ADIPOR2 Analysis Service

With years of experience in assay design and lab analysis, Creative Biolabs can support your ADIPOR2 protein discovery pipeline by providing biomarker analysis on advanced platforms. Whether your study is designed or implemented by us, our focus on strategic assay validation/qualification enables us to accurately test your study samples and provide reliable biological translation to your drug discovery program.

Introduction of ADIPOR2

ADIPOR2 is a pivotal cell-surface receptor highly expressed in the liver and skeletal muscle, serving as a primary receptor for adiponectin. Structurally, it is a non-canonical seven-transmembrane (7-TM) protein with a reverse topology (N-terminus intracellular). Critically, the 7-TM domain coordinates a crucial zinc ion (Zn2+) within its internal cavity, suggesting a novel ligand activation mechanism distinct from classic G protein-coupled receptors (GPCRs). This unique architecture necessitates specialized analytical techniques for successful therapeutic targeting and validation.

Signaling transduction via adiponectin receptors (AdipoR1 and AdipoR2) activation. (OA Literature)Fig.1 ADIPOR2 involved signaling pathways.1

ADIPOR2 primarily signals through the activation of peroxisome proliferator-activated receptor (PPAR)-α, driving robust hepatic fatty acid oxidation and reducing lipid accumulation—key anti-steatotic functions. Genetic variations like the rs11061971 SNP are associated with obesity and Type 2 Diabetes (T2D) risk, highlighting its diagnostic power. Loss of ADIPOR2 function is directly linked to impaired insulin sensitivity, confirming its central role in metabolic disease and cancer pathogenesis.

The functions of activated ADIPOR2. (Creative Biolabs Original)Fig.2 Examples of functions of activated ADIPOR2.

ADIPOR2 Analysis Services at Creative Biolabs

We offer a comprehensive suite of ADIPOR2 analysis services, moving beyond standard biomarker measurement to provide deep functional and mechanistic insights. Our customized assays are designed to overcome the unique structural challenges of this non-GPCR receptor, accelerating the development of selective small-molecule agonists for precision medicine.

Our ADIPOR2-targeting services include but are not limited to the following specialized analyses:

Used for protein validation and interaction studies, IP allows us to isolate the ADIPOR2 protein and its binding partners from cell lysates using specific anti-ADIPOR2 antibodies.

We use small interfering RNA (siRNA) to temporarily knock down ADIPOR2 gene expression. This is critical for assessing the phenotype and mechanism of action linked to ADIPOR2 function.

This technique confirms the determination of ADIPOR2 protein expression levels in various tissues and cell lines. It is essential for validating antibody specificity and monitoring drug-induced changes in protein abundance.

Quantitative reverse transcription PCR is used for the determination of ADIPOR2 mRNA expression and quantification. This allows for precise measurement of transcriptional regulation in response to therapeutic compounds.

We analyze sequence variants (e.g., rs11061971 and rs767870) in the ADIPOR2 gene. This is vital for patient stratification and understanding genetic risk factors in metabolic and cardiovascular diseases.

Service Workflow

01Initial Consultation and Assay Design

The process begins with a detailed consultation to define the therapeutic goal, review the client's starting materials (compounds, cell lines, or tissues), and co-design a customized ADIPOR2 Analysis panel focusing on the Zn2+ or differential signaling mechanism.

02Sample Receipt and QC

Client-provided samples (e.g., test compounds, plasma, or liver biopsies) are received. We perform stringent quality control (QC) checks, including compound solubility testing and genomic integrity confirmation for SNP analysis, ensuring optimal assay performance.

03Execution of ADIPOR2 Analysis

High-throughput screening (HTS) of the ADIPOR2-selective assays, including functional profiling, Zn2+ binding, and gene expression analysis (qRT-PCR), is executed using validated, proprietary Creative Biolabs platforms.

04Data Delivery and Interpretation

The final comprehensive report includes raw data, quality assurance documentation, mechanistic interpretation of ADIPOR2 agonism, and strategic recommendations for lead optimization, delivered within the agreed-upon timeline.

Applications

Non-Alcoholic Steatohepatitis (NASH) and Fibrosis

ADIPOR2 analysis is crucial for developing anti-fibrotic agents. By measuring PPAR α activation in hepatic models, we identify compounds that specifically drive fatty acid oxidation, directly combating steatosis and inhibiting hepatic stellate cell activation (fibrosis).

Oncology and Immune Checkpoint Enhancement

Profiling ADIPOR2 expression and its downstream COX-2/PPAR signaling in tumor microenvironment models helps identify leads that modulate tumor-immune interactions, potentially synergizing with existing immuno-oncology therapies.

T2D and Insulin Resistance

We validate compounds for their ability to restore ADIPOR2 function, improving glucose uptake and insulin sensitivity in muscle and liver cells, offering a highly specific therapeutic route for T2D management.

Neuroprotection and Neurodegeneration

Functional screening of small molecules against ADIPOR2's established role in mitigating tau hyperphosphorylation allows for the rapid identification of novel neuroprotective drug candidates for conditions like Alzheimer's Disease.

Service Highlights

FAQs

  1. How do you ensure the compounds identified are specific to ADIPOR2 and not the homologous ADIPOR1?

    We employ a Differential Pathway Profiling approach utilizing customized cell lines that quantitatively measure ADIPOR2's distinct PPAR α activation pathway separately from ADIPOR1's AMPK signaling. This guarantees selective ADIPOR2 agonism.

  2. Can your service analyze the adiponectin-independent functions of ADIPOR2?

    Absolutely; we utilize Membrane Fluidity Kinetics assays to assess ADIPOR2's role in membrane homeostasis and cellular stress response. This unique assay provides critical data for understanding ADIPOR2's fundamental, adiponectin-free regulatory functions.

  3. What specific genomic analyses are included beyond basic mRNA expression of the ADIPOR2 gene?

    Our translational genomic analysis includes SNP analysis for variants like rs767870 and rs11061971, alongside the evaluation of differential DNA methylation patterns. This pinpoints patient segments most likely to respond.

  4. For a client focused on NASH, which ADIPOR2 assay is the most relevant for lead prioritization?

    For NASH, the most relevant assay is the PPAR α activation assay within our Differential Pathway Profiling panel. This directly measures the anti-steatotic function of the lead compound in driving hepatic fatty acid oxidation.

  5. If a compound shows weak activity, does your report provide recommendations for optimization?

    Yes, the final report is comprehensive and includes strategic recommendations for lead optimization. Our scientific team provides mechanistic interpretation and suggests structural modifications to enhance selectivity or potency based on the data.

  6. How do you ensure the reproducibility and quality of the specialized ADIPOR2 functional assays?

    We ensure reproducibility through strategic assay validation/qualification using benchmark anti-ADIPOR2 monoclonal antibodies and reference agonists. Every assay run includes multiple quality control checks and internal standards to meet rigorous criteria.

If you are interested in our services at Creative Biolabs, please contact us for more information.

Reference

  1. Reverchon, Maxime, et al. "Adipokines and the female reproductive tract." International journal of endocrinology 2014.1 (2014): 232454. Distributed under Open Access license CC BY 3.0, without modification. https://doi.org/10.1155/2014/232454

For Research Use Only.


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