Molecular basis of ligand selectivity for melatonin receptors
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 …
and increased mortality. About 30–40% of adults are suffering from different sleep disorders …
Quantum mechanics insights into melatonin and analogs binding to melatonin MT1 and MT2 receptors
G de Lima Menezes, K Sales Bezerra… - Scientific Reports, 2024 - nature.com
Melatonin receptors MT1 and MT2 are G protein-coupled receptors that mediate the effects
of melatonin, a hormone involved in circadian rhythms and other physiological functions …
of melatonin, a hormone involved in circadian rhythms and other physiological functions …
Structural basis of the ligand binding and signaling mechanism of melatonin receptors
Q Wang, Q Lu, Q Guo, M Teng, Q Gong, X Li… - Nature …, 2022 - nature.com
Melatonin receptors (MT1 and MT2 in humans) are family AG protein–coupled receptors that
respond to the neurohormone melatonin to regulate circadian rhythm and sleep. Numerous …
respond to the neurohormone melatonin to regulate circadian rhythm and sleep. Numerous …
Structure-based discovery of potent and selective melatonin receptor agonists
Melatonin receptors MT1 and MT2 are involved in synchronizing circadian rhythms and are
important targets for treating sleep and mood disorders, type-2 diabetes and cancer. Here …
important targets for treating sleep and mood disorders, type-2 diabetes and cancer. Here …
A molecular and chemical perspective in defining melatonin receptor subtype selectivity
KH Chan, YH Wong - International Journal of Molecular Sciences, 2013 - mdpi.com
Melatonin is primarily synthesized and secreted by the pineal gland during darkness in a
normal diurnal cycle. In addition to its intrinsic antioxidant property, the neurohormone has …
normal diurnal cycle. In addition to its intrinsic antioxidant property, the neurohormone has …
Recent advances in the development of melatonin MT1 and MT2 receptor agonists
Importance of the field: Increasing clinical evidences suggest that melatonin receptor
agonists can represent a novel therapeutic approach for the treatment of sleep disturbances …
agonists can represent a novel therapeutic approach for the treatment of sleep disturbances …
Melatonin receptor structures shed new light on melatonin research
The tryptophan derivative melatonin is an evolutionary old molecule that is involved in a
pleiotropy of physiological functions. In humans, age‐related decline of circulating melatonin …
pleiotropy of physiological functions. In humans, age‐related decline of circulating melatonin …
Structural insights into melatonin receptors
The long‐anticipated high‐resolution structures of the human melatonin G protein‐coupled
receptors MT1 and MT2, involved in establishing and maintaining circadian rhythm, were …
receptors MT1 and MT2, involved in establishing and maintaining circadian rhythm, were …
Characterization of the various functional pathways elicited by synthetic agonists or antagonists at the melatonin MT1 and MT2 receptors
C Legros, C Dupré, C Brasseur… - Pharmacology …, 2020 - Wiley Online Library
Melatonin is a neurohormone that translates the circadian rhythm to the peripheral organs
through a series of binding sites identified as G protein‐coupled receptors MT1 and MT2 …
through a series of binding sites identified as G protein‐coupled receptors MT1 and MT2 …
N‐(Anilinoethyl)amide Melatonergic Ligands with Improved Water Solubility and Metabolic Stability
The MT2‐selective melatonin receptor ligand UCM765 (N‐(2‐((3‐methoxyphenyl)(phenyl)
amino) ethyl) acetamide), showed interesting sleep inducing, analgesic and anxiolytic …
amino) ethyl) acetamide), showed interesting sleep inducing, analgesic and anxiolytic …