Molecular basis defining the selectivity of substituted isoquinolinones for the melatonin MT2 receptor

KH Chan, HT Lap, X Huang, YH Wong - Biochemical Pharmacology, 2020 - Elsevier
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 …

Development of substituted N-[3-(3-methoxylphenyl) propyl] amides as MT2-selective melatonin agonists: Improving metabolic stability

Y Hu, J Zhu, KH Chan, YH Wong - Bioorganic & medicinal chemistry, 2013 - Elsevier
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 …

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 …

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 receptors, heterodimerization, signal transduction and binding sites: what's new?

R Jockers, P Maurice, JA Boutin… - British journal of …, 2008 - Wiley Online Library
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 …

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 …

N‐(Anilinoethyl)amide Melatonergic Ligands with Improved Water Solubility and Metabolic Stability

F Ferlenghi, M Mari, G Gobbi, GM Elisi, M Mor… - …, 2021 - Wiley Online Library
The MT2‐selective melatonin receptor ligand UCM765 (N‐(2‐((3‐methoxyphenyl)(phenyl)
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 …

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 …

Ligand efficacy and potency at recombinant human MT2 melatonin receptors: evidence for agonist activity of some mt1‐antagonists

R Nonno, M Pannacci, V Lucini… - British journal of …, 1999 - Wiley Online Library
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 …