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October 2022 Regulation of pulmonary surfactant by the adhesion GPCR GPR116/ADGRF5 requires a tethered mechanism "The mechanistic details of the tethered agonist mode of activation for the adhesion GPCR ADGRF5/GPR116 To examine this hypothesis, we characterized tethered agonist-mediated activation of GPR116 in vitro A knock-in mouse expressing a non-cleavable GPR116 mutant phenocopies the pulmonary phenotype of GPR116 and recapitulate these findings in a model supporting tethered agonist:ECL2 interactions for GPR116

Signaling by Neutrophil G Protein-Coupled Receptors that Regulate the Release of Superoxide Anions GPR176

GPCRs in Oncology and Immunology GPR176 Promotes Cancer Progression by Interacting with G Protein GNAS

< GPCR News < GPCRs in Oncology and Immunology GPR176 Promotes Cancer Progression by Interacting with Protein GNAS to Restrain Cell Mitophagy in Colorectal Cancer Published date March 11, 2023 Abstract " GPR176 In the present study, expression analyses of GPR176 are performed in patients with colorectal cancer. Genetic mouse models of CRC coupled with Gpr176-deficiency are investigated, and in vivo and in vitro A positive correlation between GPR176 upregulation and the proliferation and poor overall survival of

< GPCR News < GPCRs in Oncology and Immunology GPR176 promotes fibroblast-to-myofibroblast transition Among them, we focused on Gpr176 owing to its significant correlation with a myofibroblast marker α-smooth Furthermore, fibroblasts abundantly expressed Gpr176 compared to alveolar epithelial cells, endothelial of Gpr176 by siRNA reduced TGFβ1-induced expression of αSMA, fibronectin, and collagen as well as Smad2 This suggested that Gpr176 regulates fibroblast activation.

Brendan’s PhD project focuses on the orphan GPCR GPR146. This project aims to characterise the molecular pharmacology of GPR146 and to validate the proposed ligands of GPR146 in line with IUPHAR-NC guidelines on deorphanisation of orphan GPCRs.