Chemokine receptors are serpentine G-protein-coupled receptors that are expressed by both cancer and stromal cells. The receptors and their ligands are important inflammatory mediators, controlling leukocyte extravasation and directing migration into inflamed and diseased organs. Targeting overexpressed chemokine receptors directly kills tumor cells and has a favorable effect on hematological malignancies, making them appealing tractable targets for the pharmaceutical sector.
Fig.1 Chemokine receptors in cancer therapy.1
As a leader in GPCRs functional assay, Creative Biolabs provides a top-ranking Magic™ in vitro cell-based chemokine receptor functional assay service to advance drug development in cancer therapy. Our Magic™ in vitro cell-based chemokine receptor functional assay service includes fluorescence and multiple second messenger readouts, including cAMP and calcium flux, and allows us to assay or analyze compounds' ability to modulate chemokine receptor activation and subsequent redistribution inside cells. We can assist worldwide clients in the following ways:
Fig.2 Chemokine receptors signaling pathway.2
Fig.3 The simplified workflow of our Magic™ in vitro cell-based chemokine receptor functional assay.
Representative data 1: To investigate the physiological significance of biased signaling at CXCR3, researchers screened a panel of publically accessible small-molecule CXCR3 ligands and discovered two agonists with biased signaling properties: VUF10661 and VUF11418. These small-molecule CXCR3 agonists also showed the distinct ability to recruit -arrestin1, attract GPCR kinases (GRKs) and induce CXCR3 internalization, consistent with their biased signaling features.
Fig.4 VUF10661 and VUF11418 are biased agonists of CXCR3.3
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 are interested in our Magic™ in vitro cell-based chemokine receptor functional assay service, please feel free to contact us. We are sincerely looking forward to working with you.
References
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