Magic™ In Vitro Cell-based Cholecystokinin Receptor Functional Assay Service

Cholecystokinin Receptors Overview

Cholecystokinin receptors (CCKRs) are a subfamily of GPCRs that bind the peptide hormones cholecystokinin (CCK) and gastrin. CCKAR and CCKBR are two important types of CCKRs and they are neurointestinal peptide hormone receptors. Functionally, they display essential roles in various physiological activities, such as consuming food and appetite control. Therefore, cholecystokinin receptors have the potential to be targeted for the treatment of related disorders.

Fig.1 The structure of cholecystokinin receptors.¹

Our Magic™ In Vitro Cell-based Cholecystokinin Receptor Functional Assay Service

With our extensive expertise and advanced technology in GPCR, Creative Biolabs succeeded in developing Magic™ in vitro cell-based cholecystokinin receptor functional assay service. We are committed to serving as a high-quality partner for global customers.

Our Magic™ in vitro cell-based cholecystokinin receptor functional assay service is carried out by measuring the calcium flux. Once a ligand attaches to the CCKR, it activates a G protein, causing intracellular calcium mobilization and activating PKC through the PLC-IP3 and DAG pathways, respectively. This assay allows us to assay compounds, as well as analyze their capability to modulate CCKR and signaling pathways. Throughout the process, we provide a full range of services to advance global customers' projects smoothly and we are confident in presenting the ideal results for every customer.

Fig.2 The signaling pathway of cholecystokinin receptors.²

Benefit for You

• A Diverse Range of Cell Types Aid in Our Assay Service.
  Prominent in the field of cell research, we provide a wide range of cell lines including CHO cell lines, HEK293T cell lines, etc. These cell lines allowed us to complete a number of initiatives for global customers.
• Fast Timeline Advances Our Assay Service.
  We employ within-the-firm kits to ensure high-quality, on-time delivery of global customers' projects and present the desirable results in 1-2 weeks.
• Competent Professional Teams Guarantee Our Assay Service.
  Each of our customers may be certain that their projects will go forward smoothly together with our competent research teams. Our Magic™ in vitro cell-based chemokine receptor functional assay combines with cell-based assays and an easy-to-operate process, which boosts drug development with no risk.
• Integrated Bespoke Services Empower Our Assay Service.
  We provide a full-around customized Magic™ in vitro cell-based cholecystokinin receptor functional assay service from sample processing to data visualization with the most up-to-date technical solutions.

Case Study

Purpose: The author hypothesized that binding to CCK8s would cause intracellular Ca²⁺ mobilization through this mechanism.

Methods: A cell-based Ca²⁺ imaging test was developed by creating stable monoclonal GPCR transgenic CHO cell lines for CHO-GPR173, CHO-CCK1R, and CHO-CCK2R. We utilized a microplate reader to track Ca²⁺ mobilization and a β-arrestin2 recruitment assay to verify if GPR173 is a CCK receptor.

Results: These results indicate that CCK8s may elicit a dose-dependent reaction in CHO-CCK1R/2R cells and demonstrate the high efficacy of CCK8s in triggering intracellular Ca²⁺ mobilization. The recruitment signal for CCK1R was substantially stronger in the β-arrestin1/2 test than in the β-arrestin2 assay. Meanwhile, CCK2R's β-arrestin1/2 recruitment efficiency was considerably greater than that of the β-arrestin2 recruitment assay.

Fig.3 CCK8s could activate intracellular Ca²⁺ mobilization in CHO-GPR173 cells.³

Work with Creative Biolabs

In the field of GPCR functional identification, Creative Biolabs is constantly optimizing and innovating and is committed to presenting the most ideal results for each customer. If you have an interest in our Magic™ in vitro cell-based cholecystokinin receptor functional assay service, please contact us. Our team is looking forward to working with you.

References

1. Zhang, Xuefeng, et al. "Structures of the human cholecystokinin receptors bound to agonists and antagonists." Nature Chemical Biology 17.12 (2021): 1230-1237.
2. Zeng, Qiang, et al. "Gastrin, cholecystokinin, signaling, and biological activities in cellular processes." Frontiers in Endocrinology 11 (2020): 112.
3. He, Ling, et al. "A Novel CCK Receptor GPR173 Mediates Potentiation of GABAergic Inhibition." Journal of Neuroscience 43.13 (2023): 2305-2325.

For Research Use Only.