Table 1.
Summary of related TGR5 information.
Gene | GPBAR1, 2q35 | ||||
---|---|---|---|---|---|
Expression in human tissues | Placenta, Spleen, Small intestine, Stomach, Liver, Lung, Heart, Skeletal muscle, Kidney, Peripheral blood leukocytes | ||||
Natural agonists | Name | Structures | References | ||
Primary bile acid | CA | ![]() |
Kawamata et al., 2003 | ||
CDCA | ![]() |
Kawamata et al., 2003 | |||
Secondary bile acid | LCA | ![]() |
Kawamata et al., 2003 | ||
TLCA | ![]() |
Kawamata et al., 2003 | |||
DCA | ![]() |
Kawamata et al., 2003 | |||
Natural phytochemical agonists | Linolenic acid | ![]() |
Katsuma et al., 2005 | ||
OA | ![]() |
Sato et al., 2007 | |||
Obacunone | ![]() |
Horiba et al., 2015 | |||
Synthetic agonists | INT-777 | ![]() |
Pellicciari et al., 2009 | ||
TRC210258 | ![]() |
Zambad et al., 2013 | |||
WB403 | ![]() |
Zheng et al., 2015 | |||
Relevant diseases | Agonists | References | |||
Type 2 diabetes | LCA, DCA, Lionlenic acid, OA, INT-777, WB403 | Katsuma et al., 2005; Sato et al., 2007; Perino et al., 2014; Zheng et al., 2015 | |||
Obesity | CA, TCA, DCA, CDCA | Watanabe et al., 2006 | |||
Inflammation | Betulinic acid, 23(S)-mCDCA, TLCA, TLC, CDCA, DCA | Kawamata et al., 2003; Keitel et al., 2008; Wang et al., 2011; Mobraten et al., 2015; Guo et al., 2015b; McMillin et al., 2015 | |||
Gastric cancer | 23(S)-mCDCA, GPBARA | Guo et al., 2015a | |||
Liver regeneration | CA | Péan et al., 2013 |