Targeting G-protein-coupled receptor GPR119, summary 2010 and 2011

Diabetes mellitus is a group of disorders characterized by abnormal glucose homeostasis, resulting in high levels of blood glucose. The most common cases of diabetes mellitus are Type I and Type II. 


- Type I diabetes, also known as insulin-dependent diabetes mellitus, is caused by the autoimmune destruction of the insulin producing pancreatic beta-cells, and requires regular administration of exogenous insulin. Type I diabetes usually starts in childhood or young adulthood manifesting sudden symptoms of high blood sugar (hyperglycemia).

 

- Type II diabetes, also known as non-insulin-dependent diabetes mellitus, manifests with an inability to adequately regulate blood-glucose levels. Type II diabetes may be characterized by a defect in insulin secretion or by insulin resistance.

 

Insulin resistance refers to the inability of body tissues to respond properly to endogenous insulin. Insulin resistance develops because of multiple factors, including genetics, obesity, increasing age, and having high blood sugar over long periods of time.  

Type II diabetes, sometimes called mature or adult onset diabetes, can develop at any age, but most commonly becomes apparent during adulthood. However, the incidence of Type II diabetes in children is rising.  

 

GPR119 is a constitutively active G-protein coupled receptor. In humans, GPR119 is expressed in the pancreas and intestinal tissues. Independently, GPR119 has been studied and described in the literature under various synonyms including SNORF25, RUP3, GPCR2, 19AJ, OSGPR116, and glucose-dependent insulinotropic receptor. 

 

GPR119 agonists have been shown to stimulate the release of GLP-1* from the GI tract. By doing this, GPR119 agonists,

- Enhance glucose-dependent insulin release from the pancreas, leading to improvements in oral glucose tolerance;

- Attenuate disease progression by increasing b-cells cAMP concentrations;

- Induce weight loss, possibly through GLP-1’s ability to reduce food intake.  

 

Then, GPR119 agonists could prove valuable agents for the treatment of type II diabetes and obesity by improving glucose homoeostasis while concurrently limiting food intake and body weight gain.

 

*The incretin hormone, GLP-1 is a powerful antihyperglycaemic agent.

Company Patent number
BOEHRINGER INGELHEIM INTERNATIONAL GMBH WO2010029089
BRISTOL-MYERS SQUIBB COMPANY WO2010009183
IRM LLC WO2010006191
KALYPSYS, INC WO2010048149
KALYPSYS, INC WO2010088518 
METABOLEX, INC. WO2010008739
NIPPON CHEMIPAR CO., LTD. WO2010013849
NIPPON CHEMIPAR CO., LTD. WO2010123018
PFIZER INC. WO2010106457
PFIZER INC. WO2010128414
PFIZER INC. WO2010128425
PFIZER INC. WO2010140092
PROSIDION LIMITED WO2010001166
PROSIDION LIMITED WO2010004347
PROSIDION LIMITED WO2010004348
PROSIDION LIMITED WO2010103333
PROSIDION LIMITED WO2010103334
PROSIDION LIMITED WO2010103335
SCHERING CORPORATION WO2010009195
SMITHKLINE BEECHAM CORPORATION WO2010014593
TAKEDA PHARMACEUTICAL COMPANY LIMITED WO2010074271
TAKEDA PHARMACEUTICAL COMPANY LIMITED WO2010095663
ARENA PHARMACEUTICALS, INC. WO2011005929
ASTRAZENECA AB WO2011030139
ELI LILLY AND COMPANY WO2011008663
IRM LLC. WO2011014520
NIPPON CHEMIPHAR CO., LTD. WO2011025006
PFIZER INC. WO2011036576
SCHERING CORPORATION WO2011053688
TAKEDA PHARMACEUTICAL COMPANY LIMITED WO2011055770

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