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 …
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 …
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 …
In silico drug discovery of melatonin receptor ligands with therapeutic potential
Introduction The neurohormone melatonin (N-acetyl-5-methoxytryptamine) regulates
circadian rhythms exerting a variety of effects in the central nervous system and in periphery …
circadian rhythms exerting a variety of effects in the central nervous system and in periphery …
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 …
MT1‐Selective Melatonin Receptor Ligands: Synthesis, Pharmacological Evaluation, and Molecular Dynamics Investigation of N‐{[(3‐O‐Substituted)anilino]alkyl} …
The design of compounds selective for the MT1 melatonin receptor is still a challenging task
owing to the limited knowledge of the structural features conferring selectivity for the MT1 …
owing to the limited knowledge of the structural features conferring selectivity for the MT1 …
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 …
Highly Potent and Selective MT2 Melatonin Receptor Full Agonists from Conformational Analysis of 1-Benzyl-2-acylaminomethyl-tetrahydroquinolines
Molecular superposition models guided the design of novel melatonin receptor ligands
characterized by a 2-acylaminomethyltetrahydroquinoline scaffold. Starting from the …
characterized by a 2-acylaminomethyltetrahydroquinoline scaffold. Starting from the …
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 …
MT1 and MT2 Melatonin Receptors: Ligands, Models, Oligomers, and Therapeutic Potential
Numerous physiological functions of the pineal gland hormone melatonin are mediated via
activation of two G-protein-coupled receptors, MT1 and MT2. The melatonergic drugs on the …
activation of two G-protein-coupled receptors, MT1 and MT2. The melatonergic drugs on the …