Nuclear Receptor Screening Services
INQUIRYBOC Sciences, relying on its professional drug screening platform and molecular pharmacology technologies, has established a high-throughput, high-sensitivity system for nuclear receptor screening and analysis, supporting end-to-end services from primary screening to mechanistic studies. The company offers more than 30 functionally stable cell lines expressing nuclear receptors, covering key targets such as ER, AR, PPAR, LXR, and FXR, suitable for various types of small molecule compounds, including agonists, antagonists, and selective modulators. The platform integrates multiple core technical modules such as reporter gene analysis, ligand binding assays, coactivator recruitment, RT-qPCR, HTS screening, and target specificity validation to ensure accurate and reliable screening results.
Service Highlights and Advantages
- Comprehensive coverage of the nuclear receptor family: includes over 40 known nuclear receptor targets, including orphan receptors, metabolic receptors, and steroid receptors.
- Extensive nuclear receptor functional cell lines: offers over 30 cell lines stably expressing nuclear receptors, covering common drug targets such as ER, AR, and PPAR.
- Supports various small molecule types: suitable for screening and analyzing multiple categories of small molecule compounds, including agonists, antagonists, and selective modulators.
- High-throughput screening capability: supports 96/384-well plate formats and is equipped with automated workstations for large-scale compound library screening.
- Diverse detection formats: supports multiple detection methods such as fluorescence, luminescence, TR-FRET, and qPCR to meet different experimental needs.
- Flexible customized services: enables combinations of various techniques (reporter gene + ligand binding + coactivator recruitment + RT-qPCR) as needed to suit different R&D stages.
Nuclear Receptor Screening and Profiling Services
BOC Sciences has developed a complete, high-sensitivity, high-throughput, and quantitative technical system for nuclear receptor screening and analysis, fully covering ligand recognition, receptor activation, signal transduction, gene regulation, and functional validation. These modules address not only the early-stage screening needs of nuclear receptor drug discovery but also extend to mechanism research and druggability validation. The following are the seven core technical modules of our platform:
Reporter Gene Assays
- Utilize reporter gene vectors (such as luciferase or GFP) containing hormone response elements (HRE).
- Co-transfection of receptor and reporter systems into cells to monitor signal changes triggered by receptor activation.
- Evaluate the agonistic or antagonistic effects of compounds and determine their potency (EC50/IC50).
- Supports 96- and 384-well formats, suitable for medium- to high-throughput screening.
Ligand Binding Assays
- Use radioactive labels (e.g., [3H], [14C]) or non-radioactive methods (e.g., FRET, TR-FRET, fluorescence polarization).
- Measure candidate ligand affinity (Kd) and inhibitory ability (Ki) toward nuclear receptors.
- Provide full-length receptor proteins or expression and purification of ligand-binding domains (LBDs).
- Suitable for structure-activity relationship studies and mechanism elucidation.
Coactivator Recruitment Assays
- Use AlphaScreen, TR-FRET, or BRET technologies to monitor interactions between nuclear receptors and coactivators.
- Reveal conformational changes upon receptor activation and binding to transcriptional complexes.
- Facilitate screening of ligands with selective modulation mechanisms, such as partial agonists or selective modulators.
- Suitable for elucidating regulatory mechanisms and non-traditional modes of action.
Transcription Factor Microarrays and RT-qPCR Analysis
- Provide nuclear receptor pathway gene chip services covering multiple target gene pathways.
- Perform RT-qPCR to quantify the expression of specific genes (e.g., CYP3A4, UCP1, FABP4).
- Analyze gene regulatory effects and downstream pathway activity following receptor activation.
- Offer molecular-level data support for functional screening and mechanistic studies of candidate compounds.
High-Throughput Screening (HTS) Platform
- Establish an automated liquid handling and detection platform compatible with large-scale compound library screening.
- Support multiplexed testing across various nuclear receptors and compound dosages to improve screening efficiency and data consistency.
- Conduct primary screening, secondary validation, and targeted SAR analysis.
- Offer customized screening services, including compound library design and strategy optimization.
Target Selectivity and Specificity Analysis
- Simultaneously evaluate compound activity across multiple nuclear receptor subtypes to determine target selectivity.
- Apply reporter gene systems or transcriptomics to identify off-target effects.
- Support selectivity testing for various nuclear receptors, such as PPAR, LXR, RAR, FXR, and ER.
- Use CRISPR knockout cell lines to verify action pathways and target specificity.
Cytotoxicity and Functional Validation Assays
- Use MTT, CellTiter-Glo, and other methods to assess the effects of candidate compounds on cell viability.
- Provide functional assays such as lipid accumulation detection (Oil Red O staining), glucose uptake, and ELISA.
- Validate the physiological effects of compounds at the cellular level and their relevance to nuclear receptor regulation.
- Offer biological support for pharmacodynamic screening and lead optimization.
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BOC Sciences integrates innovative technologies to empower your drug discovery with strong momentum, fully dedicated to building next-generation drug screening platforms.
Nuclear Receptor Targets Supported by BOC Sciences
Our screening system covers over 40 human nuclear receptor targets, including classical steroid receptors (e.g., estrogen receptor, androgen receptor), non-steroidal receptors (e.g., PPAR, LXR, FXR, RXR), and orphan receptors (e.g., NR4A, ROR, ERR), meeting various research needs.
| Category | Nuclear Receptor Target | Alias | Primary Function | Common Application Areas |
|---|---|---|---|---|
| Steroid Hormone Receptors | Androgen Receptor (AR) | NR3C4 | Regulates male sexual development, reproductive function, and muscle growth | Prostate cancer research, androgen antagonist screening |
| Estrogen Receptor α (ERα) | NR3A1 | Regulates female reproductive system, bone metabolism, cardiovascular health | Breast cancer drug screening, endocrine disorder research | |
| Estrogen Receptor β (ERβ) | NR3A2 | Complements ERα, involved in neuroprotection and anti-inflammatory processes | Neurological disorders, osteoporosis research | |
| Progesterone Receptor (PR) | NR3C3 | Associated with menstrual cycle, pregnancy, and mammary gland development | Gynecological drug development, hormone antagonist studies | |
| Glucocorticoid Receptor (GR) | NR3C1 | Regulates stress response, immunosuppression, glucose metabolism | Anti-inflammatory drug screening, autoimmune disease research | |
| Mineralocorticoid Receptor (MR) | NR3C2 | Regulates sodium-potassium balance and blood pressure | Hypertension treatment, water-electrolyte balance studies | |
| Thyroid/Vitamin Receptors | Thyroid Hormone Receptor α (TRα) | NR1A1 | Mediates thyroid hormone effects, affects metabolism and development | Metabolic syndrome, thyroid disease screening |
| Thyroid Hormone Receptor β (TRβ) | NR1A2 | Similar function to TRα, with tissue-specific expression | Liver disease, cardiovascular metabolic regulation | |
| Vitamin D Receptor (VDR) | NR1I1 | Maintains calcium-phosphorus balance and bone health | Osteoporosis, cancer prevention, immune regulation | |
| Retinoic Acid Receptor (RAR) | NR1B1–3 | Regulates embryonic development, skin health, and cellular differentiation | Anti-cancer drug screening, dermatology research | |
| Retinoid X Receptor (RXR) | NR2B1–3 | Forms heterodimers with RAR, PPAR, etc., to regulate multiple pathways | Metabolic disease, cancer, inflammation research | |
| Metabolic Sensors | PPARα | NR1C1 | Promotes fatty acid oxidation and cholesterol metabolism | Hyperlipidemia, atherosclerosis research |
| PPARβ/δ | NR1C2 | Regulates muscle metabolism, fatty acid oxidation, insulin sensitivity | Type 2 diabetes, obesity treatment target | |
| PPARγ | NR1C3 | Regulates adipogenesis and insulin sensitivity | Insulin sensitizer development, metabolic syndrome screening | |
| Liver X Receptor α (LXRα) | NR1H3 | Controls cholesterol efflux and lipid metabolism | Atherosclerosis, fatty liver research | |
| Liver X Receptor β (LXRβ) | NR1H2 | Similar function to LXRα, broadly expressed | Hyperlipidemia, metabolic regulation research | |
| Farnesoid X Receptor (FXR) | NR1H4 | Regulates bile acid and lipid metabolism | NAFLD, bile acid-related disorder research | |
| Pregnane X Receptor (PXR) | NR1I2 | Senses xenobiotics and regulates expression of drug-metabolizing enzymes | Drug metabolism and toxicology studies, inducer screening | |
| Constitutive Androstane Receptor (CAR) | NR1I3 | Regulates drug metabolism and bilirubin clearance | Drug metabolism and enzyme induction research | |
| Circadian/Energy Receptors | Rev-Erbα | NR1D1 | Regulates circadian rhythm, metabolic homeostasis, and inflammatory responses | Chronobiotic screening, metabolic disorder research |
| Rev-Erbβ | NR1D2 | Similar function to Rev-Erbα | Circadian-related disease drug development | |
| RORα | NR1F1 | Involved in immune regulation, circadian rhythm, and neurodevelopment | Inflammation, neurological disorder research | |
| RORγ | NR1F3 | Regulates T cell differentiation and immune response | Autoimmune diseases (e.g., psoriasis, rheumatoid arthritis) |
Project Workflow
Preliminary Communication and Requirement Assessment
We provide feasibility assessments, preliminary solution proposals, and time-cost estimates based on project requirements. We assist in determining the technical route to ensure that the screening strategy is efficient, controllable, and scientifically aligned with project objectives.
Target Construction and Cell Model Preparation
We construct expression vectors based on the characteristics of the target nuclear receptors and introduce them into host cells such as HEK293 or CHO. Stable cell lines are established in combination with reporter gene systems. Additionally, purified receptor proteins can be expressed for ligand-binding assays.
Primary Screening
Using high-throughput reporter gene detection systems (e.g., Luciferase), we rapidly assess the agonistic or antagonistic activity of compounds. Ligand-binding assays (fluorescence polarization or radiolabeling) are conducted to screen candidate molecules. Dose-response curves are generated through gradient testing to preliminarily determine compound potency and affinity.
Secondary Screening and Mechanism Validation
For hit compounds from the primary screen, we conduct further coactivator recruitment verification using AlphaScreen or TR-FRET. RT-qPCR is used to detect downstream target gene expression to confirm regulatory mechanisms. False-positive compounds are eliminated through cell viability and functional assays (e.g., MTT, ELISA).
Target Specificity and Off-Target Evaluation
For hit compounds, activity across multiple nuclear receptor subtypes (e.g., ERα/β, PPARγ/δ) is tested to compare selectivity and assess off-target risks. We can construct CRISPR knockout cell models to validate dependency of action, and use proteomics and transcriptomics data to reveal potential off-target effects and non-specific interference.
Data Analysis and Report Preparation
All experimental data are processed by a professional bioinformatics team, including statistical analysis, dose-response curve fitting, and signal-to-noise ratio calculation. Visualized charts and heatmaps are generated. A complete report is submitted, including experimental methods, analytical procedures, major findings, and technical recommendations.
Applications of Nuclear Receptor Screening
Drug Discovery
Nuclear receptors are key drug targets. BOC Sciences' screening platform supports early-stage compound activity screening, lead compound structural optimization, and mechanism validation. Techniques such as reporter gene assays and ligand-binding experiments facilitate the screening and evaluation of candidate agonists and antagonists.
Metabolic Disease Research
Nuclear receptors such as PPAR, LXR, and FXR play central roles in glucose and lipid metabolism. Our platform establishes specific screening systems to study regulatory mechanisms of these receptors in metabolic disorders, aiding in the discovery of new therapeutic targets and candidate drugs for diseases such as type II diabetes, non-alcoholic fatty liver disease, and atherosclerosis.
Cancer Therapy
Nuclear receptors such as estrogen receptor (ER) and androgen receptor (AR) are highly expressed in tumors like breast and prostate cancers. We offer screening solutions based on cell models and reporter genes to identify novel modulators of ER/AR pathways, supporting cancer target research and anticancer drug development.
Toxicity and Endocrine Disruptor Assessment
Certain environmental chemicals may disrupt the endocrine system by activating or inhibiting nuclear receptor pathways. BOC Sciences provides high-throughput screening services based on reporter genes to evaluate compound agonism or antagonism toward receptors such as ER, AR, TR, and PPAR, aiding in the identification of endocrine disruptors.
FAQs
Which types of nuclear receptors can BOC Sciences screen?
Our platform covers more than 40 nuclear receptors, including estrogen receptors (ER), androgen receptors (AR), peroxisome proliferator-activated receptors (PPARα/γ/δ), liver X receptors (LXR), pregnane X receptors (PXR), and vitamin D receptors (VDR), suitable for multi-target screening needs.
What types of compounds can be screened? Are both agonists and antagonists supported?
Yes, we support the screening of agonists, antagonists, and selective modulators among various small molecules. We also provide customized analysis schemes based on the mechanisms of action.
Do you provide high-throughput screening (HTS) services?
Yes. Our platform is equipped with automated HTS systems that can handle 96-/384-well formats, suitable for large-scale compound library screening and lead optimization stages.
Can receptor selectivity and specificity be evaluated?
Yes. We evaluate the targeting selectivity of candidate molecules through coactivator recruitment, ligand-binding assays, and target comparison analysis, helping clients identify highly specific active compounds.
Can natural products or complex samples be screened?
Absolutely. With extensive experience in natural product screening, our platform is compatible with crude extracts, metabolite fractions, or compound mixtures and can systematically analyze their nuclear receptor regulatory activity.
What will the experimental data include?
We provide complete experimental reports, including raw data, graphical analyses, statistical results, IC₅₀/EC₅₀ calculations, and detailed experimental conditions, ensuring transparency, reproducibility, and publication readiness.
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