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 …
2-Arylmelatonin analogues: Probing the 2-phenyl binding pocket of melatonin MT1 and MT2 receptors
In crystal structures of melatonin MT 1 and MT 2 receptors, a lipophilic subpocket has been
characterized which accommodates the phenyl ring of the potent agonist 2-phenylmelatonin …
characterized which accommodates the phenyl ring of the potent agonist 2-phenylmelatonin …
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 …
Molecular basis defining the selectivity of substituted isoquinolinones for the melatonin MT2 receptor
Melatonin MT 1 and MT 2 receptors represent attractive drug targets for the treatment of
various disorders. However, the high conservation of the melatonin binding pocket has …
various disorders. However, the high conservation of the melatonin binding pocket has …
Design and Synthesis of N-(3,3-Diphenylpropenyl)alkanamides as a Novel Class of High-Affinity MT2-Selective Melatonin Receptor Ligands
A novel series of melatonin receptor ligands was discovered by opening the cyclic scaffolds
of known classes of high affinity melatonin receptor antagonists, while retaining the …
of known classes of high affinity melatonin receptor antagonists, while retaining the …
Synthesis, pharmacological characterization and QSAR studies on 2-substituted indole melatonin receptor ligands
A number of 6-methoxy-1-(2-propionylaminoethyl) indoles, carrying properly selected
substituents at the C-2 indole position, were prepared and tested as melatonin receptor …
substituents at the C-2 indole position, were prepared and tested as melatonin receptor …
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 …
Three-Dimensional Quantitative Structure−Activity Relationship Studies on Selected MT1 and MT2 Melatonin Receptor Ligands: Requirements for Subtype …
The three-dimensional quantitative structure− activity relationship comparative molecular
field analysis (3D-QSAR CoMFA) approach was applied to some classes of melatonin (MLT) …
field analysis (3D-QSAR CoMFA) approach was applied to some classes of melatonin (MLT) …
New MT2 Melatonin Receptor-Selective Ligands: Agonists and Partial Agonists
JA Boutin, A Bonnaud, C Brasseur, O Bruno… - International Journal of …, 2017 - mdpi.com
The search for melatonin receptor agonists and antagonists specific towards one of the
receptor subtypes will extend our understanding of the role of this system in relaying …
receptor subtypes will extend our understanding of the role of this system in relaying …
Structural Basis for Agonistic Activity and Selectivity toward Melatonin Receptors hMT1 and hMT2
M Cantarini, D Rusciano, R Amato, A Canovai… - International Journal of …, 2023 - mdpi.com
Glaucoma, a major ocular neuropathy originating from a progressive degeneration of retinal
ganglion cells, is often associated with increased intraocular pressure (IOP). Daily IOP …
ganglion cells, is often associated with increased intraocular pressure (IOP). Daily IOP …