Molecular basis of ligand selectivity for melatonin receptors.

ABSTRACT: Sleep disorders in adults are related to adverse health effects such as reduced quality of life and increased mortality. About 30-40% of adults are suffering from different sleep disorders. The human melatonin receptors (MT1 and MT2) are family A G protein-coupled receptors that respond to the neurohormone melatonin MEL which regulates circadian rhythm and sleep. Many efforts have been made to develop drugs targeting melatonin receptors to treat insomnia, circadian rhythm disorders, and even cancer. However, designing subtype-selective melatonergic drugs remains challenging due to their high similarities in both sequences and structures. MEL (a function-selective compound with a bulky β-naphthyl group) behaves as an MT2-selective antagonist, whereas it is an agonist of MT1. Here, molecular

SUBMITTER: Cui W 

PROVIDER: S-EPMC9891099 | biostudies-literature | 2023 Jan

REPOSITORIES: biostudies-literature