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GPBAR1 agonism has a broad impact on blocking macrophage activation


ABSTRACT: Human D14+ / CD16+ monocytes were treated with GPBAR1 agonists or controls, and were stimulated with interferon gamma and LPS. At 6 and 24 hours, the cells were profiled by RNAseq 40 total samples, 5 per group with eight groups. Individual donors used for multiple comparisons, so paired analysis is possible. Control samples include unstimulated cells, and stimulated cells treated with vehicle control (DMSO).

ORGANISM(S): Homo sapiens

SUBMITTER: Jonathan Hill 

PROVIDER: E-GEOD-57494 | biostudies-arrayexpress |

REPOSITORIES: biostudies-arrayexpress

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Publications

A GPBAR1 (TGR5) small molecule agonist shows specific inhibitory effects on myeloid cell activation in vitro and reduces experimental autoimmune encephalitis (EAE) in vivo.

Lewis Nuruddeen D ND   Patnaude Lori A LA   Pelletier Josephine J   Souza Donald J DJ   Lukas Susan M SM   King F James FJ   Hill Jonathan D JD   Stefanopoulos Dimitria E DE   Ryan Kelli K   Desai Sudha S   Skow Donna D   Kauschke Stefan G SG   Broermann Andre A   Kuzmich Daniel D   Harcken Christian C   Hickey Eugene R ER   Modis Louise K LK  

PloS one 20140626 6


GPBAR1 is a G protein-coupled receptor that is activated by certain bile acids and plays an important role in the regulation of bile acid synthesis, lipid metabolism, and energy homeostasis. Recent evidence suggests that GPBAR1 may also have important effects in reducing the inflammatory response through its expression on monocytes and macrophages. To further understand the role of GPBAR1 in inflammation, we generated a novel, selective, proprietary GPBAR1 agonist and tested its effectiveness at  ...[more]

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