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Updated: May 19, 2026

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
G protein-coupled receptor FPR1 as a pharmacologic target in inflammation and human glioblastoma
Mingyong Liu1, Jianhua Zhao, Keqiang Chen
1Department of Spine Surgery, Daping Hospital, Third Military Medical University, Chongqing 400042, China.
Abstract:
Formylpeptide receptor1 (FPR1) is a G protein-coupled receptor (GPCR) originally identified in phagocytic leucocytes and mediates cell chemotaxis and activation in response to bacterial formylated chemotactic peptides. However, FPR1 also participates in a signal relay which regulates the infiltration of phagocytes, in particular neutrophils, to inflammatory sites in response to tissue-derived chemoattractant ligands. In addition to participating in innate immune responses, recently, FPR1 has been shown to be expressed by highly malignant glioblastoma (GBM) cells. Upon activation by an endogenous agonist Annexin 1 (Anx A1) released by necrotic glioma cells, FPR1 transactivates the receptor for epithelial growth factor (EGFR) and consequently to promote glioma cell chemotaxis, invasion, growth and production of angiogenic factors. The observations demonstrate that FPR1, as a multifunctional GPCR with pattern recognition properties, is not only involved in innate immune responses but also in the progression of GBM. Thus, FPR1 is an immunopharmacologic target for development of novel therapies.
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