GPR119
Encyclopedia
G protein-coupled receptor 119 also known as GPR119 is a G protein-coupled receptor
that in humans is encoded by the GPR119 gene
.
GPR119, along with GPR55
and GPR18
, have been implicated as novel cannabinoid receptor
s.
and gastrointestinal tract
in rodents and humans, as well as in the brain
in rodents. Activation of the receptor has been shown to cause a reduction in food intake and body weight gain in rats. GPR119 has also been shown to regulate incretin
and insulin
hormone
secretion. As a result, new drugs acting on the receptor have been suggested as novel treatments for obesity
and diabetes.
and synthetic
ligand
s for this receptor have been identified:
G protein-coupled receptor
G protein-coupled receptors , also known as seven-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein-linked receptors , comprise a large protein family of transmembrane receptors that sense molecules outside the cell and activate inside signal...
that in humans is encoded by the GPR119 gene
Gene
A gene is a molecular unit of heredity of a living organism. It is a name given to some stretches of DNA and RNA that code for a type of protein or for an RNA chain that has a function in the organism. Living beings depend on genes, as they specify all proteins and functional RNA chains...
.
GPR119, along with GPR55
GPR55
G protein-coupled receptor 55 also known as GPR55 is a G protein-coupled receptor that in humans is encoded by the GPR55 gene.GPR55, along with GPR119 and GPR18, have been implicated as novel cannabinoid receptors.- History :...
and GPR18
GPR18
N-arachidonyl glycine receptor also known as G-protein coupled receptor 18 is a protein that in humans is encoded by the GPR18 gene...
, have been implicated as novel cannabinoid receptor
Cannabinoid receptor
The cannabinoid receptors are a class of cell membrane receptors under the G protein-coupled receptor superfamily. As is typical of G protein-coupled receptors, the cannabinoid receptors contain seven transmembrane spanning domains...
s.
Pharmacology
GPR119 is expressed predominantly in the pancreasPancreas
The pancreas is a gland organ in the digestive and endocrine system of vertebrates. It is both an endocrine gland producing several important hormones, including insulin, glucagon, and somatostatin, as well as a digestive organ, secreting pancreatic juice containing digestive enzymes that assist...
and gastrointestinal tract
Gastrointestinal tract
The human gastrointestinal tract refers to the stomach and intestine, and sometimes to all the structures from the mouth to the anus. ....
in rodents and humans, as well as in the brain
Brain
The brain is the center of the nervous system in all vertebrate and most invertebrate animals—only a few primitive invertebrates such as sponges, jellyfish, sea squirts and starfishes do not have one. It is located in the head, usually close to primary sensory apparatus such as vision, hearing,...
in rodents. Activation of the receptor has been shown to cause a reduction in food intake and body weight gain in rats. GPR119 has also been shown to regulate incretin
Incretin
Incretins are a group of gastrointestinal hormones that cause an increase in the amount of insulin released from the beta cells of the islets of Langerhans after eating, even before blood glucose levels become elevated. They also slow the rate of absorption of nutrients into the blood stream by...
and insulin
Insulin
Insulin is a hormone central to regulating carbohydrate and fat metabolism in the body. Insulin causes cells in the liver, muscle, and fat tissue to take up glucose from the blood, storing it as glycogen in the liver and muscle....
hormone
Hormone
A hormone is a chemical released by a cell or a gland in one part of the body that sends out messages that affect cells in other parts of the organism. Only a small amount of hormone is required to alter cell metabolism. In essence, it is a chemical messenger that transports a signal from one...
secretion. As a result, new drugs acting on the receptor have been suggested as novel treatments for obesity
Obesity
Obesity is a medical condition in which excess body fat has accumulated to the extent that it may have an adverse effect on health, leading to reduced life expectancy and/or increased health problems...
and diabetes.
Ligands
A number of endogenousEndogenous
Endogenous substances are those that originate from within an organism, tissue, or cell. Endogenous retroviruses are caused by ancient infections of germ cells in humans, mammals and other vertebrates...
and synthetic
Chemical synthesis
In chemistry, chemical synthesis is purposeful execution of chemical reactions to get a product, or several products. This happens by physical and chemical manipulations usually involving one or more reactions...
ligand
Ligand
In coordination chemistry, a ligand is an ion or molecule that binds to a central metal atom to form a coordination complex. The bonding between metal and ligand generally involves formal donation of one or more of the ligand's electron pairs. The nature of metal-ligand bonding can range from...
s for this receptor have been identified:
- 2-Oleoylglycerol2-Oleoylglycerol2-Oleoylglycerol is a monoacylglycerol that is found in biologic tissues. Its synthesis is derived from diacylglycerol precursors. It is metabolized to oleic acid and glycerol primarily by the enzyme monoacylglycerol lipase . In 2011, 2OG was found to be an endogenous ligand to GPR119...
- AnandamideAnandamideAnandamide, also known as N-arachidonoylethanolamide or AEA, is an endogenous cannabinoid neurotransmitter. The name is taken from the Sanskrit word ananda, which means "bliss, delight", and amide. It is synthesized from N-arachidonoyl phosphatidylethanolamine by multiple pathways...
- AR-231,453AR-231,453AR-231,453 is an agonist for the suggested novel cannabinoid receptor GPR119....
- MBX-2982
- OleoylethanolamideOleoylethanolamideOleoylethanolamine is an endogenous peroxisome proliferator-activated receptor alpha agonist. It is a naturally occurring ethanolamide lipid that regulates feeding and body weight in vertebrates ranging from mice to pythons....
- PSN-375,963PSN-375,963PSN-375,963 is a selective ligand for the suggested novel cannabinoid receptor GPR119....
- PSN-632,408PSN-632,408PSN-632,408 is a selective ligand for the suggested novel cannabinoid receptor GPR119....
- PalmitoylethanolamidePalmitoylethanolamidePalmitoylethanolamide is an endogenous fatty acid amide, belonging to the class of endocannabinoids. PEA has been demonstrated to bind to a receptor in the cell-nucleus and exerts a great variety of biological functions related to chronic pain and inflammation. The main target is thought to be...