The GPER1 Knockout AGS Polyclonal Cells are a CRISPR/Cas9-edited polyclonal knockout population derived from AGS gastric adenocarcinoma cells, with targeted disruption of the GPER1 gene. This loss-of-function model enables the study of GPER1-mediated rapid estrogen signaling in a gastric epithelial context. The polyclonal format provides a diverse yet uniform knockout pool suitable for comparative functional assays.
AGS cells originate from a human gastric adenocarcinoma and exhibit epithelial morphology with adherent growth. They are widely employed as a model for gastric mucosal biology and gastric cancer research. The AGS line retains key signaling properties of gastric epithelial cells, making it particularly relevant for investigating oncogenic processes such as proliferation, migration, and estrogen responsiveness.
GPER1 encodes an estrogen-responsive GPCR that couples to G proteins (G??s/G??i) and interacts with ??-arrestin. Ligand binding by estradiol or G-1 triggers transactivation of EGFR, leading to activation of ERK1/2 in the MAPK pathway and AKT in the PI3K pathway, along with modulation of cAMP and calcium. Downstream targets include transcription factors NF-??B and STAT3, and target genes such as c-Fos, Cyclin D1, and matrix metalloproteinases. The receptor also interacts with ER??, ER??, and HSP90, and is antagonized by G-15, tamoxifen, and ICI 182,780.
In gastric adenocarcinoma, GPER1 signaling may influence proliferation, survival, and migration, processes that are often dysregulated in gastrointestinal malignancies. The GPER1 knockout AGS cells allow direct functional dissection of these processes. By ablating GPER1 expression, researchers can evaluate its contribution to oncogenic signaling and crosstalk with EGFR, as well as assess its role in the MAPK/ERK and PI3K/AKT/mTOR pathways that are critical in gastric cancer progression.
These cells are suited for a range of experimental approaches: Western blotting for phospho-ERK and phospho-AKT, qPCR for downstream targets, MTT proliferation assays, Transwell migration/invasion assays, calcium flux and cAMP measurements, co-immunoprecipitation of GPER1-EGFR, and immunofluorescence localization. Applications include estrogen signaling research, GPCR pharmacology, gastric cancer biology, and screening of endocrine therapies. For more information, contact Ascent Research.
