GPBAR1

Overview

GPBAR1 (G Protein-Coupled Bile Acid Receptor 1), also known as TGR5, is a membrane-bound receptor activated by bile acids. Its role in cholangiocarcinoma (CCA) is context-dependent: hepatoprotective in early cholestasis but pro-tumorigenic in advanced CCA, where it promotes apoptosis resistance via PKA/CD95 signaling.

Alterations observed in the corpus

• Context-dependent role in cholangiocarcinoma: hepatoprotective in early cholestasis (M2 macrophage polarization, NF-kB suppression) but pro-tumorigenic in advanced CCA (apoptosis resistance via PKA/CD95); transactivates EGFR via Src signaling to amplify ERK1/2 proliferative signaling in cholangiocytes; antagonist SBI-115 reduces pro-fibrotic and metastatic signaling PMID:25608663

Cancer types (linked)

• CCA: Pro-tumorigenic in advanced cholangiocarcinoma; antagonist SBI-115 reduces pro-fibrotic and metastatic signaling PMID:25608663

Co-occurrence and mutual exclusivity

• Linked partner genes with the relationship and the paper(s) reporting it.

Therapeutic relevance

• Antagonist SBI-115 reduces pro-fibrotic and metastatic signaling in advanced CCA PMID:25608663

Open questions

• Conflicts or unresolved findings across papers.

Sources

• PMID:25608663

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