Enterically Delivered Bitter Oligopeptides for the Treatments of Type 2 Diabetes

Tech ID: pan000897



The growing epidemic of Type 2 diabetes mellitus (T2DM) and other obesity-related metabolic disorders requires radical and impactful therapeutic solutions rooted in fundamental molecular mechanisms. One such radical solution with wide-ranging impact on prevention and treatment of T2DM is within reach and is based on understanding the dramatic reversal of T2DM in bariatric surgery patients that is thought to be caused, at least in part, by an augmentation of the meal-induced increases in the gut hormones glucagon-like peptide-1 (GLP-1) and peptide tyrosine tyrosine (PYY) released from enteroendocrine L cells. Systemic effects of both GLP-1 and PYY hormones involve inhibition of gastric emptying and appetite. GLP-1 also causes stimulation of insulin secretion and inhibition of glucagon secretion. There is growing evidence for the presence of nutrient-sensing chemosensory receptors on gut enteroendocrine cells, including the L-cells located in the distal small intestine and colon. To highlight a few nutrient receptors, the G protein-coupled receptors (GPCRs) for sensing taste (bitter, sweet, umami) and free fatty acids or their G protein effectors have been shown to be present in these L-cells in human and animal intestinal cell lines and tissues.


Technology Description

Inventors have previously identified that the GI lumen location of TAS2R38 on the L-cell makes it a relatively safe drug target as systemic absorption is not needed for a TAS2R38 agonist drug to effect GLP-1 release. They have investigated the mechanistic role of bitter taste receptor TAS2R38 in the release of the GLP-1 hormone from L-cells. The inventors have identified four novel bitter oligopeptides that may be used as therapeutic agents in patients with type 2 diabetes.


Stage of Development

Preclinical; in-vivo animal data available.



Novel oliogopeptides are safe (derived from food) with limited adverse effects.



Novel compositions to treat Type 2 Diabetes.


Intellectual Property

PCT application PCT/US2016/028841 filed.



Patent Information:
For Information, Contact:
Wenyue Du
Associate - IP Management & Licensing
Stephen Pandol
Ravinder Abrol
Hung Pham