GPCR targeted Functional Assay Services

The Evolving Landscape of GPCR Signaling and Drug Discovery

G protein-coupled receptors (GPCRs) represent the largest and most versatile superfamily of cell surface receptors, playing pivotal roles in nearly every physiological process. Their interaction with a diverse array of ligands, from hormones and neurotransmitters to light, positions them as central therapeutic targets for over a third of all marketed drugs. The classical understanding of GPCR signaling, primarily via G proteins, has evolved, revealing a far more intricate network. This complexity underscores the critical need for sophisticated functional assays to fully elucidate their signaling pathways, identify novel drug candidates, and address unmet medical needs. Developing these assays is fundamental to advancing drug discovery and therapeutic development, ensuring targets are thoroughly characterized for optimal drug design.

Fig.1 GPCR-interacting proteins' functions in GPCR localization at the cell surface.¹

GPCR targeted Functional Assays at Creative Biolabs

Creative Biolabs' GPCR targeted functional assays provide comprehensive solutions for drug discovery, from target validation to lead optimization. Our services are designed to deliver precise, actionable data to accelerate your research and development efforts. You can expect high-quality results backed by our expertise and rigorous quality control.

Our assays primarily leverage cell-based systems where GPCRs are functionally expressed. The principle involves detecting changes in intracellular second messengers (such as calcium or cAMP) or reporter gene activity upon GPCR activation or inhibition by test compounds. This allows for a direct measurement of the functional consequence of compound-receptor interaction. Projects typically range from 8 to 16 weeks, depending on the complexity of your specific GPCR target and the scope of the screening. Throughout this process, our commitment to quality is paramount, ensuring that all data are meticulously validated, reproducible, and of the highest scientific standard to support critical decision-making in your drug development pipeline.

Service Packages

Step1. Project Discussion & Design

We begin with an in-depth consultation to understand your specific research goals and design a tailored assay strategy. This involves selecting the most appropriate assay format (e.g., calcium flux, cAMP, reporter assays) and developing a customized analytical scheme.

Step2. Cell Line Development (if needed)

For targets without an existing suitable cell model, we offer Hi-Affi™ GPCR Stable Cell Line Development. This involves constructing and validating stable cell lines that robustly express your GPCR of interest, ensuring functional integrity.

Step3. Assay Optimization & Validation

We optimize the selected functional assay conditions for your specific GPCR and ensure its robustness and sensitivity. This includes dose-response curve generation and Z'-factor determination for high-throughput compatibility.

Step4. Compound Screening/Profiling

Utilizing our high-throughput screening (HTS) platforms, we screen your compound libraries or profile specific compounds against the validated GPCR assay. We measure second messenger readouts according to the natural pathways of GPCRs.

Step5. Data Analysis & Reporting

Comprehensive analysis of the collected data is performed, including statistical evaluation and hit identification. A detailed report summarizing all experimental procedures, raw data, analyzed results, and conclusions is provided.

Service Highlights

• High Sensitivity: Detect even subtle receptor activation or inhibition.
• High Throughput: Screen vast compound libraries efficiently, accelerating hit identification.
• Diverse Readouts: Cover multiple second messenger pathways for comprehensive target characterization.
• Customization: Tailored assay design to meet unique project requirements.
• Validated Cell Lines: Utilize robust, functionally validated GPCR stable cell lines for reliable results.

FAQs

1. Q1: Can Creative Biolabs assist with compounds that have unique solubility or stability challenges?

   A1: Yes, our experienced team is adept at handling challenging compounds. We employ specialized protocols and formulation techniques to address solubility and stability issues, ensuring your compounds are accurately tested in our assays. Let's discuss your specific compound's characteristics during your inquiry.

2. Q2: What types of GPCRs can Creative Biolabs' assays target?

   A2: Our assays are designed to target a wide range of GPCRs, including Class A, B, C, and F receptors. We have extensive experience with both well-characterized and uninvestigated GPCRs. If you have a specific target in mind, please reach out, and we'll discuss the best approach.

3. Q3: How do your functional assays ensure high sensitivity and specificity?

   A3: We achieve high sensitivity and specificity through meticulous assay design, optimization using our proprietary Hi-Affi™ GPCR Stable Cell Lines, and the use of state-of-the-art detection technologies. Our rigorous validation processes ensure that the assays accurately reflect the target's physiological function.

Contact Us

Creative Biolabs is your trusted partner in accelerating drug discovery through advanced GPCR Targeted Functional Assays. Our expertise, state-of-the-art platforms, and commitment to quality ensure that your projects are successful. If you are interested in our GPCR targeted functional assays, please feel free to get in touch with us or directly send us an inquiry.

Reference

1. Roux, Benoît T, and Graeme S Cottrell. "G protein-coupled receptors: what a difference a 'partner' makes." International journal of molecular sciences vol. 15,1 1112-42. 16 Jan. 2014, doi:10.3390/ijms15011112. Distributed under an Open Access License CC BY 3.0, without modification.

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