What does TGR5 do?

1. Introduction. The TGR5 receptor is the first known G-protein coupled receptor specific for bile acids. Since its identification in 2002, TGR5 has been found to be ubiquitously expressed in humans and animals, and to activate various intracellular signalling pathways upon interaction with bile acids.

Where is TGR5 expressed?

TGR5 is widely expressed in many tissues including intestine, gallbladder, liver, and brain [26–28]. In the liver, TGR5 is expressed in Kupffer cells and sinusoidal endothelial cells, but not in hepatocytes [28, 29].

What is a TGR5 agonist?

TGR5 Receptor Agonist is a synthetic cell-permeable small molecule agonist for the G protein-coupled bile acid receptor TGR5 (pEC50=6.8-7.5nM). Improves glucagon like peptide-1 (GLP-1) secretion from intestinal cells, and mediates energy balance, inflammation, and digestion.

How do I activate TGR5?

TGR5 can be activated by bile acids and then it induces cAMP production (Maruyama et al., 2002). As a membrane receptor, TGR5 can be internalized into the cytoplasm in response to its ligands (Kawamata et al., 2003).

What are the two types of bile salts?

There are four types of bile salts: primary and secondary, conjugated, and non-conjugated (2, 3). Conjugation involves the formation of an amide bond with either taurine or glycine. Primary bile salts are the immediate products of cholesterol degradation.

What are the two bile pigments?

The two main pigments of bile are bilirubin, which is yellow, and its oxidised form biliverdin, which is green. When mixed, they are responsible for the brown color of feces. About 400 to 800 millilitres of bile is produced per day in adult human beings.

What are examples of bile salts?

In humans, taurocholic acid and glycocholic acid (derivatives of cholic acid) and taurochenodeoxycholic acid and glycochenodeoxycholic acid (derivatives of chenodeoxycholic acid) are the major bile salts.

What are the names of bile salts?

Bile salts are composed of the salts of four different kinds of free bile acids (cholic, deoxycholic, chenodeoxycholic, and lithocholic acids); each of these acids may in turn combine with glycine or taurine to form more complex acids and salts. Bile salts and acids can…

What is bile pigment example?

The bile pigments are formed by decomposition of the porphyrin ring and contain a chain of four pyrrole rings. Bilirubin, for example, the brownish yellow pigment that gives feces its characteristic colour, is the end product of the breakdown of heme from destroyed red blood cells.

What is biliverdin and bilirubin?

Bilirubin is generated from the breakdown of heme present in hemoproteins (e.g., hemoglobin and myoglobin) that is released from the catabolism of red blood cells. The heme ring is broken open by heme oxygenase forming biliverdin, which is reduced to bilirubin by biliverdin reductase (BVR; Fig. 1; 104).

What are the two bile salts?

The primary bile salts in humans, i.e., synthesized de novo from cholesterol in the liver, are cholate and chenodeoxycholate. The primary bile salts are excreted via de bile into the intestine.