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.1,3
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:
Case: This study investigated biased agonism at human CC chemokine receptors CCR4, CCR7, and CCR10, examining how different chemokine ligands preferentially activate G protein- and adaptor protein-mediated signaling pathways within the same cellular context, given the promiscuous nature of chemokine receptor interactions and the known biased signaling of these receptors. The results demonstrate the considerable variations between the intracellular signals evoked.
Adaptor protein recruitment assay
Fig.2 The recruitment of adaptor protein to the chemokine receptors CCR4, CCR7, and CCR10 stimulated by different chemokine ligands.2,3
G protein activation assay
Fig.3 The G protein activation via CCR4, CCR7, and CCR10 stimulated by different chemokine ligands.2,3
cAMP synthesis assay
Fig.4 The cAMP synthesis inhibition via CCR4, CCR7, and CCR10 stimulated by different chemokine ligands.2,3
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
For Research Use Only.