Receptors

Choose Metabolic and Orphan NR Targets for Screening

Mechanistic and Binding Modules

Select Quantitative and High-Content Services

Nuclear Receptor Assay Service Workflow

Comprehensive Functional and Binding Analysis

Client Testimonials on Nuclear Receptor Assays

FAQs about Nuclear Receptor Assays