The GPR171 Knockout TE1 Polyclonal Cells are a CRISPR/Cas9-edited polyclonal knockout cell population with targeted disruption of GPR171 in the TE1 cell line. This mixed knockout population provides a loss-of-function model without clonal isolation, suitable for evaluating GPR171-dependent phenotypes in a bulk population.
TE1 is an epithelial cell line derived from a poorly differentiated human esophageal squamous cell carcinoma (ESCC). It serves as a model for ESCC research, retaining oncogenic properties such as dysregulated proliferation and invasion, making it an appropriate host for studying GPR171’s role in esophageal cancer.
GPR171 encodes a Gi/o-coupled receptor activated by the BigLEN neuropeptide, which is proteolytically processed from the proSAAS precursor. Upon BigLEN binding, GPR171 couples to G??i/o proteins and recruits ??-arrestin, leading to inhibition of adenylyl cyclase and a reduction in intracellular cAMP levels. This attenuation of cAMP signaling relieves tonic inhibition on effector pathways, resulting in altered phosphorylation of ERK and Akt, key nodes in MAPK/ERK and PI3K/Akt cascades. Consequently, GPR171 modulates cellular processes including proliferation, survival, and metabolic adaptation, positioning it at the intersection of neuropeptide and cancer signaling.
In the TE1 ESCC model, GPR171 knockout provides a powerful tool to investigate how this receptor contributes to tumor biology. Esophageal squamous cell carcinomas frequently exhibit dysregulated GPCR signaling, and GPR171 may sustain oncogenic signaling through cAMP-dependent and -independent mechanisms. Because the receptor is also implicated in metabolic regulation via BigLEN, this knockout model is well-suited for exploring links between obesity, metabolic syndrome, and esophageal cancer, offering potential insights into tumor metabolism and therapeutic vulnerabilities.
Research applications span functional genomics, metabolic regulation, and preclinical target validation. Typical assays include cAMP accumulation assays to quantify G??i activity, Western blot analysis of phospho-ERK (Thr202/Tyr204) and phospho-Akt (Ser473), cell proliferation (MTT/CCK-8), migration (wound healing), and invasion (transwell) assays. Gene expression studies via RT-qPCR or RNA-seq, receptor surface expression by flow cytometry, and drug sensitivity testing further expand the utility of this polyclonal knockout population. For additional information, please reach out to Ascent Research.