GPBAR1 (TGR5) regulates production of the anti-inflammatory cytokine IL-10 from intestinal macrophages and attenuates inflammation in models of Crohn's disease. Activation of GPBAR1 increases IL-10 production by promoting CREB phosphorylation and binding to the IL-10 promoter. Stimulation of GPBAR1 rescues mice from colitis by shifting intestinal macrophages from a pro-inflammatory M1 phenotype to an anti-inflammatory M2 phenotype.

1. GPBAR1 (TGR5) regulates IL-10 production from intestinal
macrophages and attenuates inflammation in Crohn disease models
PKa
CREB
BAR501
LCA
DCA CRE
IL-10 promoter
IL-10
P-CREB
The Bile Acid Receptor GPBAR1 Regulates the M1/M2 Phenotype of Intestinal Macrophages and Activation of GPBAR1 Rescues Mice from Murine Colitis
Michele Biagioli, Adriana Carino, Sabrina Cipriani, Daniela Francisci, Silvia Marchianò, Paolo Scarpelli, Daniele Sorcini, Angela Zampella and Stefano Fiorucci
J Immunol June 12, 2017, ji1700183; DOI: https://doi.org/10.4049/jimmunol.1700183
GPBAR1