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 …
Development of substituted N-[3-(3-methoxylphenyl) propyl] amides as MT2-selective melatonin agonists: Improving metabolic stability
A series of novel and selective N-[3-(6-benzyloxy-3-methoxyphenyl) propyl] amides has
recently been shown to possess sub-nanomolar range binding affinity to the type 2 …
recently been shown to possess sub-nanomolar range binding affinity to the type 2 …
Differences in binding sites of two melatonin receptors help to explain their selectivity to some melatonin analogs: a molecular modeling study
AO Chugunov, A Farce, P Chavatte… - Journal of Biomolecular …, 2006 - Taylor & Francis
Numerous diseases have been linked to the malfunction of G-protein coupled receptors (GP-
CRs). Their adequate treatment requires rational design of new high-affinity and high …
CRs). Their adequate treatment requires rational design of new high-affinity and high …
Benzocyclobutane, benzocycloheptane and heptene derivatives as melatonin agonists and antagonists
A Tsotinis, PA Afroudakis, PJ Garratt… - …, 2014 - Wiley Online Library
Two series of analogues were designed, synthesised and evaluated as potential human
melatonin type 1 and 2 receptor (hMT1 and hMT2) ligands. Their biological effects were …
melatonin type 1 and 2 receptor (hMT1 and hMT2) ligands. Their biological effects were …
Melatonin receptors, heterodimerization, signal transduction and binding sites: what's new?
Melatonin is a neurohormone that has been claimed to be involved in a wide range of
physiological functions. Nevertheless, for most of its effects, the mechanism of action is not …
physiological functions. Nevertheless, for most of its effects, the mechanism of action is not …
Important amino acids for the function of the human MT1 melatonin receptor
T Kokkola, SM Foord, MA Watson, O Vakkuri… - Biochemical …, 2003 - Elsevier
Models of G protein-coupled melatonin receptor structure suggest that ligand recognition
occurs in a binding pocket formed by transmembrane helices III, V and VII. Constitutively …
occurs in a binding pocket formed by transmembrane helices III, V and VII. Constitutively …
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 …
N-{2-[2-(4-Phenylbutyl) benzofuran-4-yl] cyclopropylmethyl} acetamide: an orally bioavailable melatonin receptor agonist
LQ Sun, K Takaki, J Chen, L Iben, JO Knipe… - Bioorganic & medicinal …, 2004 - Elsevier
N-{2-[2-(4-Phenylbutyl)benzofuran-4-yl]cyclopropylmethyl}acetamide: an orally bioavailable
melatonin receptor agonist - ScienceDirect Skip to main contentSkip to article Elsevier logo …
melatonin receptor agonist - ScienceDirect Skip to main contentSkip to article Elsevier logo …
Design and validation of the first family of photo-activatable ligands for melatonin receptors
G Somalo-Barranco, C Serra, D Lyons… - Journal of medicinal …, 2022 - ACS Publications
Melatonin is a neurohormone released in a circadian manner with peak levels at night.
Melatonin mediates its effects mainly through G protein-coupled MT1 and MT2 receptors …
Melatonin mediates its effects mainly through G protein-coupled MT1 and MT2 receptors …
Ligand efficacy and potency at recombinant human MT2 melatonin receptors: evidence for agonist activity of some mt1‐antagonists
NIH3T3 fibroblast cells transfected with the full‐length coding region of the MT2 human
melatonin receptor stably expressed the receptor that is coupled to a pertussis toxin …
melatonin receptor stably expressed the receptor that is coupled to a pertussis toxin …