The human MT1 and MT2 melatonin receptors1,2 are G-proteincoupled receptors (GPCRs) that help to regulate circadian rhythm and sleep patterns. Drug development efforts have targeted both receptors for the treatment of insomnia, circadian rhythm and mood disorders, and cancer, and MT2 has also been implicated in type 2 diabetes.
Melatonin is produced by the pineal gland in the center of the brain. Humans respond naturally to changes in sunlight through the pineal gland near the hypothalamus. As night falls, the glands produce more melatonin and then bind to the MT1 and MT2 receptors of the cells. Before dawn, the gland will lower the level of melatonin, which indicates that it is time to wake up.
Recently, a team of international scientists has developed a new method for treating sleep disorders based on two new 3D models of melatonin receptors.
The researchers created a 3D map of two melatonin receptors MT1 and MT2. They hope to use this information to design drug molecules that bind to melatonin receptors and monitor their potential effects. This will treat a variety of diseases in a more targeted manner, including diabetes, cancer and sleep disorders.
"By comparing the three-dimensional structure of the MT1 and MT2 receptors, we can better distinguish the unique structural differences between the two receptors and their role in the circadian clock. With this knowledge, the design is only one or Another receptor binds, but the drug-like molecules that do not simultaneously bind to the two receptors become easier. This selective binding is important because it reduces unwanted side effects." the researcher said:
The structure of these two receptors was obtained by using a laser called the LCLS linear continuous accelerator source in the SLAC National Accelerator Laboratory. This laser uses X-rays to capture stop-work photos of receptor atoms and molecules in motion.