Glucagon-Like Peptide 1 Receptor or GLP1-R uses the glucagon-like peptide to signal the body to secrete insulin and inhibit glucagon secretion. When glucose levels in the blood rise (usually after consuming food), GLP-1R activates, creating a signaling cascade to signal cAMP. After the signaling cascade, the final result is the secretion of insulin to the rest of the body. Discovered in 1990s while trying to understand the mechanism of GLP-1 action. The structure was determined using cryogenic electron microscopy.

Function

GLP-1R works in conjunction with GIP-R to maintain blood glucose levels after the ingestion of food. It is imperative for these receptors to work well so diseases like diabetes and obesity do not ensue.

uses pi stacking and hydrophilic interactions to dock into the receptor.

Disease

Diabetes and Obesity

Type II Diabetes is when the pancreas does not produce enough insulin for the body.[1] This in turn makes the blood glucose level dangerously low. When the sugar levels in our blood become too low people can become dizzy and tired. On the other hand, when blood sugar levels become too high then can become feverish and sick.

Ligand and Receptor Interactions

Hormone Interactions

Drug Interactions

Relevance

Tirzepatide and other GLP-1R related antagonist drugs help to regulate blood glucose levels. Although these drugs can make remarkable changes, the long term effects of GLP-1R related drugs are unknown. There have been some hints toward thyroid cancers but this was only shown in mice during trial periods.

References